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(+)-JQ1
- JQ1
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C23H25ClN4O2S
- MW: 456.99
Description
(+)-JQ1 is a potent and selective BET (bromodomain and extraterminal domain) bromodomain inhibitor that blocks the interaction between BET proteins and acetylated histones. It inhibits binding of a tetra-acetylated histone H4 peptide to BRD4 with IC50 values of 77 nM and 33 nM for the first and second bromodomains, respectively.
BET family proteins, including BRD2, BRD3, BRD4, and BRDT, function as epigenetic readers that recognize acetylated lysine residues on histones and regulate transcriptional programs involved in inflammation, cancer, cell cycle progression, and viral latency. (+)-JQ1 has become one of the most widely used chemical probes in epigenetics and transcriptional regulation research. The compoundssuppresses macrophage inflammatory responses through BET inhibition and has been shown to reactivate latent HIV by antagonizing BRD4-mediated inhibition of Tat-dependent transcription. In oncology research, cotreatment with (+)-JQ1 and the FLT3 inhibitor AC220 (Axon 1696) synergistically induces apoptosis in FLT3-ITD-positive acute myeloid leukemia (AML) progenitor cells.
Key Features
- Potent and selective BET bromodomain inhibitor
- Targets BRD4 bromodomains with IC50 values of 77 nM and 33 nM
- Widely used chemical probe for BET protein biology
- Suppresses inflammatory gene expression
- Useful tool for epigenetics, oncology, and HIV latency research
Applications
- BET protein and bromodomain research
- Epigenetics and transcriptional regulation studies
- Cancer biology and AML investigations
- Inflammation and immune signaling research
- HIV latency and viral reactivation studies
Related Products
(-)-JQ1 (Axon 3873) is available as the inactive control compound for (+)-JQ1 and is recommended for validating BET-dependent biological effects. For leukemia research, AC220 (Axon 1696) can be used in combination with (+)-JQ1, as synergistic induction of apoptosis has been reported in FLT3-ITD-positive AML cells.
More Information
| Parent CAS No. | 1268524-70-4 |
|---|---|
| Chemical Name | (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 |
| SMILES | N12C(C)=NN=C1[C@H](CC(OC(C)(C)C)=O)N=C(C1=CC=C(Cl)C=C1)C1C(C)=C(C)SC=12 |&1:6,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | DNVXATUJJDPFDM-KRWDZBQOSA-N |
| CID | 46907787 |
| Short Description | BET inhibitor |
References
- P Filippakopoulos et al. Selective inhibition of BET bromodomains. Nature 2010, 468(7327), 1067-1073.
- MM Matzuk et al. Small-molecule inhibition of BRDT for male contraception. Cell 2012, 150(4), 673-684.
- W Fiskus et al. BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD. Mol Cancer Ther. 2014 Oct;13(10):2315-27.
- AC Belkina et al. BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses. J Immunol. 2013 Apr 1;190(7):3670-8.
- Z Li et al. The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Nucleic Acids Res. 2013 Jan 7;41(1):277-87.
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