GSK503 - Histone Methyltransferase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK503Cat. No.: HY-12856CAS No.: 1346572-63-1分式: CHNO分量: 526.67作靶点: Histone Methyltransferase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 44 mg/mL (83.54 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8987 mL 9.4936 mL 18.9872 mL5 mM 0.3797 mL 1.8987 mL 3.7974 mL10 mM 0.1899 mL 0.9494 mL 1.8987 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 GSK503效特异性的EZH2甲基转移酶抑制剂，Kiapp值为3到27 nM。IC50 & Target Ki:

3、 3 to 27 nM (EZH2) 1体外研究GSK503 inhibits the methyltransferase activity of wild type and mutant EZH2 with similar potency (Kiapp=3-27 nM) and is structurally related to GSK126 and GSK343. GSK503 is 200 fold selective over EZH11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE(Kiapp=636 nM) and 4000 fo

4、ld selective over other histone methyltransferases 1.体内研究 In a melanoma mouse model, conditional EZH2 ablation as much as treatment with the GSK503 stabilizesthe disease through inhibition of growth and virtually abolishes metastases formation without affecting normalmelanocyte biology 2. GSK503 dis

5、plays favorable pharmacokinetics in mice. GSK503, but not vehicle,prevents the formation of germinal center after SRBC or NP-KLH immunization, phenocopying the Ezh2 nullphenotype. GSK503 treatment leads to reduced numbers of GC B-cells by flow cytometry, reduces numberand volume of GCs by immunohist

6、ochemistry, and impairs formation high affinity antibodies 1.PROTOCOLAnimal Mice: To pharmacologically inhibit Ezh2 activity, Tyr:N-RasQ61K Ink4a-/- and C57Bl/6 mice are subjected toAdministration 2 treatment with GSK503, which is diluted (15 mg/mL) in 20% Captisol solution. Efficient Ezh2 inhibitio

7、n isachieved by daily intraperitoneal injections of 150 mg/kg GSK503 over 35 consecutive days. Mice aremonitored during and after treatment to measure GSK503-induced reversible weight loss. C57Bl/6 andFoxn1nu/nu mice engrafted with melanoma cells are subjected to TM and GSK503 treatment as described

8、above 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. Patent. US20180263995A1. Oncotarget. 2017 Apr 25;8(35):58654-58667.See more customer validations on HYPERLINK / www.MedChemEREFER

9、ENCES1. Bguelin W, et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation.Cancer Cell. 2013 May 13;23(5):677-92.2. Zingg D, et al. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumoursuppressors. Nat Commun. 2015 Jan 22;6:6051.McePdfHeightCaution: Product has not been fully validated for med