GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a K i of 10 nM and an IC 50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
性状
Solid
IC50 & Target[1][2]
KDM5 10 nM (Ki) KDM5 26 nM (IC50)
体外研究(In Vitro)
GSK467 (0-100 μM; 6 days) shows antiproliferative effect against human multiple myeloma tumor cells.GSK467 is located in the 2-OG-binding pocket.GSK467 inhibits spheroid formation, colony formation, invasion and migration of HCC cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
GSK-467 can inhibit the proliferation and growth of HCC tumor cells by promoting the expression of miR-448 and inhibiting the YTHDF3/ITGA6 pathway in female BALB/c nude mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45.[2]. Fu YD, et al. Targeting histone demethylase KDM5B for cancer treatment. Eur J Med Chem. 2020 Dec 15;208:112760.[3]. Guo JC, et al. KDM5B promotes self-renewal of h
溶解度数据
In Vitro: DMSO : 20.83 mg/mL (65.23 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液