(+)-JQ-1
Cat. No.:YN430158
产品名称: | (+)-JQ-1 |
CAS No.: | 1268524-70-4 |
Chemical Name: | (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 1,1-dimethylethyl ester |
Synonyms: | JQ1 |
分子量: | 456.99 |
分子式: | C₂₃H₂₅ClN₄O₂S |
SMILES: | O=C(C[C@H]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | (+)-JQ-1 (JQ1) 是一种有效特异性的可逆BET bromodomain抑制剂,抑制BRD4(1/2)的IC50分别为 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。 |
IC50和靶点: | |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Filippakopoulos, P., Qi, J., Picaud, S., et al.Selective inhibition of BET bromodomainsNature468(7327),1067-1073(2010)
Dawson, M.A., Kouzarides, T., and Huntly, B.J.Targeting epigenetic readers in cancerN. Engl. J. Med.367(7),647-657(2012)
Delmore, J.E., Issa, G.C., Lemieux, M.E., et al.BET bromodomain inhibition as a therapeutic strategy to target c-MycCell146(6),904-917(2011)
Mertz, J.A., Conery, A.R., Bryant, B.M., et al.Targeting MYC dependence in cancer by inhibiting BET bromodomainsProc. Natl. Acad. Sci. USA108(40),16669-16674(2011)
Dawson, M.A., Prinjha, R.K., Dittmann, A., et al.Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemiaNature478,529-533(2011)