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產品描述： VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70. |
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靶點：
HSP70:0.5 μM (IC50);HSC70:2.6 μM (IC50);Grp78:2.6 μM (IC50);GPR;?HSP;?Autophagy |
體內研究：
VER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice |
參考文獻：
1. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. 2. Yang X, et al. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimer's Disease. Front Pharmacol. 2018 Jan 30;9:48. 3. Kita K, et al. Heat shock protein 70 inhibitors suppress androgen receptor expression in LNCaP95 prostate cancer cells. Cancer Sci. 2017 Sep;108(9):1820-1827. |
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溶解性：
DMSO : ≥ 37 mg/mL (66.50 mM) |
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保存條件：
2-8℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
1.797 ml |
8.986 ml |
17.972 ml |
| 5 mM |
0.359 ml |
1.797 ml |
3.594 ml |
| 10 mM |
0.18 ml |
0.899 ml |
1.797 ml |
| 50 mM |
0.036 ml |
0.18 ml |
0.359 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京