2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
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(+)-JQ1 is a BET potent BET bromodomain Inhibitor. Bromodomain and extra terminal domain (BET) proteins are important epigenetic regulators facilitating the transcription of genes in chromatin areas linked to acetylated histones. JQ1 has antiproliferative activity against many cancers, mainly through inhibition of c-MYC and upregulation of p21. JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer. JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models. JQ1 disrupts human dendritic cell maturation by inhibiting STAT5.
Name: (+)-JQ1
CAS#: 1268524-70-4
Chemical Formula: C23H25ClN4O2S
Exact Mass: 456.13867
Molecular Weight: 456.99
Elemental Analysis: C, 60.45; H, 5.51; Cl, 7.76; N, 12.26; O, 7.00; S, 7.02
Synonym: (+)-JQ1; (+)-JQ-1; (+)-JQ 1; Bromodomain Inhibitor
IUPAC/Chemical Name: tert-butyl (S)-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
InChi Key: DNVXATUJJDPFDM-KRWDZBQOSA-N
InChi Code: 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
SMILES Code: O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
REFERENCES
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5: Kumar K, Raza SS, Knab LM, Chow CR, Kwok B, Bentrem DJ, Popovic R, Ebine K, Licht JD, Munshi HG. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1. Sci Rep. 2015 Mar 25;5:9489. doi: 10.1038/srep09489. PubMed PMID: 25807524.
6: Qiu H, Jackson AL, Kilgore JE, Zhong Y, Chan LL, Gehrig PA, Zhou C, Bae-Jump VL. JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer. Oncotarget. 2015 Mar 30;6(9):6915-30. PubMed PMID: 25762632.
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9: Horne GA, Stewart HJ, Dickson J, Knapp S, Ramsahoye B, Chevassut T. Nanog requires BRD4 to maintain murine embryonic stem cell pluripotency and is suppressed by bromodomain inhibitor JQ1 together with Lefty1. Stem Cells Dev. 2015 Apr 1;24(7):879-91. doi: 10.1089/scd.2014.0302. Epub 2014 Dec 17. PubMed PMID: 25393219; PubMed Central PMCID: PMC4367495.
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