PTC-209 (PTC209
- Product Name
- PTC-209 (PTC209
- CAS No.
- 315704-66-6
- Chemical Name
- PTC-209 (PTC209
- Synonyms
- PTC-209;CS-1315;PTC 209 NEW;PTC-209, >=98%;PTC-209 (PTC209;PTC-209 free base;N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine;N-(2,6-dibroMo-4-Methoxyphenyl)-4-(2-MethyliMidazo[1,2-a]pyriMidin-3-yl)thiazol-2-aMine;2-THIAZOLAMINE, N-(2,6-DIBROMO-4-METHOXYPHENYL)-4-(2-METHYLIMIDAZO[1,2-A]PYRIMIDIN-3-YL)-;N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine PTC-209
- CBNumber
- CB02682264
- Molecular Formula
- C17H13Br2N5OS
- Formula Weight
- 495.19
- MOL File
- 315704-66-6.mol
PTC-209 (PTC209 Property
- Density
- 1.86±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble20mg/mL, clear
- pka
- 3.77±0.30(Predicted)
- form
- powder
- color
- white to brown
- Stability:
- Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- CAS DataBase Reference
- 315704-66-6
N-Bromosuccinimide Price
- Product number
- SML1143
- Product name
- PTC-209
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $118
- Updated
- 2024/03/01
- Product number
- SML1143
- Product name
- PTC-209
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $476
- Updated
- 2024/03/01
- Product number
- 5.30154
- Product name
- BMI-1 Expression Inhibitor, PTC-209 - CAS 315704-66-6 - Calbiochem
- Purity
- A cell-permeable compound that downregulates cellular BMI-1 levels by inhibiting BMI-1 transcription.
- Packaging
- 10MG
- Price
- $265
- Updated
- 2024/03/01
- Product number
- 16277
- Product name
- PTC-209
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $29
- Updated
- 2024/03/01
- Product number
- 16277
- Product name
- PTC-209
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $109
- Updated
- 2024/03/01
PTC-209 (PTC209 Chemical Properties,Usage,Production
Description
PTC-209 (315704-66-6) 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
Uses
Polycomb complex protein BMI-1 is a polycomb ring finger oncogene that regulates the p16 and p19 cell cycle inhibitor genes. It is necessary for efficient self-renewing cell divisions of stem cells in several tissues and can be over-expressed in tumors. PTC-209 is a BMI-1 inhibitor (IC50 = ~ 0.5 μM) that irreversibly impairs colorectal cancer-initiating cell (CIC) growth. It reduces tumor growth in CIC xenograft assays and abrogates colorectal cancer cell self-renewal in vivo, reducing their tumorigenic potential.[Cayman Chemical]
Uses
PTC 209 is a compound involved in thedown-reglation of NOTCH signaling and aids in suppressing acute leukemia cells.
Uses
PTC-209 has been used as a B lymphoma Mo-MLV insertion region 1 homolog (BMI1) inhibitor to study its effects on:
- the cell viability of canine osteosarcoma (OSA) cell lines
- lipidated microtubule-associated protein 1 light chain 3 (LC3B-II) and Sequestosome 1 (SQSTM1) protein levels in ovarian cancer (OvCa) cells
- cardiac reprogramming efficiency in mouse embryonic fibroblasts (MEF)
Biochem/physiol Actions
PTC-209 inhibits the expression of the oncogene BMI-1 (B lymphoma Mo-MLV insertion region 1 homolog), which encodes a polycomb group RING finger protein involved in cell cycle. PTC-209 lowers the self-renewal properties of colorectal cancer-initiating cells (CICs) The compound inhibits tumor growth, and reduces the levels of CICs present in colon cancer tumor xenografts in mice.
storage
Store at -20°C
References
Kreso et al. (2013), Self-renewal as a therapeutic target in human colorectal cancer; Nat. Med. 20 29 Srinivasan et al. (2017), Downregulation of Bmi1 in breast cancer stem cells suppresses tumor growth and proliferation; Oncotarget. 8 38731 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 Kong et al. (2018), Targeting of BMI-1 with PTC-209 inhibits glioblastoma development; Cell Cycle 17 1199 Elango et al. (2019), Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo; Sci. Rep. 9 13696 Shields et al. (2021), Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target; Mol. Oncol. 1002/1878-0261.12914 Guo et al. (2019), Chemical suppression of specific C-C chemokine signaling pathways enhances cardiac reprogramming; J. Biol. Chem. 294 9134 Testa et al.. (2020),Bmi1 inhibitor PTC-209 promotes Chemically-induced Direct Cardiac Reprogramming of cardiac fibroblasts into cardiomyocytes; Sci. Rep. 10 7129
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View Lastest Price from PTC-209 (PTC209 manufacturers
- Product
- PTC-209 (PTC209 315704-66-6
- Price
- US $9.80/KG
- Min. Order
- 1KG
- Purity
- ≥98%
- Supply Ability
- 20 tons
- Release date
- 2020-01-09