An inhibitor of CBP/EP300 bromodomains (IC50s = 30 and 51 nM in a TR-FRET assay); selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 μM); is active at bromodomain BRD9 (IC50 = 0.73 μM); inhibits CBP (IC50 = 0.3 μM in a BRET assay) and inhibits MYC expression (EC50 = 0.6 μM) in AMO-1 cells

CPI-637 – 1 mg

Brand:
Cayman
CAS:
1884712-47-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{40412} 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.  

 

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SKU: 23500 - 1 mg Category:

Description

An inhibitor of CBP/EP300 bromodomains (IC50s = 30 and 51 nM in a TR-FRET assay); selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 μM); is active at bromodomain BRD9 (IC50 = 0.73 μM); inhibits CBP (IC50 = 0.3 μM in a BRET assay) and inhibits MYC expression (EC50 = 0.6 μM) in AMO-1 cells

Formal name: (4R)-1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-2H-1,5-benzodiazepin-2-one

Synonyms: 

Molecular weight: 386.5

CAS: 1884712-47-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area

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