Corin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECorinCat. No.: HY-111048CAS No.: 1808113-09-8分式: CHNO分量: 428.53作靶点: Histone Demethylase; HDAC作通路: Epigenetics; Cell Cycle/DNA Damage储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen

2、)溶解性数据体外实验 DMSO : 100 mg/mL (233.36 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (3.90 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.67 mg/mL (3.90 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Co

3、rin组氨酸赖氨酸特异性去甲 化酶 (LSD1) 和组氨酸脱酰化酶 (HDAC) 的双重 抑制剂，其对 LSD1 的Ki(inact) 值为 110 nM，对 HDAC1 的 IC50 值为 147 nM。IC50 & Target IC50: 147 nM (HDAC1), Ki(inact): 110 nM (LSD1) 1.体外研究 Corin is able to inhibit the deacetylation of semisynthetic, reconstituted nucleosomes by the CoREST ternarycomplex. Corin shows

4、irreversible inhibition of HDAC1 activity. In Comparison to MS-275, corin appears tomore potently (Corin EC50 95 nM vs. MS-275 EC50 420 nM) and efficaciously induce cellular H3K9acetylation. Interestingly, Corin (1 M) is non-toxic to primary human melanocytes in contrast to MS-275 (1 M) 1.REFERENCES1. Kalin JH, et al. Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nat Commun. 2018 Jan4;9(1):53.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;/p>