PTC-209, BMI-1 inhibitor (TBI4022)

Description

Product Details

Formal Name: N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazol[1,2-a]pyrimidin-3-yl)-2-thiazolamine

Molecular Formula: C₁₇H₁₃Br₂N₅OS

Formula Weight: 495.20

CAS Number: 315704-66-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

BMI-1 inhibitor

Functions

Inhibitor of BMI-1 (IC50 = 500 nM), part of the polycomb repressive complex 1 (PCR1). 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 breast, head and neck, glioblastoma, prostate, colon, and rhabdomyosarcoma. It also promoted chemically-induced direct cardiac reprogramming of cardiac fibroblasts into cardiac myocytes.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.