219:
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390:. It was developed by the James Bradner laboratory at Brigham and Women's Hospital and named after chemist Jun Qi. The chemical structure was inspired by patent of similar BET inhibitors by Mitsubishi Tanabe Pharma. Structurally it is related to
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340:
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
402:
Interest in JQ1 as a cancer therapeutic stemmed from its ability to inhibit BRD4 and BRD3, both of which form fusion oncogenes that drive
394:. While widely used in laboratory applications, JQ1 is not itself being used in human clinical trials because it has a short half life.
906:
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44:
702:"BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia"
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484:. National Library of Medicine, National Institutes of Health, U.S. Department of Health and Human Services.
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structurally similar to JQ1 are being tested in clinical trials for a variety of cancers including
73:
700:
Da Costa D, Agathanggelou A, Perry T, Weston V, Petermann E, Zlatanou A, et al. (July 2013).
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749:
Banerjee C, Archin N, Michaels D, Belkina AC, Denis GV, Bradner J, et al. (December 2012).
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Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, et al. (December 2010).
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Schwartz BE, Hofer MD, Lemieux ME, Bauer DE, Cameron MJ, West NH, et al. (April 2011).
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Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, et al. (August 2012).
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infection, as a male contraceptive, and in slowing the progression of heart disease.
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Anand P, Brown JD, Lin CY, Qi J, Zhang R, Artero PC, et al. (August 2013).
406:. Subsequent work demonstrated that a number of cancers including some forms of
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653:"The mechanisms behind the therapeutic activity of BET bromodomain inhibition"
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751:"BET bromodomain inhibition as a novel strategy for reactivation of HIV-1"
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JQ1 has also been investigated for other applications in the treatment of
849:"BET bromodomains mediate transcriptional pause release in heart failure"
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717:
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93:
563:"Differentiation of NUT midline carcinoma by epigenomic reprogramming"
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20:
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O=C(C1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C
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612:"BET domain co-regulators in obesity, inflammation and cancer"
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800:"Small-molecule inhibition of BRDT for male contraception"
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60:-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6
8:
362:and a potent inhibitor of the BET family of
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506:"Selective inhibition of BET bromodomains"
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64:-thieno triazolo diazepin-6-yl)acetate
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7:
418:(ALL) were also highly sensitive to
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610:Belkina AC, Denis GV (June 2012).
478:"Studies found for: bet inhibitor"
398:Efficacy in mouse models of cancer
378:, and the testis-specific protein
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27:
345:Key:DNVXATUJJDPFDM-KRWDZBQOSA-N
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1:
651:Shi J, Vakoc CR (June 2014).
579:10.1158/0008-5472.CAN-10-3513
755:Journal of Leukocyte Biology
669:10.1016/j.molcel.2014.05.016
416:acute lymphoblastic leukemia
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865:10.1016/j.cell.2013.07.013
816:10.1016/j.cell.2012.06.045
408:acute myelogenous leukemia
230:Chemical and physical data
907:Experimental cancer drugs
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308:
40:
26:
912:Thienotriazolodiazepines
902:Contraception for males
366:proteins which include
360:thienotriazolodiazepine
616:Nature Reviews. Cancer
426:In other applications
404:NUT midline carcinoma
388:NUT midline carcinoma
917:Tert-butyl compounds
706:Blood Cancer Journal
767:10.1189/jlb.0312165
718:10.1038/bcj.2013.24
530:10.1038/nature09504
522:2010Natur.468.1067F
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482:ClinicalTrials.Gov
444:Male contraceptive
516:(7327): 1067–73.
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299:Interactive image
199:CompTox Dashboard
16:Chemical compound
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761:(6): 1147–54.
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382:in mammals.
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188:CHEBI:137113
83:1268524-70-4
61:
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53:
712:(7): e126.
364:bromodomain
282: g·mol
36:Identifiers
896:Categories
465:References
414:(MM), and
287:3D model (
275:Molar mass
168:1MRH0IMX0W
139:ChemSpider
119:IUPHAR/BPS
74:CAS Number
45:IUPAC name
454:TDI-11861
883:23911322
834:22901802
785:22802445
736:23872705
687:24905006
646:22722403
597:21447744
548:20871596
449:CDD-2807
438:See also
148:26323622
108:46907787
874:4090947
825:3420011
776:3501896
727:3730202
678:4236231
637:3934568
588:3070805
539:3010259
518:Bibcode
410:(AML),
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94:PubChem
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510:Nature
459:YCT529
313:SMILES
280:456.99
358:is a
333:InChI
289:JSmol
179:ChEBI
879:PMID
853:Cell
830:PMID
804:Cell
781:PMID
732:PMID
683:PMID
642:PMID
593:PMID
544:PMID
380:BRDT
376:BRD4
372:BRD3
368:BRD2
159:UNII
128:7511
58:tert
869:PMC
861:doi
857:154
820:PMC
812:doi
808:150
771:PMC
763:doi
722:PMC
714:doi
673:PMC
665:doi
632:PMC
624:doi
583:PMC
575:doi
534:PMC
526:doi
514:468
432:HIV
356:JQ1
204:EPA
98:CID
21:JQ1
898::
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