| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Celecoxib - SC 58635 | Celebrex | Celebra | Axon 1919
CAS [169590-42-5]
MF C17H14F3N3O2SMW 381.37
Purity:
99%
Soluble in DMSO
Description
Selective cyclooxygenase-2 (COX-2) inhibitor (IC50: 15 and 0.04 μM for COX-1 and COX-2 respectively); inhibition of COX-2 inhibits only prostaglandin synthesis without affecting thromboxane (TXA2) and thus offers no cardioprotective effects of NSAIDs, which inhibits both COX-1 and COX-2 non-selectively.
References
Certificates
Categories
Extra info
TD Penning et al. Synthesis and Biological Evaluation of the 1.5 Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazole-(...). J. Med. Chem. 1997, 40 (9), 1347–1365.
DL DeWitt. Cox-2-selective inhibitors: the new super aspirins. Mol. Pharmacol. 1999, 55(4), 625-631.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
EC 1.14.99.1
COX
Pfizer Licensed Products
Selective COX-2 inhibitor
Chemical name
4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[169590-42-5]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| Alpelisib - NVP-BYL719 | BYL-719 | Axon 2925
CAS [1217486-61-7]
MF C19H22F3N5O2SMW 441.47
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Alpelisib is a potent and selective PI3K α-isoform inhibitor with an IC50 value of 5 nM. Moreover, Alpelisib has shown good efficacy in inhibiting the growth of PI3K α-isoform driven tumors in animal xenograft models as well as good tolerability.
KEYWORDS: Alpelisib | supplier | PI3K inhibitor | NVP-BYL719 | BYL-719 | NVPBYL719 | BYL719 | BYL 719 | CAS [1217486-61-7] | CAS [1584128-91-5] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | | axonmedchem |
| AZD 6482 - KIN-193 | Axon 2926
CAS [1173900-33-8]
MF C22H24N4O4MW 408.45
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
AZD 6482 is a potent and selective inhibitor of the p110β isoform of PI3K with an IC50 value of 0.69 nM. In addition, AZD 6482 can inhibit the growth of tumors driven by p110β or PTEN-loss in vivo.
KEYWORDS: AZD 6482 | supplier | PI3K p110β inhibitor | KIN-193 | AZD6482 | AZD-6482 | KIN193 | KIN 193 | CAS [1173900-33-8] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | PTEN | | axonmedchem |
| ML 351 | Axon 2312
CAS [847163-28-4]
MF C15H11N3OMW 249.27
Purity:
98%
Soluble in DMSO
Description
Potent and selective inhibitor of 12/15-lipoxygenase (IC50 value 200 nM against human 12/15-LOX) with >250-fold selectivity versus related LOX isozymes. ML351 is protective against oxidative glutamate toxicity in mouse neuronal HT22 cells and does not reduce the active-site ferric ion. ML 351 significantly reduced infarct size following permanent focal ischemia in a mouse model of ischemic stroke
References
Certificates
Categories
Extra info
G. Rai et al. Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies. J. Med. Chem. 2014, 57, 4035-4048.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cardiovascular
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Pain & Inflammation
LOX
EC 1.13.11.31
Potent and selective inhibitor of 12/15-lipoxygenase (LOX)
Chemical name
5-(methylamino)-2-(naphthalen-1-yl)oxazole-4-carbonitrile
Parent CAS No.
[847163-28-4]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| SC 236 - SC 58236 | Axon 2108
CAS [170569-86-5]
MF C16H11ClF3N3O2SMW 401.79
Purity:
99%
Soluble in DMSO
Description
Selective COX-2 inhibitor, which showed an impressive selectivity for COX-2 over COX-1 (IC50 0.01 µM vs. 17.8 µM respectively); NSAID and early lead compound during the discovery of Celecoxib (Axon 1919). However, SC236 showed an extremely long plasma half-life, not preferred for further development as potential therapeutic
References
Certificates
Categories
Extra info
TD Penning et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene (...). J. Med. Chem. 1997, 40(9), 1347-1365.
A Planagumà et al. The selective cyclooxygenase-2 inhibitor SC-236 reduces liver fibrosis by mechanisms involving non-parenchymal cell apoptosis and PPARγ activation. FASEB J. 2005, 19(9), 1120-1122.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
EC 1.14.99.1
COX
Pfizer Licensed Products
Selective COX-2 inhibitor
Chemical name
4-(5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[170569-86-5]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| ATB 346 | Axon 2288
CAS [1226895-20-0]
MF C21H19NO3SMW 365.45
Purity:
99%
Soluble in DMSO
Description
Orally active hydrogen sulfide-releasing cyclooxygenase inhibitor and a derivative of Naproxen (significantly reduced exudate leukocyte and PGE2 levels at 30 µmol/kg oral administration). ATB-346 exhibits anti-inflammatory properties similar to naproxen.In a mouse airpouch model, ATB-346 suppressed cyclooxygenase-2 activity and inhibited leukocyte infiltration more effectively than naproxen but with substantially reduced gastrointestinal toxicity (100-fold safer than naproxen).
KEYWORDS: ATB 346 | supplier | COX inhibitor; H2S-releasing compound | ATB346 | CAS [1226895-20-0] | Fatty acid (Arachidonic acid) | COX | Inhibitor | cyclooxygenase | Naproxen | anti-inflammatory | leukocyte infiltration | | axonmedchem |
| ML 355 | Axon 2873
CAS [1532593-30-8]
MF C21H19N3O4S2MW 441.52
Purity:
98%
Soluble in DMSO
Description
Potent inhibitor of 12-lipoxygenase (12-LOX) (IC50 value of 0.34 µM) which shows excellent selectivity against related enzymes (15-LOX-1, 5-LOX, 15-LOX-2, COX-1/-2). Besides, ML 355 exhibits a favourable in vitro ADME and in vivo PK profile with activity in disease relevant cell-based systems, such thrombosis (platelet aggregation and calcium mobilization), and diabetes (12-HETE reducing in β -cells).
KEYWORDS: ML 355 | supplier | Lipoxygenase inhibitor | ML355 | ML-355 | CAS [1532593-30-8] | Fatty acid (Arachidonic acid) | LOX | Inhibitor | Enzymes | Thrombosis | Diabetes | | axonmedchem |
| ThioLox - Thiophene A9 | Axon 2844
CAS [1202193-89-2]
MF C15H18N2OSMW 274.38
Purity:
99%
Soluble in DMSO
Description
Inhibitor of 15-lipoxygenase-1 (15-LOX-1) with both anti-inflammatory and neuroprotective properties (IC50 value of 12 µM). Ex vivo biological evaluation in precision-cut lung slices (PCLS) showed inhibition of pro-inflammatory gene expression and in vitro studies on neuronal HT-22 cells showed a strong protection against glutamate toxicity for this 15-LOX-1 inhibitor.
KEYWORDS: Thiolox | supplier | Lipoxygenase inhibitor | CAS [1202193-89-2] | Fatty acid (Arachidonic acid) | LOX | Inhibitor | Enzymes | | axonmedchem |
| Valdecoxib - SC 65872 | Bextra | Axon 2106
CAS [181695-72-7]
MF C16H14N2O3SMW 314.36
Purity:
99%
Soluble in DMSO
Description
NSAID. Highly selective and potent inhibitor of COX-2 in human whole blood and against the recombinant human enzyme, showing exceptional potency after oral administration. Valdecoxib showed weak inhibitory activity against COX-1 (IC50 = 140 µM), and potent activity against COX-2 (IC50 = 0.005 µM)
References
Certificates
Categories
Extra info
JJ Talley et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J. Med. Chem. 2000, 43(5), 775-777.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
EC 1.14.99.1
COX
Pfizer Licensed Products
Selecive COX-2 inhibitor
Chemical name
4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[181695-72-7]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| GW 406381 - GW 406381X | Axon 1974
CAS [221148-46-5]
MF C21H19N3O3SMW 393.46
Purity:
99%
Soluble in DMSO
Description
Highly selective cyclooxygenase-2 (COX-2) inhibitor that is effective in animal models of central sensitization and of inflammatory pain
References
Certificates
Categories
Extra info
S Bingham et al. The Cyclooxygenase-2 Inhibitor GW406381X [2-(4-Ethoxyphenyl)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[1,5-b]pyridazine] Is Effective in Animal Models of Neuropathic Pain (...). J. Pharmacol. Exp. Ther. 2005, 312(3), 1161-1169.
DJ Boswell et al. Evaluation of GW406381 for Treatment of Osteoarthritis of the Knee: Two Randomized, Controlled Studies. Medscape J. Med. 2008, 10(11), 259.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
EC 1.14.99.1
COX
COX-2 inhibitor
Chemical name
2-(4-ethoxyphenyl)-3-(4-(methylsulfonyl)phenyl)pyrazolo[1,5-b]pyridazine
Parent CAS No.
[221148-46-5]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Pravadoline - WIN 48098 | Axon 1523
CAS [92623-83-1]
MF C23H26N2O3MW 378.46
Purity:
99%
Soluble in DMSO
Description
COX inhibitor and cannabinoid CB agonist, an antiinflammatory and analgesic agent
References
Certificates
Categories
Extra info
DR Haubrich et al. Pharmacology of pravadoline: a new analgesic agent. J. Pharmacol. Exp. Ther. 1990, 255(2), 511–522.
TE D'Ambra et al. Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. J. Med. Chem. 1992, 35(1), 124–135.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
EC 1.14.99.1
COX
COX inhibitor; CB agonist
Chemical name
(4-Methoxy-phenyl)-[2-methyl-1-(2-morpholin-4-yl-ethyl)-1H-indol-3-yl]-methanone
Parent CAS No.
[92623-83-1]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SC 26196 - PF 06341724 | Axon 2112
CAS [218136-59-5]
MF C27H29N5MW 423.55
Purity:
99%
Soluble in DMSO
Description
Selective Δ6-desaturase inhibitor (IC50 = 0.2 µM in vitro; >100 fold selective over Δ5- and Δ9-desaturases), an enzyme essential for the synthesis of arachidonic acid. It showed anti-inflammatory effects to the same extent as indomethacin or essential fatty acid deficiency in established mouse models
References
Certificates
Categories
Extra info
MG Obukowicz et al. Novel, selective delta6 or delta5 fatty acid desaturase inhibitors as antiinflammatory agents in mice. J. Pharmacol. Exp. Ther. 1998, 287(1), 157-166.
MB Hansen-Petrik et al. Selective inhibition of Delta-6 desaturase impedes intestinal tumorigenesis. Cancer Lett. 2002, 175(2), 157-163.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Pain & Inflammation
FADS2
EC 1.14.19.1
Pfizer Licensed Products
Selective Δ6-desaturase inhibitor
Chemical name
2,2-diphenyl-5-(4-(pyridin-3-ylmethyleneamino)piperazin-1-yl)pentanenitrile
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[218136-59-5]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| LX2343 | Axon 2869
CAS [333745-53-2]
MF C22H19ClN2O6SMW 474.91
Purity:
99%
Soluble in DMSO
Description
Inhibitor of human β-secretase (BACE-1) and PI3K (non-ATP competitive) with IC50 values of 11 µM and 16 µM, respectively. Moreover, LX2343 ameliorates cognitive dysfunction in APP/PS1 transgenic mice via both Aβ production inhibition and clearance promotion. Potentially effective in the treatment of Alzheimer's disease.
KEYWORDS: LX2343 | supplier | BACE inhibitor | LX 2343 | LX-2343 | CAS [333745-53-2] | Amyloids | BACE-1 | Amyloid-β | PI3K | Inhibitor | Enzymes | Alzheimer's disease | Cognitive Dysfunction | | axonmedchem |
| Acalisib - GS 9820 | CAL 120 | Axon 2857
CAS [870281-34-8]
MF C21H16FN7OMW 401.40
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Acalisib is a potent and selective PI3K δ-isoform inhibitor (p110δ: IC50 value of 12.7 nM).
KEYWORDS: Acalisib | supplier | PI3K p110δ inhibitor | GS 9820 | CAL 120 | GS9820 | GS-9820 | CAL120 | CAL-120 | CAS [870281-34-8] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Osteoclast | | axonmedchem |
| PF 3845 | Axon 1711
CAS [1196109-52-0]
MF C24H23F3N4O2MW 456.46
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Highly selective and irreversible fatty acid amide hydrolase (FAAH) inhibitor
References
Certificates
Categories
Extra info
K Ahn et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem. Biol. 2009, 16, 411-420.
L Booker et al. The FAAH Inhibitor PF-3845 Acts in the Nervous System to Reverse Lipopolysaccharide-induced Tactile Allodynia in Mice. Br. J. Pharmacol. 2012, 165(8), 2485-2496.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Pain & Inflammation
FAAH
EC 3.5.1.99
Selective fatty acid amide hydrolase (FAAH) inhibitor
Chemical name
N-(pyridin-3-yl)-4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)piperidine-1-carboxamide
Parent CAS No.
[1196109-52-0]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| BACE-1 Inhibitor | Axon 1125
CAS [797035-11-1]
MF C31H38N4O5SMW 578.72
Purity:
97%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective cell-permeable inhibitor of human β-secretase (BACE-1).
References
Certificates
Categories
Extra info
H Potter and D Dressler. The potential of BACE inhibitors for Alzheimer's therapy. Nature Biotech. 2000, 18, 125 - 126.
SJ Stachel et al. Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1). J. Med. Chem. 2004, 47, 6447-6450.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
BACE-1
EC 3.4.23.46
BACE 1 inhibitor
Chemical name
N-((1S,2R)-1-Benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
Parent CAS No.
[797035-11-1]
Order
Size
Unit Price
Stock
2 mg
€110.00
In Stock | | axonmedchem |
| Autophinib | Axon 2748
CAS [1644443-47-9]
MF C14H11ClN6O3MW 346.73
Purity:
99%
Soluble in DMSO
Description
Autophinib targets the lipid kinase vacuolar protein sorting 34 (VPS34), which is a promising target for selective autophagy modulation (IC50 value of 0.019 µM). Autophinib inhibits autophagy induced by starvation or rapamycin with IC50 values of 0.04 µM and 0.09 µM, respectively.
KEYWORDS: Autophinib | supplier | VPS34 inhibitor | CAS [1644443-47-9] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Autophagy | | axonmedchem |
| SAR405 | Axon 2716
CAS [1523406-39-4]
MF C19H21ClF3N5O2MW 443.85
Purity:
98%
Optical purity:
>99% ee
Soluble in DMSO
Description
SAR405 is a potent kinase inhibitor of PI3K class III (PIK3C3), highly specific on VPS34 (with IC50 value of 1 nM and Kd value of 1.5 nM for PIK3C3/VPS34). This compound has an exquisite protein and lipid kinase selectivity profile that is explained by its unique binding mode and molecular interactions within the ATP binding cleft of human Vps34. Inhibition of Vps34 kinase activity by SAR405 affects both late endosome-lysosome compartments and prevents autophagy. Concomitant inhibition of Vps34 and mTOR, with SAR405 and mTOR inhibitor everolimus, results in synergistic antiproliferative activity in renal tumor cell lines.
KEYWORDS: SAR405 | VPS34 inhibitor | PI3K inhibitor | SAR 405 | SAR-405 | CAS [1523406-39-4] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Vsp34 | PI3K(class III) | Autophagy | PIK3C3 | Kinase | | axonmedchem |
| RO 4929097 | Axon 2521
CAS [847925-91-1]
MF C22H20F5N3O3MW 469.40
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent γ-secretase inhibitor (GSI; IC50 value 4 nM) targeting Notch signaling with in vivo efficacy in various tumor cells, showing >100-fold selectivity with respect to 75 other proteins of various types (receptors, ion channels, and enzymes). Treatment of HEK293 cells with RO4929097 caused a dose-dependent decrease in the amount of Aβ peptides secreted into the culture medium (EC50 value 14 nM), and a strong dose-dependent inhibition of Notch processing in a Notch cell-based reporter assay (EC50 value 5 nM).
KEYWORDS: RO 4929097 | Supplier | γ-Secretase inhibitor | RO4929097 | CAS [847925-91-1] | Amyloids | γ Secretase | Inhibitor | GSI | Notch | signaling | Aβ peptides | tumor | melanoma | gamma Secretase | | axonmedchem |
| Z-VAD-FMK - Z-VAD(OMe)-FMK | Axon 2159
CAS [187389-52-2]
MF C22H30FN3O7MW 467.49
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Pan-caspase inhibitor with in vivo activity (Ki values 18.4 μM, 0.45 μM, and 17.1 μM for Caspase-3, -8, and -9 resp). Z-VAD-FMK inhibits apoptosis by blocking the processing of CPP32, and in pyrogallol-treated lung cancer Calu-6 cells via the prevention of GSH depletion. Z-VAD-FMK is a key compound for studies on apoptosis.
Product is currently not in stock
References
Certificates
Categories
Extra info
R. Sadhukhan et al. An efficient method to express and refold a truncated human procaspase-9: a caspase with activity toward Glu-X bonds. Protein Expr. Purif. 2006, 46, 299-308.
Y.H. Han et al. Caspase inhibitor decreases apoptosis in pyrogallol-treated lung cancer Calu-6 cells via the prevention of GSH depletion. Int. J. Oncol. 2008, 33, 1099-1105.
G.P. McStay et al. Overlapping cleavage motif selectivity of caspases: implications for analysis of apoptotic pathways. Cell Death Differ. 2008, 15, 322-331.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
EC 3.4.22.56
Caspase
Pan-caspase inhibitor with in vivo activity
Chemical name
(5S,8S,11S)-methyl 11-(2-fluoroacetyl)-5-isopropyl-8-methyl-3,6,9-trioxo-1-phenyl-2-oxa-4,7,10-triazatridecan-13-oate
Parent CAS No.
[187389-52-2]
Inquire | | axonmedchem |
| Boc-D-FMK - Boc-Asp(OMe)-fluoromethyl ketone | BAF | Axon 2158
CAS [187389-53-3]
MF C11H18FNO5MW 263.26
Purity:
98%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Broad spectrum caspase inhibitor. Causes concentration-dependent inhibition of only TNFα-stimulated apoptosis (IC50 value 39 μM). Boc-D-FMK could significantly promote the survival of spinal motoneurons after root avulsion in neonates, but not in adult rats. Boc-D-FMK treatment reduces acute cell death after traumatic brain injury (TBI) by inhibiting mitochondrial release of cytochrome c, possibly via a mechanism involving initiator caspases-2, and -3-like, but not -8).
KEYWORS: Boc-D-FMK | supplier | Caspase inhibitor | apoptosis | TNF | boc-Aspartyl(OMe)-fluoromethylketone | BAF | traumatic | Brain injury | TBI | survival | motoneurons | | axonmedchem |
| PS 1145 | Axon 1568
CAS [431898-65-6]
MF C17H11ClN4OMW 322.75
Purity:
99%
Soluble in DMSO
Description
A highly specific IKB kinase (IKK) inhibitor; efficiently inhibits both basal and induced NF-kB activity in PC cells
References
Certificates
Categories
Extra info
A Yemelyanov et al. Effects of IKK inhibitor PS1145 on NF-kB function, proliferation, apoptosis and invasion activity in prostate carcinoma cells. Oncogene 2006, 25, 387–398.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Transcription Factors
NF-κB
EC 2.7.11.10
IKK
IKK inhibitor
Chemical name
N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)nicotinamide
Parent CAS No.
[431898-65-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Begacestat - GSI 953 | Axon 2117
CAS [769169-27-9]
MF C9H8ClF6NO3S2MW 391.74
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective γ-secretase inhibitor (γ-secratase inhibitor, GSI); Capable of reducing both Aβ40 and Aβ42 production in a cell line stably expressing human recombinant APP (EC50 values of 14.8 and 12.4 nM for Aβ40 and Aβ40 respectively). Begacestat was found to have >16-fold selectivity in vitro for the inhibition of APP processing over Notch
References
Certificates
Categories
Extra info
RL Martone et al. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. J. Pharmacol. Exp. Ther. 2009, 331(2), 598-608.
SC Mayer et al. Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease. J. Med. Chem. 2008, 51(23), 7348-7351.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
γ Secretase
EC 3.4.23.46
Pfizer Licensed Products
Selective γ-secretase inhibitor (GSI)
Chemical name
(S)-5-chloro-N-(4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butan-2-yl)thiophene-2-sulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[769169-27-9]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Apoptosis Activator 2 | Axon 2006
CAS [79183-19-0]
MF C15H9Cl2NO2MW 306.14
Purity:
99%
Soluble in DMSO
Description
A cell-permeable apoptosis activator; activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells by promoting the oligomerization of Apaf-1 into the mature apoptosome
References
Certificates
Categories
Extra info
JT Nguyen and JA Wells. Direct activation of the apoptosis machinery as a mechanism to target cancer cells. Proc. Natl. Acad. Sci. USA. 2003, 100(13), 7533–7538.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
EC 3.4.22.62
Procaspase
A cell-permeable apoptosis activator
Chemical name
1-(3,4-dichlorobenzyl)indoline-2,3-dione
Parent CAS No.
[79183-19-0]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| NS 3694 | Axon 1883
CAS [426834-38-0]
MF C15H10ClF3N2O3MW 358.70
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Apoptosis inhibitor; NS3694 inhibits the formation of the apoptosome Apaf-1 by blocking the activation of the initiator caspase 9; NS2694 exhibits no effect on apoptosome-independent caspase activation and enzymatic activity of caspases
References
Certificates
Categories
Extra info
U Lademann et al. Diarylurea compounds inhibit caspase activation by preventing the formation of the active 700-kilodalton apoptosome complex. Mol. Cell Biol. 2003, 23(21), 7829-7837.
A. Degterev et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nature Chem. Biol. 2005, 1, 112.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
EC 3.4.22.62
Procaspase
Inhibitor of apoptosis; Inhibits formation of apoptosome complex
Chemical name
4-chloro-2-(3-(3-(trifluoromethyl)phenyl)ureido)benzoic acid
Parent CAS No.
[426834-38-0]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| PAC 1 - Procaspase activating compound 1 | Axon 1743
CAS [315183-21-2]
MF C23H28N4O2MW 392.49
Purity:
100%
Soluble in DMSO
Description
A procaspase activating compound activates procaspase-3 to produce caspase-3; induces apoptosis in cancerous cells
References
Certificates
Categories
Extra info
C Wiśniewski and H Car. (S)-3,5-DHPG: a review. CNS Drug Rev. 2002, 8(1), 101–116.
WM Zho et al. The group I metabotropic glutamate receptor agonist (S)-3,5-dihydroxyphenylglycine induces a novel form of depotentiation in the CA1 region of the hippocampus. J. Neurosci. 2002, 22(20), 8838-8849.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
EC 3.4.22.56
Procaspase
Procaspase activating compound 1
Chemical name
N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acEthanolydrazide
Parent CAS No.
[315183-21-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| DBZ, γ-Secretase Inhibitor | Axon 1488
CAS [209984-56-5]
MF C26H23F2N3O3MW 463.48
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Very potent and cell-permeable inhibitor of γ-secretase (GSI); potently inhibits Notch processing (IC50 values to be 1.7 nM in SupT1 cells)
KEYWORDS: γ-Secretase Inhibitor DBZ | supplier | gamma-secretase inhibitor | DBZ | CAS [209984-56-5] | Amyloids | GSI | Notch signaling | lineage | differentiation | ERK-1 | MAPK | | axonmedchem |
| BZ, γ-Secretase Inhibitor - Compound E | Axon 1487
CAS [209986-17-4]
MF C27H24F2N4O3MW 490.50
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Very potent and cell-permeable inhibitor of γ-secretase (GSI); potently inhibits Notch processing (IC50 values to be 2.2 nM in SupT1 cells); inhibits β-ammyloid production in cell culture with an IC50 of 0.3 nM.
KEYWORDS: γ-Secretase Inhibitor BZ | supplier | γ-Secretase inhibitor | Compound E | CAS [209986-17-4] | Amyloids | γ Secretase | γ-Secretase inhibitor (GSI) | Inhibitor | Enzymes | | axonmedchem |
| Ivachtin | Axon 1375
CAS [745046-84-8]
MF C20H21N3O7SMW 447.46
Purity:
99%
Moderately soluble in DMSO
Description
A potent caspase-3 inhibitor
References
Certificates
Categories
Extra info
Kravchenko et al. Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. J. Med. Chem. 2005, 48, 3680.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
EC 3.4.22.56
Caspase
Caspase-3 inhibitor
Chemical name
Acetic acid 2-[4-methyl-8-(morpholine-4-sulfonyl)-1,3-dioxo-1,3-dihydro-pyrrolo[3,4-c]quinolin-2-yl]-ethyl ester
Parent CAS No.
[745046-84-8]
Order
Size
Unit Price
Stock
1 mg
€55.00
In Stock | | axonmedchem |
| Isoquinolinediol, 1,5- - NSC 65585 | Axon 2537
CAS [5154-02-9]
MF C9H7NO2MW 161.16
Purity:
100%
Soluble in 0.1N NaOH(aq) and DMSO
Description
PARP1-specific inhibitor (IC50 value 0.39 - 1.00 μM) and neuroprotective agent, that leads to an increase up to 8-fold in the absolute frequency of gene targeting in the correction of the mutation at the stable integrated HSV tk gene in mouse Ltk cells. Treatment of 1,5-Isoquinolinediol significantly blocked mitochondrial membrane potential loss and AIF (apoptosis inducing factor) and cytochrome c release from the mitochondria. 1,5-Isoquinolinediol did not suppress pristimerin-induced JNK activation.
KEYWORDS: 1,5-Isoquinolinediol | supplier | PARP inhibitor |NSC65585 |NSC65585 | CAS [5154-02-9] |DNA-RNA | PARP1 | Inhibitor | DHIQ | DIQ | poly |ADP-ribose | SSB | single strand breaks | Ltk cells | mitochondrial membrane potential |AIF| apoptosis inducing factor | neuroprotetcive | JNK | | axonmedchem |
| ABT 888 - Veliparib | A 861695 | Axon 1593
CAS [912444-00-9]
MF C13H16N4OMW 244.29
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Potent and orally bioavailable PARP inhibitor, with Ki values to be 5.2 nM for PARP1 and 2.9 nM for PARP2 respectively; inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.
The hydrochloride salt of ABT 888 is also available as Axon 2888.
KEYWORDS: ABT 888 | supplier | PARP inhibitor | Veliparib | A 861695 | ABT888 | ABT-888 | A-861695 | A861695 | CAS [912444-00-9] | DNA-RNA | PARP | PARP1 | PARP2 | Inhibitor | Enzymes | | axonmedchem |
| SMI 481 - 6748-481 | Axon 2387
CAS [432020-20-7]
MF C17H15ClFN3O3MW 363.77
Purity:
99%
Soluble in DMSO
Description
Small-molecule inhibitor (SMI) of the yeast PITP Sec14 (IC50 values of 211 nM and 2.87 μM for Sec14 mediated [3H]PtdIns transfer in vitro, and Sec14 dependent cell growth inhibition of WT (CTY182, gray) strains, respectively). SMI481 (aka 6748-481 ) is a water-soluble bioactive compound exhibiting exquisite pathway selectivity in inhibiting phosphoinositide signaling in cells with >200-fold selectivity over other yeast Sec14-like transfer activities. PITP-directed SMIs offer new and generally applicable avenues for intervening with phosphoinositide signaling pathways with selectivities superior to those afforded by contemporary lipid kinase-directed strategies.
References
Certificates
Categories
Extra info
A.H. Nile et al. PITPs as targets for selectively interfering with phosphoinositide signaling in cells. Nat Chem Biol. 2014 Jan;10(1):76-84.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Sec14
First small-molecule inhibitor (SMI) of the yeast PITP Sec14
Chemical name
(4-chloro-3-nitrophenyl)(4-(2-fluorophenyl)piperazin-1-yl)methanone
Parent CAS No.
[432020-20-7]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| GeA-69 | Axon 2885
CAS [2143475-98-1]
MF C20H16N2OMW 300.35
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| Talazoparib - BMN 673 | LT 00673 | Axon 2502
CAS [1207456-01-6]
MF C19H14F2N6OMW 380.35
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, selective, and orally available PARP1/2 inhibitor (IC50 value 0.57 nM for PARP1) that shows antitumor cytotoxicity with 20- to more than 200-fold greater potency than earlier-generation PARP1/2 inhibitors and with selectivity for tumor cells with BRCA1, BRCA2, or PTEN gene defects.
KEYWORDS: Talazoparib | PARP inhibitor | Axon 2502 | BMN 673 | LT 00673 | BMN673 | LT00673 | CAS [1207456-01-6] | DNA-RNA | PARP | Inhibitor | BRCA1 | BRCA2 | PTEN | gene defects | | axonmedchem |
| AG 014699 - PF 01367338 | Rucaparib | Axon 1529
CAS [459868-92-9]
MF C19H18FN3O.H3O4PMW 421.36
Purity:
98%
Soluble in water and DMSO
Description
A PARP 1 inhibitor with potential chemosensitizing, radiosensitizing and antineoplastic activities; selectively binds to PARP1 (Ki=1.4 nM) and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. AG-014699 is the phosphate salt of AG 014447 (CAS 283173-50-2) and has improved aqueous solubility
References
Certificates
Categories
Extra info
HD Thomas et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer Ther. 2007, 6(3), 945-56.
P Plummer et al. Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res. 2008, 14(23), 7917-23.
M Ali et al. Vasoactivity of AG014699, a Clinically Active Small Molecule Inhibitor of Poly(ADP-ribose) Polymerase: a Contributory Factor to Chemopotentiation In vivo? Clin. Cancer Res. 2009, 15(19), 6106-6112.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
PARP1 inhibitor
Chemical name
8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one phosphate
Parent CAS No.
[283173-50-2]
Order
Size
Unit Price
Stock
2 mg
€75.00
In Stock | | axonmedchem |
| SF 1670 | Axon 2186
CAS [345630-40-2]
MF C19H17NO3MW 307.34
Purity:
98%
Soluble in DMSO
Description
Inhibitor of phosphatase and tensin homologue deleted on chromosome 10 (PTEN, IC50 value 2 µM), an important regulator of insulin-dependent signaling, that augments the efficacy of granulocyte transfusion in a clinically relevant mouse model. SF 1670 enhances neutrophil functions and fMLP-induced PtdIns(3,4,5)P3 signaling in neutrophils. SF 1670 is also a potent inhibitor of protein tyrosine phosphatase (PTP) CD45 (aka PTPRC; IC50 values 0.2 µM and 0.1 µM for CD45 induced pNPP hydrolysis and T-cell proliferation, respectively) and of galactokinase (GALK, IC50 value 0.7 µM).
References
Certificates
Categories
Extra info
Y. Li et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model. Blood. 2011, 117, 6702-6713.
R.A. Urbanek et al. Potent reversible inhibitors of the protein tyrosine phosphatase CD45. J. Med. Chem. 2001, 44, 1777-1793.
E. Rosivatz et al. A small molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS Chem. Biol. 2006, 1, 780-790.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Diabetes & Metabolism
p53-Tumor Suppression
PI3K-Akt-mTOR
PTEN
PTPRC
GALK
EC 3.1.3.67
Inhibitor of PTEN with significant inhibitory effect on PTPRC and GALK
Chemical name
N-(9,10-dioxo-9,10-dihydrophenanthren-2-yl)pivalamide
Parent CAS No.
[345630-40-2]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| UPF 1069 | Axon 2369
CAS [1048371-03-4]
MF C17H13NO3MW 279.29
Purity:
99%
Soluble in DMSO
Description
PARP-2 inhibitor with >26 fold selectivity over PARP1 (IC50 values 8.0 µM and 0.3 µM for PARP1 and PARP2, respectively) that exacerbates oxygen-glucose deprivation (OGD) injury in the hippocampus, but significantly attenuates OGD damage in mixed cortical cell cultures at concentrations high enough to inhibit both PARP1 and PARP2. UPF 1069 is a valuable tool to explore the function of PARP-2 in biological systems and to examine the different roles of PARP isoenzymes in the mechanisms of cell death and survival.
References
Certificates
Categories
Extra info
F. Moroni et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br. J. Pharmacol. 2009, 157, 854-862.
R. Pellicciari et al. On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. ChemMedChem. 2008, 3, 914-923.
T. Haikarainen et al. Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors. ACS Med. Chem. Lett. 2013, 5, 18-22.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
PARP-2 inhibitor with >26 fold selectivity over PARP1
Chemical name
5-(2-oxo-2-phenylethoxy)isoquinolin-1(2H)-one
Parent CAS No.
[1048371-03-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| KU 0058948 hydrochloride | Axon 2001
CAS [N.A.]
MF C21H21FN4O2.HClMW 416.88
Purity:
99%
Soluble in water and DMSO
Description
Potent and specific PARP inhibitor (IC50: 3.4 nM for PARP1); KU-0058948 activates transfected extracellular signal-regulated kinase 8 (ERK8) in cells and induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro.
KEYWORDS: KU 0058948 hydrochloride | supplier | PARP1 inhibitor | KU0058948 HCl | KU58948 | KU-0058948 | KU058948 | CAS [763111-49-5] | DNA-RNA | PARP | ERK8 | extracellular signal-regulated kinase 8 | cell cycle arrest | apoptosis | repair | Poly(ADP-Ribose) Polymerase | | axonmedchem |
| NQ301 - Compound 211 | Axon 2702
CAS [130089-98-4]
MF C18H12ClNO3MW 325.75
Purity:
99%
Soluble in DMSO
Description
NQ301 is an allosteric noncompetitive selective CD45 inhibitor (IC50 value 200 nM). Antithrombotic agent.
KEYWORDS: NQ301 | supplier | CD45 inhibitor | Compound 211 | NQ-301 | NQ 301 | Compound211 | Compound-211 | CAS [130089-98-4] | Non Selective (Tyrosine Specific Phosphomonoesters) | PTPRC | Inhibitor | Enzymes | Antithrombotic | CD45 | | axonmedchem |
| AZD 2461 | Axon 2241
CAS [1174043-16-3]
MF C22H22FN3O3MW 395.43
Purity:
99%
Soluble in DMSO
Description
PARP inhibitor (IC50 value 5 nM) with poor P-glycoprotein substrate qualities. Unlike treatment with AZD 2281 (Olaparib, Axon 1464), AZD 2461 succesfully circumvents drug resistance of Pgp-proficient tumors, and inactivation of p53-binding protein 1 (53BP1) as a causal factor in PARPi resistance.
KEYWORDS: AZD 2461 | supplier | PARP inhibitor | AZD2461 | AZD-2461 | CAS [1174043-16-3] | DNA-RNA | PARP1 | P-gp | AZD 2281 | Olaparib | drug resistance | tumors | p53 | binding protein 1 | 53BP1 | PARPi | resistance | | axonmedchem |
| SHP099 | Axon 2633
CAS [1801747-42-1]
MF C16H19Cl2N5MW 352.26
Purity:
99%
Soluble in DMSO
Description
Highly potent, selective and orally bioavailable SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 potently inhibits ERK phosphorylation and the growth of cancer cell lines that have alterations in RTKs or other tyrosine kinases such as the Janus kinases JAK1 and JAK2. SHP099 showed no detectable activity against a panel of 21 phosphatases and 66 kinases (including the closest homologue SHP1), and only had modest activity against 5HT3 when profiled against a preclinical safety pharmacology panel representing 49 common adverse drug reaction targets.
KEYWORDS: SHP099 | supplier | SHP2 inhibitor | SHP-099 | SHP 099 | CAS [1801747-42-1] | [1801747-11-4] | Tyrosine Phosphatase | PTP | PTPN11 | PTP-2C | programmed cell death pathway | PD-1/PD-L1 | Noonan | Leopard | RAS-ERK signaling | | axonmedchem |
| Sephin 1 - NSC 65390 | Axon 2524
CAS [951441-04-6]
MF C8H9ClN4MW 196.64
Purity:
99%
Soluble in DMSO
Description
Selective PPP1R15A inhibitor devoid of PPP1R15B and α2-adrenergic activity. In cells, Sephin1 selectively disrupted the PPP1R15A-PP1c complex, therebye prolonging eIF2α phosphorylation after stress, delaying translation recovery, and consequently, attenuated expression of stress genes such as the pro-apoptotic protein CHOP. The cytoprotectant prevents protein misfolding, motor deficits, motor neuron loss, and the molecular defects in SOD1 mutant mice.
KEYWORDS: Sephin 1 | supplier| | | | axonmedchem |
| TEPP 46 - ML 265 | Axon 2240
CAS [1221186-53-3]
MF C17H16N4O2S2MW 372.46
Purity:
99%
Soluble in DMSO
Description
Potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR. Continuous dosing of mice with TEPP 46 decreased the development of human cancer cell xenografts, suggesting that increased pyruvate kinase activity can impair tumorigenesis.TEPP 46 can mimic the enzymatic properties of PKM1 in PKM2-expressing cells, alter cell metabolism, and induces changes in the kinetic properties of PKM2 that are identical to those induced by the endogenous PKM2 activator FBP.
KEYWORDS: TEPP 46 | supplier | PKM2 activator | ML 265 | TEPP46 | ML265 | TEPP-46 | ML-265 | CAS [1221186-53-3] | Pyyruvate | PKM2 | Activator | Enzymes | Glycolysis | Warburg | tumorigenesis | cancer | glucose metabolism | | axonmedchem |
| BCI - NSC 150117 | Axon 2178
CAS [1245792-51-1]
MF C22H23NOMW 317.42
Purity:
99%
Soluble in DMSO
Description
Allosteric inhibitor of dual-specificity phosphatases (DUSP). BCI treatment of DUSP6-Myc–transfected cells blocks DUSP6 or DUSP1 activity, but not DUSP5 (IC50 values 12.3 μM and 11.5 μM for DUSP6 and DUSP1 inhibition, resp.). BCI mediated DUSP6 inhibition can induce expansion of myocardial progenitors that ultimately increases heart size in zebrafish embryos.BCI also inhibits lung cancer and uveal melanoma cells viability (IC50 values ranging from 0.1 to 90 μM).The dual-specificity phosphatase 6 (DUSP6) functions a feedback regulator of fibroblast growth factor (FGF) signaling to limit the activity of extracellular signal–regulated kinases (ERKs) 1 and 2.
The more hydrophilic BCI hydrochloride (Axon 2852) is also available.
KEYWORDS: BCI | supplier | DUSP inhibitor | NSC 150117 | NSC150117 | NSC-150117 | CAS [1245792-51-1] | Non Selective (Serine-Threonine and Tyrosine Specific Phosphodiesters) | DUSP | Inhibitor | Enzymes | | axonmedchem |
| TPI-1 | Axon 2723
CAS [79756-69-7]
MF C12H6Cl2O2MW 253.08
Purity:
99%
Soluble in DMSO
Description
SHP1 inhibitor TPI-1 (IC50 value 40 nM) selectively increased SHP1 phospho-substrates (pLck-pY394, pZap70 and pSlp76) in Jurkat T cells but had little effects on pERK1/2 or pLck-pY505 regulated by phosphatases SHP2 or CD45, respectively. TPI-1 was shown to be more effective than sodium stibogluconate in SHP1 inhibition, immune cell activation and anti-tumor action.
KEYWORDS: TPI-1 | supplier | SHP1 inhibitor | TPI1 | TPI 1 | CAS [ 79756-69-7 ] | Non Selective (Tyrosine Specific Phosphomonoesters) | SHP | Inhibitor | Enzymes | SHP-1 | tyrosine phosphatase inhibitor-1 | cancer | anti-tumor | | axonmedchem |
| Mitapivat | Axon 2149
CAS [1260075-17-9]
MF C24H26N4O3SMW 450.55
Purity:
99%
Soluble in DMSO
Description
Activator of pyruvate kinase isoenzyme M2 (PKM2), an enzyme involved in glycolysis. Since all tumor cells exclusively express the embryonic M2 isoform of PK, it is hypothesized that PKM2 is a potential target for cancer therapy. Modulation of PKM2 might also be effective in the treatment of obesity, diabetes, autoimmune conditions, and antiproliferation-dependent diseases.
KEYWORDS: Mitapivat | supplier | PKM2 activator | CAS [1260075-17-9] | Pyruvate | PKM2 | Isoenzyme M2 | Iso-enzyme | Activator | Enzymes | | axonmedchem |
| NHI 2 | Axon 2450
CAS [1269802-97-2]
MF C17H12F3NO3MW 335.28
Purity:
99%
Soluble in DMSO
Description
Selective cell membrane permeable inhibitor of human lactate dehydrogenase isoform A (LDH-A; IC50 values 14.7 µM and 55.8 µM in a NADH competition assay for LDH-A and LDH-B, respectively). NHI-2 caused 87% LDH-A inhibition at 125 μM (with minimal activity (11%) on LDH-B at the same concentration), exhibiting anti-proliferative activity in cancer cells. NHI 2 synergistically enhanced the activity of Gemcitabine in multiple cancer cell lines.
KEYWORDS: NHI2 | supplier | LDH-A inhibitor | CAS [1269802-97-2] | Lactate | LDH | Inhibitor | pyruvate | glycolysis | dehydrogenase | anti-proliferative | cancer | cytotoxic | hypoxia | cell-cycle | apoptosis | NADH | | axonmedchem |
| PFK 158 | Axon 2542
CAS [1462249-75-7]
MF C18H11F3N2OMW 328.29
Purity:
99%
Soluble in DMSO
Description
Nanomolar small molecule inhibitor of PFKFB3 (IC50 value 137 nM) that is selectively cytotoxic to cancer cells and displays broad anti-tumor activity causing significant growth inhibition in preclinical models of breast, lung, glioblastoma, ovarian, pancreatic, melanoma and colon cancer. PFK158 is well tolerated in rats and dogs resulting in an acceptable pre-clinical therapeutic index.
KEYWORDS: PFK 158 | supplier | PFKFB3 inhibitor | PFK158 | CAS [1462249-75-7] | Fructose 6-phosphate | PFKFB3 | Inhibitor | glycolysis | solid malignancy | Ras | AKT | PI3K | p53 | PTEN | cytotoxic | cancer cells | anti-tumor activity | breast cancer | lung cancer | glioblastoma | ovarian cancer | pancreatic cancer | melanoma | colon cancer | | axonmedchem |
| 3PO | Axon 2175
CAS [18550-98-6]
MF C13H10N2OMW 210.23
Purity:
99%
Soluble in DMSO
Description
Inhibitor of HIF-1-induced PFKFB3, an enzyme with a key role in glycolysis. Potential application as suppressor of tumor glucose metabolism and growth of non-small cell lung cancer cells. The PFKFB3 family member has the highest kinase:bisphosphatase ratio (740:1) of the four known PFKFB family members. 3PO markedly attenuated the stimulation of F2,6BP synthesis, 2-[1-14C]-deoxy-D-glucose uptake, lactate secretion, TNF-α secretion and T cell aggregation and proliferation.
KEYWORDS: 3PO | supplier | PFKFB3 inhibitor | 3PO | 3PO | CAS [18550-98-6] | Fructose 6-phosphate | PFKFB3 | F6P | F2 | 6BP | Inhibitor | Enzymes | | axonmedchem |
| BCI hydrochloride - NSC 150117 hydrochloride | Axon 2852
CAS [95130-23-7]
MF C22H23NO.HClMW 353.89
Purity:
100%
Soluble in DMSO
Description
Allosteric inhibitor of dual-specificity phosphatases (DUSP). BCI treatment of DUSP6-Myc–transfected cells blocks DUSP6 or DUSP1 activity, but not DUSP5 (IC50 values 12.3 μM and 11.5 μM for DUSP6 and DUSP1 inhibition, resp.). BCI mediated DUSP6 inhibition can induce expansion of myocardial progenitors that ultimately increases heart size in zebrafish embryos. BCI also inhibits lung cancer and uveal melanoma cells viability (IC50 values ranging from 0.1 to 90 μM). The dual-specificity phosphatase 6 (DUSP6) functions a feedback regulator of fibroblast growth factor (FGF) signaling to limit the activity of extracellular signal–regulated kinases (ERKs) 1 and 2.
The free base BCI is also available as Axon 2178.
KEYWORDS: BCI hydrochloride | supplier | DUSP inhibitor | NSC 150117 hydrochloride | NSC150117 hydrochloride | NSC-150117 hydrochloride | CAS [95130-23-7] | [1245792-51-1] | Non Selective (Serine-Threonine and Tyrosine Specific Phosphodiesters) | DUSP | Inhibitor | Enzymes | | axonmedchem |