Chemical Name: N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazol[1,2-a]pyrimidin-3-yl)-2-thiazolamine
BMI-1 inhibitor
Molecular Weight:
495.19
Purity:
98% by HPLC , NMR (Conforms)
Form:
Yellow solid
CAS Number:
[315704-66-6]
Formula:
C17H13Br2N5OS
Application Notes:
An inhibitor of BMI-1 (IC50 = 500 nM), part of the polycomb repressive complex 1 (PCR1).1 It inhibited endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells resulting in reduced tumor volume as well as reduced cancer initiating cell (CIC) number. PTC-209 displayed potent in vivo antitumor effects in several cancer models including breast2, head and neck3, glioblastoma4, prostate5, colon5, and rhabdomyosarcoma6. It also promoted chemically-induced direct cardiac reprogramming of cardiac fibroblasts into cardiac myocytes.7,8
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