A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice

CPI-203 – 10 mg

Brand:
Cayman
CAS:
1446144-04-2
Storage:
-20
UN-No:
Non-Hazardous - /

(+)-JQ1 (Item No. 11187) binds to the acetyl-lysine recognition pocket of bromodomains 1 and 2 on BRD4 with Kd values of ~50 and 90 nM, respectively.{19044} This displaces BRD4 from nuclear chromatin in cells, inducing differentiation and growth arrest in midline carcinoma cells.{19044} CPI-203 is a primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration.{24965} It is comparable or superior to (+)-JQ1 in inhibiting BRD4 binding and action in vitro or in cells.{24965,24964} CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice.{24965}  

 

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Description

A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice

Formal 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

Synonyms: 

Molecular weight: 399.9

CAS: 1446144-04-2

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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