HSP70-IN-1 - HSP 抑制劑 - 生命科學(xué)試劑 - 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作靶點(diǎn): HSP作通路: Cell Cycle/DNA Damage; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (10

2、7.62 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使

3、；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.38 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.38 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg

4、/mL (5.38 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 HSP70-IN-1種熱休克蛋 (HSP) 抑制劑; 抑制Kasumi-1細(xì)胞的長(zhǎng)的IC50值為2.3 M。IC50 & Target HSP70 Caspase-3/71.9 M (IC50, MOLM13 cells)體外研究 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