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Submit ReviewCPI 203
Description: BET bromodomain inhibitor; arrests cell cycle at G1 phase
Alternative Names: TEN 010
Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98% (HPLC)
Biological Activity for CPI 203
CPI 203 is a BET bromodomain inhibitor. Downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Also enhances the antitumor effect of rapamycin (Cat. No. 1292) in vitro and attenuates rapamycin induced Akt activation. Also enhances fibroblast reprogramming to hiPSCs at low concentration. Orally bioavailable.
Compound Libraries for CPI 203
CPI 203 is also offered as part of the Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for CPI 203
| M. Wt | 399.9 |
| Formula | C19H18ClN5OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1446144-04-2 |
| PubChem ID | 71291068 |
| InChI Key | QECMENZMDBOLDR-AWEZNQCLSA-N |
| Smiles | NC(C[C@@H]1N=C(C4=CC=C(Cl)C=C4)C3=C(SC(C)=C3C)N2C1=NN=C2C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CPI 203
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.99 | 100 | |
| ethanol | 4 | 10 |
Preparing Stock Solutions for CPI 203
The following data is based on the product molecular weight 399.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.5 mL | 12.5 mL | 25.01 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for CPI 203
References for CPI 203
References are publications that support the biological activity of the product.
Wong et al (2014) The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis. 5 e1450 PMID: 25299775
King et al (2013) The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 153 1552 PMID: 23791182
Shao et al (2016) Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 16 3138 PMID: 27653680
If you know of a relevant reference for CPI 203, please let us know.
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Keywords: CPI 203, CPI 203 supplier, CPI203, BET, BRD4, domain, inhibitors, inhibits, (+)-JQ1, analogue, analog, 4499, Myc, G1, cell, cycle, arrest, antitumor, rapamycin, AKT, reprogramming, TEN, 010, Bromodomains, Cell, Cycle, Inhibitors, Stem, Reprogramming, Hematopoietic, Cells, 5331, Tocris Bioscience
1 Citation for CPI 203
Citations are publications that use Tocris products. Selected citations for CPI 203 include:
Shao et al (2016) Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 16 3138 PMID: 27653680
Do you know of a great paper that uses CPI 203 from Tocris? Please let us know.
Reviews for CPI 203
Average Rating: 5 (Based on 1 Review.)
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Reprogramming media with CPI203.
By
Anonymous on 02/23/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: ipsc
50 nM
Literature in this Area
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Stem Cell Research Product Guide
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