(+)-JQ1

Article No SYN-3004-M010
Product Type Chemicals & Biochemicals
Research Area Inflammation
Format Powder
Size 10 mg

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Specifications

CAS No 1268524-70-4
MW 457
Country Availability DK, EE, FI, IS, LT, LV, NO, SE
Data Sheet Link https://www.adipogen.com/productmanagement/resource/download/type/sheet/id/3522
Description (+)-JQ1
Supplier Adipogen Life Sciences
Notes 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.
Molecular Formula C23H25ClN4O2S
Purity >95%
References Selective inhibition of BET bromodomains: P. Filippakopoulos, et al.; Nature 468, 1067 (2010) | BET inhibitor JQ1 blocks inflammation and bone destruction: S. Meng, et al.; J. Dent. Res. 93, 657 (2014)
Solubility Soluble in DMSO or ethanol.
Storage -20°C
Technical Specifications (+)-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.

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