cpi-637
- CAS No.
- 1884712-47-3
- Chemical Name:
- cpi-637
- Synonyms
- CPI-637 >=98% (HPLC);CPI-637;CPI 637;CPI637;Inhibitor,inhibit,HAT,Epigenetic Reader Domain,CPI637,CPI-637,Histone Acetyltransferase,HATs;(R)-4-Methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one;2H-1,5-Benzodiazepin-2-one, 1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-, (4R)-
- CBNumber:
- CB13139528
- Molecular Formula:
- C22H22N6O
- Molecular Weight:
- 386.45
- MDL Number:
- MFCD30489741
- MOL File:
- 1884712-47-3.mol
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|
Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P305+P351+P338 | |||||||||
NFPA 704 |
|
cpi-637 price More Price(11)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 23500 | CPI-637 ≥98% | 1884712-47-3 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 23500 | CPI-637 ≥98% | 1884712-47-3 | 5mg | $122 | 2024-03-01 | Buy |
Cayman Chemical | 23500 | CPI-637 ≥98% | 1884712-47-3 | 10mg | $169 | 2024-03-01 | Buy |
Cayman Chemical | 23500 | CPI-637 ≥98% | 1884712-47-3 | 25mg | $343 | 2024-03-01 | Buy |
ApexBio Technology | B7801 | CPI-637 | 1884712-47-3 | 50mg | $348 | 2021-12-16 | Buy |
cpi-637 Chemical Properties,Uses,Production
Description
CPI-637 is an inhibitor of cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), a homologous pair of bromodomain-containing proteins (IC50s = 30 and 51 nM in a time-resolved-FRET (TR-FRET) assay). It is selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 μM), however, CPI-637 is active at bromodomain BRD9 (IC50 = 0.73 μM). CPI-637 also inhibits MYC expression (EC50 = 0.6 μM) in AMO-1 cells.
in vitro
previous study found that cpi-637 was potent against ep300, and its opposite enantiomer showed a over 200-fold loss in potency. moreover, the biochemical potency of cpi-637 translated well into cells with cbp bret ec50 of 0.3 μm, and cpi-637 demonstrated a more than 700-fold selectivity over the bet family of bromodomains. in addition, cpi-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against brd9. furthermore, it was found that cpi-637 was able to inhibit the expression of myc with an ec50 of 0.60 μm in a cellular assay,. [1].
IC 50
0.03 and 11.0 μm for cbp/ep300 and brd4, respectively.
References
[1] taylor, a. m. et al. fragment-based discovery of a selective and cell-active benzodiazepinone cbp/ep300 bromodomain inhibitor (cpi-637). acs medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).
cpi-637 Preparation Products And Raw materials
Raw materials
Preparation Products
cpi-637 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32165 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
Chemia Biotechnology(Shanghai) Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38632 | 58 | |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57505 | 58 |
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |