A selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM; ~90% inhibition in FRAP assay at 0.1 µM and 1 µM

BI-9564 – 1 mg

Brand:
Cayman
CAS:
1883429-22-8
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively.{30788,31210} It does not bind to other bromodomain-containing BET family members (IC50s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 µM.{30788} BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day).{30788} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM; ~90% inhibition in FRAP assay at 0.1 µM and 1 µM, respectively); inhibits the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day)

Formal name: 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

Synonyms: 

Molecular weight: 353.4

CAS: 1883429-22-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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