| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| PK 11195 | Axon 1208
CAS [85532-75-8]
MF C21H21ClN2OMW 352.86
Purity:
99%
No solubility data
Description
Peripheral benzodiazepine antagonist.
KEYWORDS: PK 11195 | BZD antagonist | PK11195 | CAS [85532-75-8] | GABA | GABA-A | Antagonist | Ion Channels | | axonmedchem |
| Gabapentin - GOE 3450 | CI 945 | GO 3450 | Axon 1301
CAS [60142-96-3]
MF C9H17NO2MW 171.24
Purity:
99%
Soluble in water
Description
Anticonvulsant; mechanism of action still under study; neuroprotective; GABA modulator
References
Certificates
Categories
Extra info
G de Sarro et al. Gabapentin potentiates the antiseizure activity of certain anticonvulsants in DBA/2 mice. Eur. J. Pharmacol. 1998, 349, 179-185.
MJ Field et al. Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents. Br. J. Pharmacol. 1997, 121, 1513-1522.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABA modulator; Anti-convulsant
Chemical name
(1-Aminomethyl-cyclohexyl)-acetic acid
Parent CAS No.
[60142-96-3]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Zopiclone | Axon 1197
CAS [43200-80-2]
MF C17H17ClN6O3MW 388.81
Purity:
99%
No solubility data
Description
Benzodiazepine receptor BZR agonist; hypnotic agent used in the treatment of insomnia
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
Benzodiazepine agonist
Chemical name
4-Methyl-piperazine-1-carboxylic acid 6-(5-chloro-pyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-yl ester
Parent CAS No.
[43200-80-2]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SL 651498 | Axon 1195
CAS [205881-86-3]
MF C23H20FN3O2MW 389.42
Purity:
99%
Soluble in DMSO
Description
GABAA agonist subtype α2 selective
References
Certificates
Categories
Extra info
G Griebel et al. SL651498: An Anxioselective Compound with Functional Selectivity for 2- and 3-Containing -Aminobutyric AcidA (GABAA) Receptors. J. Pharmaco. Eexp. Ther. 2001, 298(2), 753-768.
NR Mirza et al. Comparative cue generalisation profiles of L-838417, SL651498, zolpidem, CL218872, ocinaplon, bretazenil, zopiclone and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination. J. Ph. Exp. Ther. 2006, 316(3), 1291.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABAA-α2 agonist
Chemical name
6-Fluoro-9-methyl-2-phenyl-4-(pyrrolidine-1-carbonyl)-2,9-dihydro-beta-carbolin-1-one
Parent CAS No.
[205881-86-3]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| L 838417 | Axon 1196
CAS [286456-42-6]
MF C19H19F2N7OMW 399.40
Purity:
99%
Soluble in DMSO
Description
Partial agonist at non-a1 GABAA and antagonist at GABAA-a1 receptor
References
Certificates
Categories
Extra info
J. Knabl et al. Reversal of pathological pain through specific spinal GABAAreceptor subtypes. Nature 2008, 451, 330-334.
NR Mirza et al. Comparative cue generalisation profiles of L-838417, SL651498, zolpidem, CL218872, ocinaplon, bretazenil, zopiclone and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination. J. Ph. Exp. Ther. 2006, 316(3), 1291.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABAA-α1 antagonist
Chemical name
7-tert-Butyl-3-(2,5-difluoro-phenyl)-6-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-[1,2,4]triazolo[4,3-b]pyridazine
Parent CAS No.
[286456-42-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| NBI 34060 - Indiplon | Axon 1121
CAS [325715-02-4]
MF C20H17N4O2SMW 376.43
Purity:
99%
Soluble in DMSO
Description
A high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors; NBI 34060 modulates specific GABAA receptor subtypes at the benzodiazepine site; nonbenzodiazepine hypnotic
References
Certificates
Categories
Extra info
RE Petroski et al. Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors. J. Pharmacol. Exp. Ther. 2006, 317(1), 369-77.
SK Sullivan et al. Characterization of the Interaction of Indiplon, a Novel Pyrazolopyrimidine Sedative/Hypnotic, with the GABAA Receptor. J. Pharmacol. Exp. Ther. 2004, 311(2), 537-546.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
PAM of GABAA-α1
Chemical name
N-Methyl-N-{3-[3-(thiophene-2-carbonyl)-3H-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-acetamide
Parent CAS No.
[325715-02-4]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Vildagliptin - NVP-LAF 237 | Axon 1631
CAS [274901-16-5]
MF C17H25N3O2MW 303.40
Purity:
99%
Optical purity:
Optically pure
Soluble in water
Description
Highly potent, selective and orally bioavailable inhibitor of dipeptidyl peptidase-4 (DPP4), with IC50 to be 2.3 and 2.7 nM for rat and human plasma DPP4
References
Certificates
Categories
Extra info
MA Sallas et al. Vildagliptin, a dipetidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with type 2 diabetes. J. Clin. Endocrinol. Metab. 2005, 90, 4888–4894.
UV Wesley et al. Dipeptidyl peptidase inhibits malignant phenotype of prostate cancer cells by blocking basic fibroblast growth factor signaling pathway. Cancer Res. 2005, 65(4), 1325–34.
EB Villhauer et al. 1-(3-hydroxy-1-adamantyl)aminoacetyl-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J. Med. Chem. 2003, 46, 2774-2789.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
DPP4
EC 3.4.14.5
DPP4 inhibitor
Chemical name
(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
Parent CAS No.
[274901-16-5]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Biphenyl-indanone A - BINA | LS 193571 | Axon 1644
CAS [866823-73-6]
MF C30H30O4MW 454.56
Purity:
99%
Soluble in DMSO
Description
Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 2 (mGluR2)
References
Certificates
Categories
Extra info
R Galici et al. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J Pharmacol. Exp. Ther. 2006, 318(1), 173–185.
MA Benneyworth et al. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Mol. Pharmacol. 2007, 72(2), 477–484.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR2
C3
Positive allosteric modulator (PAM) of mGluR2
Chemical name
3'-((2-cyclopentyl-6,7-dimethyl-1-oxo-2,3-dihydro-1H-inden-5-yloxy)methyl)biphenyl-4-carboxylic acid
Parent CAS No.
[866823-73-6]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| MDV 3100 - Enzalutamide | Axon 1613
CAS [915087-33-1]
MF C21H16F4N4O2SMW 464.44
Purity:
99%
Soluble in DMSO
Description
An orally active and very potent antagonist of androgen receptor (AR); Second-generation of antiandrogen for the treatment of advanced prostate cancer; highly recommended tool in AR research
KEYWORDS: MDV 3100 | Enzalutamide | 915087-33-1 | 915087-33-1 | AR antagonist | MDV3100 | Androgen | prostate cancer | | axonmedchem |
| XAV 939 - NVP-XAV 939 | Axon 1527
CAS [284028-89-3]
MF C14H11F3N2OSMW 312.31
Purity:
99%
Soluble in DMSO
Description
Tankyrase (TNKS) inhibitor, with IC50 values to be 11 and 4 nM for TNKS1 and TNKS2 respectively; inhibiting Wnt / β-catenin signaling
References
Certificates
Categories
Extra info
SM Huang et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling. Nature 2009, 461, 614-620.
R Nusse. Wnt signaling and stem cell control. Cell Res. 2008, 18, 523-527.
RT Peterson, Propping up a destructive regime. Nature 2009, 461, 599–600.
EM Adler. Inhibiting Wnt signaling. Sci. Signal. 2009, 2(91), ec326.
CE Meacham et al. In vivo RNAi screening identifies regulators of actin dynamics as key determinants of lymphoma progression. Nature Gen. 2009, 41(10), 1131-1137.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
DNA-damage Response
EC 2.4.2.30
TNKS
Tankyrase (TNKS) inhibitor
Chemical name
2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-1H-thiopyrano[4,3-d]pyrimidin-4(5H)-one
Parent CAS No.
[284028-89-3]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Rolofylline - KW 3902 | Axon 1603
CAS [136199-02-5]
MF C20H28N4O2MW 356.46
Purity:
99%
Soluble in DMSO
Description
Potent and selective adenosine A1 receptor antagonist, with Ki values to be 0.19 nM and 170 nM for A1 and A2 receptors respectively
References
Certificates
Categories
Extra info
H Nonaka et al. KW-3902, a selective high affinity antagonist for adenosine A1 receptors. Br J Pharmacol. 1996, 117(8), 1645–1652.
MM Givertz et al. The effects of KW-3902, an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and renal impairment or diuretic resistance. J. Am. Coll. Cardiol. 2007, 50(16), 1551–60.
BM Massie et al. Rolofylline, an Adenosine A1−Receptor Antagonist, in Acute Heart Failure. N. Engl. J. Med. 2010, 363(15), 1419-28.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A1
A18
Adenosine A1 antagonist
Chemical name
8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione
Parent CAS No.
[136199-02-5]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| AZD 6244 - ARRY 142886 | Selumetinib | Axon 1516
CAS [606143-52-6]
MF C17H15BrClFN4O3MW 457.68
Purity:
99%
Soluble in DMSO
Description
An orally active, highly potent and selective inhibitor of MEK 1/2 that has shown tumor-suppressive activity in a wide range of preclinical models. IC50 value to be 14 nM against purified MEK1
References
Certificates
Categories
Extra info
TC Yeh et al. Biological Characterization of ARRY-142886 (AZD6244), a Potent, Highly Selective Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor. Clin. Cancer Res. 2007, 13, 1576-1583.
BR Davies et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases. Mol. Cancer Ther. 2007, 6(8), 2209-2019.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
MAPK
EC 2.7.12.2
MEK
MEK1 and MEK2 inhibitor
Chemical name
5-(4-bromo-2-chlorophenylamino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
Parent CAS No.
[606143-52-6]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| KO 143 | Axon 1409
CAS [461054-93-3]
MF C26H35N3O5MW 469.57
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and selective inhibitor of breast cancer resistance protein (BCRP) multidrug transporter.
KEYWORDS: KO 143 | supplier | BCRP inhibitor | KO143 | CAS [461054-93-3] | BCRP | Inhibitor | ABC | multidrug transporter | ABCG2 | | axonmedchem |
| CP 101606 mesylate - Traxoprodil mesylate | Axon 1406
CAS [188591-67-5]
MF C20H25NO3.CH4O3SMW 423.52
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent and NR2B selective antagonist of NMDA glutamate receptors.
CP 101606 is also available as its parent compound (Axon 2254)
References
Certificates
Categories
Extra info
K Taniguchi et al. Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonist. Br. J. Pharmacol. 1997, 122, 809–812.
FS. Menniti et al. CP-101,606: An NR2B-Selective NMDA Receptor Antagonist. CNS Drug Rev. 1998, 4(4), 307-322.
L. Yurkewicz et al. The effect of the selective NMDA receptor antagonist traxoprodil in the treatment of traumatic brain injury. J. Neurotrauma. 2005, 22(12), 1428-43.
JG Nutt et al. Effects of a NR2B selective NMDA glutamate antagonist, CP-101,606, on dyskinesia and parkinsonist. Mov. Disord. 2008, 23(13), 1860-1866.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA NR2B antagonist
Chemical name
1-[(1S,2S)-2-Hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-4-phenylpiperidin-4-ol mesylate
Parent CAS No.
[134234-12-1]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| SB 203580 hydrochloride | Axon 1465
CAS [869185-85-3]
MF C21H16FN3OS.HClMW 413.90
Purity:
99%
Soluble in water
Description
Potent, cell-permeable and selective inhibitor of p38 MAP kinase (MAPK); water-soluble salt of SB 203580 (Axon 1363)
References
Certificates
Categories
Extra info
PC Singhal et al. Role of P38 Mitogen-Activated Protein Kinase Phosphorylation and Fas-Fas Ligand Interaction in Morphine-Induced Macrophage Apoptosis. J. Immunol. 2002, 168, 4025-4033.
PR Young et al. Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site. J. Biol. Chem. 1997, 272, 12116-12121.
H Kankaanranta et al. SB 203580, an Inhibitor of p38 Mitogen-Activated Protein Kinase, Enhances Constitutive Apoptosis of Cytokine-Deprived Human Eosinophils. J. Pharm. Exp. Ther. 1999, 290, 2, 621-628.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
Stem Cell
MAPK (p38)
MAPK
EC 2.7.11.24
MAPK inhibitor (p38 specific)
Chemical name
4-[5-(4-Fluoro-phenyl)-2-(4-methanesulfinyl-phenyl)-3H-imidazol-4-yl]-pyridine hydrochloride
Parent CAS No.
[152121-47-6]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| Tariquidar - XR 9576 | Axon 1960
CAS [206873-63-4]
MF C38H38N4O6MW 646.73
Purity:
98%
Soluble in DMSO
Description
Potent and specific inhibitor of P-glycoprotein (P-gp, ABCB1); also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).
KEYWORDS: Tariquidar | supplier | P-gp inhibitor | XR 9576 | XR9576 | CAS [206873-63-4] | P-glycoprotein | PGP | breast cancer | BCRP | ABCG2 | multidrug resistance | efflux pump | | axonmedchem |
| LY 335979 - Zosuquidar trihydrochloride | Axon 1839
CAS [167465-36-3]
MF C32H31F2N3O2.3HClMW 636.99
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
High-affinity and selective inhibitor of P-glycoprotein (P-gp; Ki value 59 nM)
KEYWORDS: LY 335979 | supplier | P-gp inhibitor | Zosuquidar HCl | LY335979 | CAS [167465-36-3] | [167354-41-8] | P-glycoprotein | P-gp | ABCB1 | multidrug resistance | | axonmedchem |
| Elacridar hydrochloride - GF 120918A | Axon 1896
CAS [143851-98-3]
MF C34H33N3O5.HClMW 600.10
Purity:
100%
Poorly soluble in DMSO
Description
P-glycoprotein (P-gp) inhibitor; a third generation ABCB1 modulator, preferentially modulating p-gp in brain capillaries; also an inhibitor of breast cancer resistance protein (BCRP)–mediated drug transport
References
Certificates
Categories
Extra info
IELM Kuppens et al. A Phase I, Randomized, Open-Label, Parallel-Cohort, Dose-Finding Study of Elacridar (GF120918) and Oral Topotecan in Cancer Patients. Clin. Cancer Res. 2007, 13, 3276.
M Hubensack et al. Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. J.Cancer Res. Clin. Oncol. 2008, 134(5), 597-607.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
P-glycoprotein
Unclassified
P-gp inhibitor (3rd generation ABCB1 modulator)
Chemical name
N-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-5-methoxy-9-oxo-9,10-dihydroacridine-4-carboxamide hydrochloride
Parent CAS No.
[143664-11-3]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| MC70 hydrochloride | Axon 2591
CAS [N.A.]
MF C24H25NO3.HClMW 411.92
Purity:
98%
Soluble in DMSO
Description
Potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively), with potential as novel anticancer agent with both cytostatic and cytotoxic characteristics. MC70, as an inhibitor of the ABC transporter ABCB1 (aka MDR1), potentiates Doxorubicin efficacy in colon and breast cancer in vitro treatment.
*Sold in collaboration with Biofordrug srl | | axonmedchem |
| CP 100356 hydrochloride | Axon 1654
CAS [142715-48-8 ]
MF C31H36N4O6.HClMW 597.10
Purity:
98%
Soluble in DMSO
Description
Potent inhibitor of P-glycoprotein (P-gp), with Ki to be 58 and 94 nM for 1a and 1b isomers of P-gp; an in vivo probe to selectively assess MDR1/BCRP-mediated drug efflux
References
Certificates
Categories
Extra info
C Wandel et al. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 1999, 59, 3944.
JC Taylor et al. The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br. J. Cancer 1999, 81(5), 783-789.
AS Kalgutkar et al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" (...). J. Pharm. Sci. 2009, 98, 4914.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
P-glycoprotein
Unclassified
P-gp inhibitor
Chemical name
4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-(3,4-dimethoxyphenethyl)-6,7-dimethoxyquinazolin-2-amine
Parent CAS No.
[142716-85-6]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| KS 176 | Axon 2508
CAS [1253452-78-6]
MF C22H19N3O5MW 405.40
Purity:
98%
Soluble in DMSO
Description
Inhibitor of the ABC-transporter Breast Cancer Resistance Protein (BCRP or ABCG2; IC50 value of 1.39 µM). KS 176 is ca 50-fold more potent than Novobiocin (IC50 value 65 µM), and nearly equipotent compared to KO 143 (Axon 1409), and does not show inhibition of P-gp and MRP1.
KEYWORDS: KS 176 | Supplier | BCRP inhibitor | Axon Medchem | Axon 2508 | KS176 | CAS [1253452-78-6] | [93129-94-3] | BCRP | Inhibitor | ABC | transporter | breast | cancer | resistance | protein | Novobiocin | KO143 | KO 143 | | axonmedchem |
| AZD 7762 hydrochloride | Axon 1399
CAS [860352-01-8]
MF C17H19FN4O2S.HClMW 398.88
Purity:
99%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
Potent and selective inhibitor of checkpoint kinase (CHK; IC50 values 5 nM for Chk1/Chk2).
KEYWORDS: AZD 7762 hydrochloride | supplier | CHK inhibitor | AZD7762 HCl | AZD-7762 | CAS [860352-01-8] | DNA-RNA | checkpoint kinase | CHK1 | CHK2 | stem cell | hematopoetic | HCS | | axonmedchem |
| N 6022 | Axon 1822
CAS [1208315-24-5]
MF C24H22N4O3MW 414.46
Purity:
99%
Soluble in DMSO
Description
Potent, specific, and fully reversible inhibitor of S-nitrosoglutathione reductase (GSNOR) with an IC50 of 8 nM and a Ki of 2.5 nM.
Keywords: N 6022 | supplier | GSNOR inhibitor | N6022 | N-6022 | CAS [1208315-24-5] | S-nitrosoglutathione | GSNOR | Inhibitor | Enzymes | | axonmedchem |
| PD 169316 | Axon 1365
CAS [152121-53-4]
MF C20H13FN4O2MW 360.34
Purity:
99%
Soluble in DMSO
Description
Potent, cell-permeable and selective inhibitor of p38 MAP kinase (MAPK); it blocks apoptosis induced by trophic factor withdrawal in non-neuronal and neuronal cell lines
References
Certificates
Categories
Extra info
DJ. Samuvel et al. A Role for p38 Mitogen-Activated Protein Kinase in the Regulation of the Serotonin Transporter: Evidence for Distinct Cellular Mechanisms Involved in Transporter Surface Expression. J. Neuroscience, 2005, 25(1), 29-41.
Y Fu et al. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. Biochem. Biophys. Res. Commun. 2003, 310(2), 391-7.
JL Kummer et al. Apoptosis induced by withdrawal of trophic factors is mediated by p38 mitogen-activated protein kinase. J. Biol. Chem. 1997, 272(33), 20490-20494.
R Nath et al. Inhibition of p38 kinase mimics survival signal-linked protection against apoptosis in rat cerebellar granule neurons. Cell Mol. Biol. Lett. 2001, 6,173-184.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
MAPK (p38)
MAPK
EC 2.7.11.24
MAPK inhibitor (p38 specific)
Chemical name
4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine
Parent CAS No.
[152121-53-4]
Order
Size
Unit Price
Stock
2 mg
€50.00
In Stock | | axonmedchem |
| PD 184352 - CI 1040 | Axon 1368
CAS [212631-79-3]
MF C17H14ClF2IN2O2MW 478.66
Purity:
99%
Soluble in DMSO
Description
Potent, selective and non-competitive inhibitor of MEK 1 (also called MKK 1) and its activation; highly recommended tool to inhibit MKK1 or MKK1 plus MKK5.
A convenient set of FGFR inhibitor SU 5402 (Axon 1667), MEK inhibitor PD 184352 (Axon 1368) and GSK-3 inhibitor CHIR 99021 (Axon 1386) (conventional 3i, Axon 2129), was used together to sustain mouse embryonic stem cell (mESC) self-renewal.
*Promotion | | axonmedchem |
| SB 202190 | Axon 1364
CAS [152121-30-7]
MF C20H14FN3OMW 331.34
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, cell-permeable and selective inhibitor of p38 MAP kinase (MAPK)
References
Certificates
Categories
Extra info
PC Singhal et al. Role of P38 Mitogen-Activated Protein Kinase Phosphorylation and Fas-Fas Ligand Interaction in Morphine-Induced Macrophage Apoptosis. J. Immunol. 2002, 168, 4025-4033.
PR Young et al. Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site. J. Biol. Chem. 1997, 272, 12116-12121.
S Nemoto et al. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J. Biol. Chem. 1998, 273, 16415-16420.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
MAPK (p38)
MAPK
EC 2.7.11.24
MAPK inhibitor (p38 specific)
Chemical name
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-phenol
Parent CAS No.
[152121-30-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| SD 169 | Axon 1357
CAS [1670-87-7]
MF C9H8N2OMW 160.17
Purity:
99%
Soluble in DMSO and Ethanol
Description
ATP-competitive, orally active inhibitor of p38α MAP kinase (IC50 = 3.2 nM); being 38 fold selective vs against p38β MAP kinase (IC50 = 122 nM) and no inhibitory activity against a panel of other kinases including p38γ MAP kinase, ERK2, JNK-1 and MAPKAPK-2.
KEYWORDS: SD 169 | supplier | p38α MAPK inhibitor | SD169 | SD-169 | CAS [1670-87-7] | MAPK | p38-alpha | ATP-competitive | orally active | MAP kinase | ERK2 | JNK1 | MAPKAPK2 | | axonmedchem |
| PD 98059 - NSC 679828 | Axon 1223
CAS [167869-21-8]
MF C16H13NO3MW 267.28
Purity:
99%
Soluble in DMSO
Description
Potent and cell-permeable inhibitor of mitogen-activated protein (MAP) kinase kinase (also known as MAPK/ERK kinase or MEK)
References
Certificates
Categories
Extra info
DR Alessi et al. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J. Biol. Chem. 1995, 270(46), 27489-94.
FJ Dumont et al. Inhibition of T cell activation by pharmacologic disruption of the MEK1/ERK MAP kinase or calcineurin signaling pathways results in differential modulation of cytokine production. J. Immunol. 1998, 160(6), 2579-89.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
MAPK
EC 2.7.12.2
MEK
MEK inhibitor
Chemical name
2-(2-Amino-3-methoxy-phenyl)-chromen-4-one
Parent CAS No.
[167869-21-8]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| SB 203580 | Axon 1363
CAS [152121-47-6]
MF C21H16FN3OSMW 377.43
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, cell-permeable and selective inhibitor of p38 MAP kinase (MAPK). Also available as its water-soluble form, SB 203580 hydrochloride (Axon 1465)
References
Certificates
Categories
Extra info
PC Singhal et al. Role of P38 Mitogen-Activated Protein Kinase Phosphorylation and Fas-Fas Ligand Interaction in Morphine-Induced Macrophage Apoptosis. J. Immunol. 2002, 168, 4025-4033.
PR Young et al. Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site. J. Biol. Chem. 1997, 272, 12116-12121.
H Kankaanranta et al. SB 203580, an Inhibitor of p38 Mitogen-Activated Protein Kinase, Enhances Constitutive Apoptosis of Cytokine-Deprived Human Eosinophils. J. Pharm. Exp. Ther. 1999, 290, 2, 621-628.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
Stem Cell
MAPK (p38)
MAPK
EC 2.7.11.24
MAPK inhibitor (p38 specific)
Chemical name
4-[5-(4-Fluoro-phenyl)-2-(4-methanesulfinyl-phenyl)-3H-imidazol-4-yl]-pyridine
Parent CAS No.
[152121-47-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| SL 327 | Axon 1122
CAS [305350-87-2]
MF C16H12F3N3SMW 335.35
Purity:
99%
Soluble in DMSO
Description
Selective MEK1 and MEK2 inhibitor; brain penetrant in vivo
References
Certificates
Categories
Extra info
X Wang et al. Significant neuroprotection against ischemic brain injury of inhibition of MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis. J. Pharmacol. Exp. Ther. 2003, 304, 172-178.
R Longoni et al. The MEK inhibitor SL327 blocks acquisition but not expression of lithium-induced conditioned place aversion: a behavioral and immunohistochemical study. Psychopharmacology (Berl). 2011, 216(1), 63-73.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.12.2
MEK
MEK1 and MEK2 inhibitor
Chemical name
E/Z-α-[amino[(4-aminophenyl)thio]methylen]-2-(trifluoromethyl)benzeneacetonitrile
Parent CAS No.
[305350-87-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| BIX 02189 | Axon 1809
CAS [1094614-85-3]
MF C27H28N4O2MW 440.54
Purity:
99%
Soluble in DMSO
Description
Selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively
References
Certificates
Categories
Extra info
RJ Tatake et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem. Biophys. Res. Comm. 2008, 377(1), 120–125.
Y Obara and N Nakahata. The signaling pathway leading to extracellular signal-regulated kinase 5 (ERK5) activation via G-proteins and ERK5-dependent neurotrophic effects. Mol. Pharmacol. 2010, 77(1), 10-16.
BA Drew, ME Burowa , BS Beckman. MEK5/ERK5 pathway: The first fifteen years. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 2012, 1825 (1), 37-48.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
MAPK
EC 2.7.12.2
ERK
MEK
MEK5 inhibitor; ERK5 inhibitor
Chemical name
((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide
Parent CAS No.
[1094614-85-3
1265916-41-3 (Z-isomer)]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| XMD 8-92 | Axon 1846
CAS [1234480-50-2]
MF C26H30N6O3MW 474.55
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of big MAP kinase 1 (BMK1/ERK5).
Note: XMD 8-92 is also available as water soluble TFA-salt (Axon 1621)
References
Certificates
Categories
Extra info
Q. Yang et al. Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein. Cancer Cell, 2010, 18(3), 258-267.
Q Yang and JD Lee. Targeting the BMK1 MAP Kinase Pathway in Cancer Therapy. Clin. Cancer Res. 2011, 17, 3527-3532.
BA Drew, ME Burowa , BS Beckman. MEK5/ERK5 pathway: The first fifteen years. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 2012, 1825 (1), 37-48.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.24
ERK
BMK1 inhibitor; ERK5 inhibitor
Chemical name
2-(2-Ethoxy-4-(4-hydroxypiperidin-1-yl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
Source information
Sold under agreement with the Dana-Faber Cancer Institute
Parent CAS No.
[1234480-50-2]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| XMD 8-92 trifluoroacetate | Axon 1621
CAS [1234480-50-2]
MF C26H30N6O3.C2HF3O2MW 588.58
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective inhibitor of big MAP kinase 1 (BMK1/ERK5).
Note: Free base form of XMD 8-92 (Axon 1846) is also available
References
Certificates
Categories
Extra info
Q. Yang et al. Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein. Cancer Cell, 2010, 18(3), 258-267.
Q Yang and JD Lee. Targeting the BMK1 MAP Kinase Pathway in Cancer Therapy. Clin. Cancer Res. 2011, 17, 3527-3532.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.24
ERK
BMK1 inhibitor; ERK5 inhibitor
Chemical name
2-(2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one 2,2,2-trifluoroacetate
Source information
Sold under agreement with the Dana-Faber Cancer Institute
Parent CAS No.
[1234480-50-2]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| Ferrostatin 1 - Fer-1 | Axon 2293
CAS [347174-05-4]
MF C15H22N2O2MW 262.35
Purity:
99%
Soluble in DMSO
Description
Potent inhibitor of erastin-induced ferroptosis, an iron dependent form of cell death morphologically, biochemically and genetically distinct from apoptosis, various forms of necrosis, and autophagy (EC50 value 60 nM in HT-1080 cells). Ferrostatin-1 specifically inhibits cell death induced by RAS-selective lethal compounds (RSLs), but not cell death induced by other oxidative lethal compounds and apoptosis-inducing agents. Ferrostatin-1 does not inhibit ERK phosphorylation or arrest the proliferation of HT-1080 cells, nor does it chelate iron or inhibit protein synthesis. It is capable of blocking the cytotoxic effects of Sorafenib (Axon 1397) in HCC cells.
KEYWORDS: Ferrostatin 1 | supplier | Ferroptosis inhibitor | Fer1 |CAS[347174-05-4] |RAS proteins | Inhibitor | Apoptosis | ROS | RAS-related | nonapoptotic | RSL | Erastin induced | oxidative | cell death | cancer |Huntington's | HD | PUFA | Sorafenib | | axonmedchem |
| FR 180204 | Axon 1694
CAS [865362-74-9]
MF C18H13N7MW 327.34
Purity:
99%
Soluble in DMSO
Description
Selective, cell permeable and ATP-competitive ERK inhibitor; 30-fold selective on ERK over p38α MAPK; FR180204 was shown to inhibit ERK1 (Ki=0.31μM), ERK2 (Ki=0.14 μM) and TGFβ-induced AP-1 activation
References
Certificates
Categories
Extra info
M Ohori et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005, 336(1), 357-363.
M Ohori. ERK inhibitors as a potential new therapy for rheumatoid arthritis. Drug News Perspect. 2008, 21(5), 245-250.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Transcription Factors
MAPK
PI3K-Akt-mTOR
EC 2.7.11.24
ERK
ERK inhibitor; AP-1 inhibitor
Chemical name
3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-7H-pyrazolo[3,4-c]pyridazin-5-amine
Parent CAS No.
[865362-74-9]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| IM 12 | Axon 2511
CAS [1129669-05-1]
MF C22H20FN3O2MW 377.41
Purity:
99%
Soluble in DMSO
Description
GSK-3β inhibitor (IC50 value 53 nM) showing a bell-shaped dose-response relationship. IM12 enhances canonical Wnt signalling, and attenuates cell proliferation and neuronal differentiation of human neural progenitor cells with similar potency as SB 216763 (Axon 1303).
*Promotion | | axonmedchem |
| BAM 7 | Axon 2185
CAS [331244-89-4]
MF C21H19N5O2SMW 405.47
Purity:
98%
Soluble in DMSO
Description
Selective small-molecule activator of proapoptotic BAX (IC50 value 3.3 μM) that binds to the BH3 binding domain without interacting with other BH3-binding pockets of antiapoptotic proteins or proapoptotic BAK. BAM 7 triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death.
References
Certificates
Categories
Extra info
E. Gavathiotis et al. Direct and selective small-molecule activation of proapoptotic BAX. Nat. Chem. Biol. 2012, 8, 639-645.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
p53-Tumor Suppression
Bcl
Selective small-molecule activator of proapoptotic BAX
Chemical name
4-(2-(2-ethoxyphenyl)hydrazono)-3-methyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one
Parent CAS No.
[331244-89-4]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Kobe 0065 | Axon 2302
CAS [436133-68-5]
MF C15H11ClF3N5O4SMW 449.79
Purity:
99%
Soluble in DMSO
Description
Orally active RAS inhibitor with selectivity for HRAS (Ki value of 46 ± 13 μM ) that effectively inhibits both anchorage-dependent and -independent growth and induces apoptosis of H-rasG12V–transformed NIH 3T3 cells. This results in down-regulation of downstream molecules such as MEK/ERK, Akt, and RalA as well as an upstream molecule, Son of sevenless. Kobe 0065 exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-rasG12V gene by oral administration.
References
Certificates
Categories
Extra info
F. Shima et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. PNAS U.S.A. 2013, 110, 8182-8187.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
MAPK
EC 3.6.5.2
HRAS
HRAS inhibitor
Chemical name
N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide
Parent CAS No.
[436133-68-5]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| TIC 10 active isomer - Angular TIC 10 | Active isomer 2 | Axon 2300
CAS [1616632-77-9]
MF C24H26N4OMW 386.49
Purity:
99%
Soluble in DMSO
Description
Potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner. TIC10/ONC201 inactivates kinases Akt and extracellular signal–regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. Efficacious antitumor therapeutic agent
Prime Source Information: | | axonmedchem |
| WP 1066 | Axon 2316
CAS [857064-38-1]
MF C17H14BrN3OMW 356.22
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
Potent inhibitor of JAK2 and STAT3 activity (IC50 values 2.3 µM and 5.6 µM, respectively) that showed selective cytotoxicity toward malignant glioma U87-MG and U373-MG cells at much lower doses than its analogue AG 490 (Axon 1378). Furthermore, WP1066 selectively induces apoptosis in malignant glioma cells by downregulating antiapoptotic proteins (Bcl-XL, Mcl-1 and c-myc) and activating Bax, and significantly inhibited the growth of subcutaneous tumors generated from U87-MG cells in mice.
References
Certificates
Categories
Extra info
A. Iwamaru et al. A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo. Oncogene. 2007, 26, 2435-2444.
M.A. Hatiboglu et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models. Int. J. Cancer. 2012, 131, 8-17.
S. Verstovsek et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin. Cancer Res. 2008, 14, 788-796.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Stem Cell
Transcription Factors
JAK-STAT
EC 2.7.10.2
STAT3
JAK
Potent JAK2 and STAT3 inhibitor and downregulator of antiapoptotic proteins
Chemical name
(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
Parent CAS No.
[857064-38-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| S 12 | Axon 2165
CAS [258264-62-9]
MF C17H12BrNO5MW 390.18
Purity:
99%
Soluble in DMSO
Description
Survivin inhibitor. Alters spindle formation, causing mitotic arrest (by disrupting metaphase at the G2/M stage) and cell death. S 12 inhibits tumor growth in vitro and in vivo, and effectively inhibits cell proliferation and tumor growth independently of p53 status.
References
Certificates
Categories
Extra info
A. Berezov et al. Disabling the mitotic spindle and tumor growth by targeting a cavity-induced allosteric site of survivin. Oncogene 2012, 31, 1938–1948.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Ubiquitin
IAP
Survivin inhibitor
Chemical name
3-(2-(benzo[d][1,3]dioxol-5-yl)-2-oxoethyl)-5-bromo-3-hydroxyindolin-2-one
Parent CAS No.
[258264-62-9]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Fendiline hydrochloride | Axon 2829
CAS [13636-18-5]
MF C23H25N.HClMW 351.91
Purity:
99%
Soluble in DMSO
Description
Fendiline, an L-type calcium channel blocker (IC50 value of 17 µM), is a specific inhibitor of K-Ras plasma membrane targeting (IC50 value of 9.64 µM) with no detectable effect on the localization of H- and N-Ras. Moreover, Fendiline blocked the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras.
KEYWORDS: Fendiline hydrochloride | supplier | KRAS inhibitor | CAS [13636-18-5] | [13042-18-7] | GTP | KRAS | Inhibitor | Enzymes | Calcium Channel blocker | Ca2+ | GTPase | K-Ras | | axonmedchem |
| LCS-1 | Axon 2176
CAS [41931-13-9]
MF C11H8Cl2N2OMW 255.10
Purity:
99%
Soluble in DMSO
Description
Inhibitor of superoxide dismutase 1 (SOD1). Inhibits SOD1 enzymatic activity in vitro (IC50: 0.19 μM for cell growth inhibition in KRAS mutated H358 cell lines). Conversely, (over-) expression of SOD1 cDNA showed about a threefold reduction in sensitivity to LCS-1 and increased proliferation of H358 cells. Additionally, LCS-1 can prevent serum-induced activation of the ERK and PI 3-kinase/AKT signaling pathways.
KEYWORDS: LCS-1 | supplier | SOD1 inhibitor | LCS1 | CAS [41931-13-9] | Superoxide | SOD1 | superoxide dismutase 1 | KRAS | ERK | PI3K | AKT | signaling | lung cancer | | axonmedchem |
| APS-2-79 | Axon 2611
CAS [2002381-31-7]
MF C23H21N3O3.HClMW 423.89
Purity:
98%
Soluble in DMSO
Description
Small molecule that stabilizes the KSR (Kinase suppressor of Ras) inactive state and antagonizes oncogenic Ras signalling (IC50 value 120 nM against ATP-biotin probe-labelling of KSR2). Furthermore, APS-2-79 modulates KSR-dependent MAPK signaling, and increases the potency of several MEK inhibitors, specifically within Ras-mutant cell lines by antagonizing release of negative feedback signaling.
KEYWORDS: APS-2-79 | supplier | KSR/Raf inhibitor | APS2-79 | CAS [2002381-31-7] | [ 2002381-25-9] | MEK | KSR2 | Kinase suppressor of Ras | Raf | MAPK | K-Ras | mitogen activated | oncogenic | | axonmedchem |
| LB 42708 | Axon 1794
CAS [226929-39-1]
MF C30H27BrN4O2MW 555.46
Purity:
99%
Soluble in DMSO
Description
Selective and orally available inhibitor of farnesyltransferase (FTase), with IC50 values of 0.8 nM in vitro and 8 nM in cultured cells against p21-ras farnesylation
References
Certificates
Categories
Extra info
HJ Na et al. Inhibition of Farnesyltransferase Prevents Collagen-Induced Arthritis by Down-Regulation of Inflammatory Gene Expression through Suppression of p21ras-Dependent NF-κB Activation. J. Immunol. 2004, 173, 1276-1283.
CK Kim et al. The farnesyltransferase inhibitor LB42708 suppresses vascular endothelial growth factor-induced angiogenesis by inhibiting Ras-dependent mitogen-activated protein kinase and PI3K/Akt signal pathways. Mol. Pharmacol. 2010, 78, 142-150.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Farnesyltransferase
EC 2.5.1.58
Inhibitor of farnesyltransferase (FTase)
Chemical name
(1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone
Parent CAS No.
[226929-39-1]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ABT 199 - GDC 0199 | Venetoclax | Axon 2141
CAS [1257044-40-8]
MF C45H50ClN7O7SMW 868.44
Purity:
98%
Soluble in DMSO
Description
A highly potent, orally bioavailable BCL-2-selective inhibitor; a new Bcl-2–specific BH3 mimetic efficacious in vivo against mouse lymphomas without provoking thrombocytopenia.
KEYWORDS: ABT 199 | supplier | Bcl-2 inhibitor | GDC 0199 | Venetoclax | ABT199 | GDC0199 | ABT-199 | GDC-0199 | CAS [1257044-40-8] | Non Selective | Bcl | Inhibitor | Proteins | | axonmedchem |
| S3QEL 2 | Axon 2544
CAS [890888-12-7]
MF C19H25N5MW 323.44
Purity:
99%
Soluble in DMSO
Description
Suppressor of superoxide production from mitochondrial complex III (IC50 value 1.7 µM against superoxide production mediated by the outer Q-binding site of complex III (site IIIQo)). S3QEL-2 protects against ROS-induced, JNK-mediated cell stress in pancreatic β-cells, and strongly mitigates the oxidative stress-induced apoptosis that limits the yield of functional β-cells from intact islets. S3QEL-2 modulates HIF-1α activation without directly affecting metabolism.
KEYWORDS: S3QEL 2 | supplier | Complex III modulator | S3QEL2 | CAS [890888-12-7] | Quinol | Complex III | Coenzyme Q | superoxide | ROS | mitochondria | Q-binding site | site III Qo | oxidative stress | reactive oxygen species | | axonmedchem |
| Geranyl pyrophosphate ammonium salt - GPP | Axon 1489
CAS [116057-55-7]
MF C10H20O7P2.3NH3MW 365.30
Purity:
98%
Soluble in water
Description
Substrate for geranyl transferase; an intermediate in the HMG-CoA reductase pathway used by organisms in the biosynthesis of terpenes and terpenoids
References
Certificates
Categories
Extra info
R Croteau. Clomazone Does Not Inhibit the Conversion of Isopentenyl Pyrophosphate to Geranyl, Farnesyl, or Geranylgeranyl Pyrophosphate in Vitro. Plant Physiol. 1992, 98 (4), 1515–1517.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Geranyl Transferase
EC 2.5.1.10
Geranyl transferase substrate
Chemical name
2,6-Octadien-1-ol, 3,7-dimethyl-, trihydrogen pyrophosphate triammonium salt
Parent CAS No.
[763-10-0]
Order
Size
Unit Price
Stock
1 mg
€75.00
In Stock | | axonmedchem |
| AT 406 - SM 406 | Axon 1985
CAS [1071992-99-8]
MF C32H43N5O4MW 561.71
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and orally available antagonist of the inhibitor of apoptosis proteins (IAPs); binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively
References
Certificates
Categories
Extra info
Q Cai et al. A Potent and Orally Active Antagonist (SM-406/AT-406) of Multiple Inhibitor of Apoptosis Proteins (IAPs) in Clinical Development for Cancer Treatment. J. Med. Chem. 2011, 54 (8), 2714–2726.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
IAP
Antagonist of Inhibitor of apoptosis proteins (IAPs)
Chemical name
(5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
Parent CAS No.
[1071992-99-8]
Order
Size
Unit Price
Stock
5 mg
€145.00
In Stock | | axonmedchem |
| ML 210 - CID 49766530 | Axon 2017
CAS [1360705-96-9]
MF C22H20Cl2N4O4MW 475.32
Purity:
100%
Soluble in DMSO
Description
Chemical probe that selectively kills cells induced to express mutant RAS; more specifically, ML210 is a HRAS synthetic lethal compound with nanomolar potencies against two HRASG12V expressing cell lines and 4-fold selectivity against two control cell lines not expressing HRASG12V
References
Certificates
Categories
Extra info
JA Bittker et al. Screen for RAS-Selective Lethal Compounds and VDAC Ligands - Probe 2. Probe Reports NIH Mol. Lib. Program. PMID: 22834036.
M Weïwer et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg. Med. Chem. Lett. 2012, 22(4), 1822-1826.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
MAPK
EC 3.6.5.2
HRAS
Chemical probe that selectively kills cells induced to express mutant RAS
Chemical name
(4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)(5-methyl-4-nitroisoxazol-3-yl)methanone
Parent CAS No.
[1360705-96-9]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |