JQ1 Inhibitor CAS No. 1268524-70-4

Cat. No.	Name	Size	Price	Add Cart
KI2269	JQ1	10 mg	$432
KI2269	JQ1	25 mg	$912

Chemical Characteristic

Product Name	JQ1
CAS No.	1268524-70-4
Molecular Weight	457
Formula	C₂₃H₂₅ClN₄O₂S
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	C(=O)(CC1c2n(c3c(C(=N1)c1ccc(cc1)Cl)c(c(s3)C)C)c(nn2)C)OC(C)(C)C
Chemical Structure

Biological activities

JQ1 is a small molecule inhibitor of BET bromodomains. JQ1 is widely used as an anti-tumor drug against multiple myeloma, acute myeloid leukemia and other cancer types that are addicted to the c-Myc oncogene.^[1] JQ1 blocks the interaction of bromodomains of BET proteins with acetylated lysines (Ac). Meanwhile, JQ1 inhibits the proliferation of tumour cells expressing the BRD4??UT oncoprotein.^[2] JQ1 inhibits the binding of Brd4 to acetylated chromatin at the c-Myc gene promoter and IgH enhancers. In addition, JQ1 increases the promoter binding by CDK9, another key SEC component.^[1] JQ1 stimulates the HIV LTR-driven GFP expression in J-Lat A2 cells in a dose- and time-dependent manner.^[1] In vitro, JQ1 partially reduces the levels of AFF4, CDK9 and CTD-Ser2P at the promoter, which is consistent with JQ1?? partial suppression of Tat-independent HIV transcription in NH1 cells. In HeLa cells, JQ1 also increases Thr186 phosphorylation under conditions of Tat expression.^[1] In vivo, JQ1 causes cancer cells to differentiate and stop growing in mouse xenografts with the disease. Furthermore, JQ1 slows tumor growth in mouse models of Burkitt?? lymphoma and AML.^[3]

Protocols

In vitro, JQ1 is dissolved in DMSO.^[1]

References

[1] Li Z, et al. The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Nucleic Acids Res. 2013,41(1):277-287. [2] Taverna SD, et al. Drug discovery: Reader's block. Nature. 2010, 468(7327):1050-1051. [3] Moyer MW. First drugs found to inhibit elusive cancer target. Nat Med. 2011, 17(11):1325.

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