(+)-JQ1 ≥95%
Supplier: ADIPOGEN CORP MS
Synonyms:
(S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor (IC(50) values of 17.7, 32.6, 76.9 and 12942nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP, respectively. In binding assays, (+)-JQ1 binds competitive with acetyl lysine to BRD4 bromodomain 1 (Kd=50nM) and and BRD4 bromodomain 2 (Kd=90 nM). May be a useful chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis. (+)-JQ1 exhibited strong dose- and time-dependent inhibition of BRDT, a bromodomain-containing protein highly enriched in testis. BRDT is involved in chromatin remodeling and is essential for healthy sperm development. (+)-JQ1 appears to block that function and causes a decrease in sperm viability, being examined as a potential male contraceptive. Inhibitor of inflammation and bone destruction.
Formula:
C₂₃H₂₅ClN₄O₂S Storage Temperature: Freezer |
MDL Number:
MFCD22683748 CAS Number: 1268524-70-4 |
Specification Test Results
Purity |
|
Appearance/Color | Solid. |
Solubility | Soluble in DMSO or ethanol. |
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