GSK-J4 hydrochloride
Cat. No.:YN310276
产品名称: | GSK-J4 hydrochloride |
CAS No.: | 1797983-09-5 |
Chemical Name: | N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochloride |
Synonyms: | |
分子量: | 453.96 |
分子式: | C₂₄H₂₈ClN₅O₂ |
SMILES: | O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1.Cl |
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: | GSK-J4 hydrochloride 是一种有效的 H3K27me3/me2 去甲基化酶JMJD3/KDM6B和UTX/KDM6A双抑制剂,IC50分别为 8.6 μM 和 6.6 μM。GSK-J4 hydrochloride 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α,IC50值为 9 μM。GSK-J4 hydrochloride 是 GSK-J1 的细胞通透性前药。 |
IC50和靶点: | |
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Agger, K., Cloos, P.A.C., Christensen, J., et al.UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and developmentNature449(7163),731-734(2011)
Hübner, M.R., and Spector, D.L.Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulationCold Spring Harb. Symp. Quant. Biol.75,43-49(2010)
Kruidenier, L., Chung, C.W., Cheng, Z., et al.A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage responseNature488,404-408(2012)