PTC-209 | BMI-1 inhibitor

PTC-209 is 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

References:

  1. Kreso et al. (2013), Self-renewal as a therapeutic target in human colorectal cancer; Nat. Med. 20 29
  2. Srinivasan et al. (2017), Downregulation of Bmi1 in breast cancer stem cells suppresses tumor growth and proliferation; Oncotarget. 8 38731
  3. Wang et al. (2017), Pharmacological inhibition of Bmi1 by PTC-209 impaired tumor growth in head neck squamous cell carcinoma; Cancer Cell Int. 17 107
  4. Kong et al. (2018), Targeting of BMI-1 with PTC-209 inhibits glioblastoma development; Cell Cycle 17 1199
  5. Elango et al. (2019), Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo; Sci. Rep. 9 13696
  6. Shields et al. (2021), Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target; Mol. Oncol. 1002/1878-0261.12914
  7. Guo et al. (2019), Chemical suppression of specific C-C chemokine signaling pathways enhances cardiac reprogramming; J. Biol. Chem. 294 9134
  8. Testa et al.. (2020),Bmi1 inhibitor PTC-209 promotes Chemically-induced Direct Cardiac Reprogramming of cardiac fibroblasts into cardiomyocytes; Sci. Rep. 10 7129
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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CAS:
315704-66-6
Catalog Number:
10-4022
Activity:
BMI-1 inhibitor
Chemical Names:
N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazol[1,2-a]pyrimidin-3-yl)-2-thiazolamine
Molecular Weight:
495.19
Molecular Formula:
C17H13Br2N5OS
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

PTC-209 | BMI-1 inhibitor

$65.00$240.00

CAS:
315704-66-6
Catalog Number:
10-4022
Activity:
BMI-1 inhibitor
Chemical Names:
N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazol[1,2-a]pyrimidin-3-yl)-2-thiazolamine
Molecular Weight:
495.19
Molecular Formula:
C17H13Br2N5OS
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
Clear
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