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Further Information
Solid.
1268524-70-4
32160000
liquid
InChI=1S/C23H25ClN4O2S/c1-12-13(2)31-22-19(12)20(15-7-9-16(24)10-8-15)25-17(11-18(29)30-23(4,5)6)21-27-26-14(3)28(21)22/h7-10,17H,11H2,1-6H3/t17-/m0/s1
DNVXATUJJDPFDM-KRWDZBQOSA-N
Chemical. CAS: 1268524-70-4. Formula: C23H25ClN4O2S. MW: 457. (+)-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.
C23H25ClN4O2S
457
Plastic Vial
(+)-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.
>95%
Soluble in DMSO or ethanol.
Non-hazardous
Protein Kinase Modulators
12352200
Stable for at least 2 years after receipt when stored at -20°C.