产品名称 SGI 1027 dihydrochloride - S 1027 dihydrochloride
产品货号 Axon 2347 CAS [N.A.] MF C27H25Cl2N7OMW 534.44 Purity: 99% Soluble in DMSO Description SGI 1027 inhibits DNMT activity (IC50 values 35 μM and 10 μM for DNMT1 and DNMT3A2/3L, respectively) in colon cancer cell lines, and was shown to degrade the enzymes. Prolonged treatment of RKO cells with SGI 1027 led to demethylation and reexpression of the silenced tumor suppressor genes (TSGs) P16, MLH1, and TIMP3 and did not exhibit significant toxicity in a rat hepatoma (H4IIE) cell line. SGI 1027 shows moderate affinity (IC 50 value 65 μM) for G9a-like protein (GLP), another AdoMet-dependent enzyme, as well. References Certificates Categories Extra info J. Datta et al.A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009, 69, 4277-4285.   S. Valente et al. Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J. Med. Chem. 2014, 57, 701-713.   E. Rilova et al. Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation. ChemMedChem. 2014, 9, 590-601. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Epigenetics Stem Cell EC 2.1.1.37 DNA methyltransferase Inhibitor of DNMT activity in colon cancer cell lines Chemical name N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide dihydrochloride Parent CAS No. [1020149-73-8] Order Size Unit Price Stock 10 mg €110.00 In Stock
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SGI 1027 dihydrochloride - S 1027 dihydrochloride

Based on 12 reference(s) in Google Scholar 9 10 12

Axon 2347

CAS [N.A.]

MF C27H25Cl2N7O
MW 534.44

  • Purity: 99%
  • Soluble in DMSO

SGI 1027 dihydrochloride

Description

SGI 1027 inhibits DNMT activity (IC50 values 35 μM and 10 μM for DNMT1 and DNMT3A2/3L, respectively) in colon cancer cell lines, and was shown to degrade the enzymes. Prolonged treatment of RKO cells with SGI 1027 led to demethylation and reexpression of the silenced tumor suppressor genes (TSGs) P16, MLH1, and TIMP3 and did not exhibit significant toxicity in a rat hepatoma (H4IIE) cell line. SGI 1027 shows moderate affinity (IC 50 value 65 μM) for G9a-like protein (GLP), another AdoMet-dependent enzyme, as well.
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