1884712-47-3 Usage
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).
Check Digit Verification of cas no
The CAS Registry Mumber 1884712-47-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,8,4,7,1 and 2 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1884712-47:
(9*1)+(8*8)+(7*8)+(6*4)+(5*7)+(4*1)+(3*2)+(2*4)+(1*7)=213
213 % 10 = 3
So 1884712-47-3 is a valid CAS Registry Number.
1884712-47-3Relevant articles and documents
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)
Taylor, Alexander M.,C?té, Alexandre,Hewitt, Michael C.,Pastor, Richard,Leblanc, Yves,Nasveschuk, Christopher G.,Romero, F. Anthony,Crawford, Terry D.,Cantone, Nico,Jayaram, Hariharan,Setser, Jeremy,Murray, Jeremy,Beresini, Maureen H.,De Leon Boenig, Gladys,Chen, Zhongguo,Conery, Andrew R.,Cummings, Richard T.,Dakin, Leslie A.,Flynn, E. Megan,Huang, Oscar W.,Kaufman, Susan,Keller, Patricia J.,Kiefer, James R.,Lai, Tommy,Li, Yingjie,Liao, Jiangpeng,Liu, Wenfeng,Lu, Henry,Pardo, Eneida,Tsui, Vickie,Wang, Jian,Wang, Yongyun,Xu, Zhaowu,Yan, Fen,Yu, Dong,Zawadzke, Laura,Zhu, Xiaoqin,Zhu, Xiaoyu,Sims, Robert J.,Cochran, Andrea G.,Bellon, Steve,Audia, James E.,Magnuson, Steven,Albrecht, Brian K.
, p. 531 - 536 (2016/06/01)
CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively targeting bromodomains, we set out to identify a CBP/EP300 bromodomain inhibitor that was potent both in vitro and in cellular target engagement assays and was selective over the other members of the bromodomain family. Reported here is a series of cell-potent and selective probes of the CBP/EP300 bromodomains, derived from the fragment screening hit 4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one.
