HSP70-IN-1 - HSP 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHSP70-IN-1Cat. No.: HY-12622CAS No.: 1268273-90-0分式: CHNOS分量: 464.58作靶点: HSP作通路: Cell Cycle/DNA Damage; Metabolic Enzyme/Protease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 : 50 mg/mL (10

2、7.62 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1525 mL 10.7624 mL 21.5248 mL5 mM 0.4305 mL 2.1525 mL 4.3050 mL10 mM 0.2152 mL 1.0762 mL 2.1525 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使

3、；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.38 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.38 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg

4、/mL (5.38 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 HSP70-IN-1种热休克蛋 (HSP) 抑制剂; 抑制Kasumi-1细胞的长的IC50值为2.3 M。IC50 & Target HSP70 Caspase-3/71.9 M (IC50, MOLM13 cells)体外研究 The heat shock protein 70 (Hsp70) is a molecular chaperone which plays an important

5、 function in proteinhomeostasis as well as in cell signaling and survival. Hsp70 is frequently overexpressed in cancer, where theelevated expression is furthermore believed to be a cause of or to lead to resistance to chemotherapy andother treatments. HSP70-IN-1 interferes with the formation of func

6、tional Hsp70-HOP-Hsp90 machinery by itsability to dose-dependently alter the megacomplex components and to destabilize an Hsp70-Hsp90machinery client, Raf-1. In cells, the refolding of heat-denatured luciferase by endogenous as well astransfected Hsp70 is inhibited by HSP70-IN-1. HSP70-IN-1 also res

7、ults in induction of apoptosis in cancercells. Addition of HSP70-IN-1to cancer cells dose-dependently alters the formation of the Hsp70-HOPcomplex, a phenomenon associated with their destabilization and reduction in half-life 1.REFERENCES1. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5-

8、thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014 Feb 27;57(4):1208-24.McePdfHeightCaution: Product has not been fully validated for medical applications.For