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CAS No.: 1134156-31-2

VER-155008 Catalog No. CSN13116

Synonyms: C07

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, > 100-fold selectivity over HSP90.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HSP70

IC50:0.5μM HSPA8

IC50:2.6μM GRP78

IC50:2.6μM
描述HSC70 and HSP70 are the two major cytosolic isoforms of the HSP70 family. Between this two proteins, HSP70 is present at relatively low levels in normal cells but can be elevated in expression to protect cells from apoptosis in response to various stressful stimuli such as anticancer agents, especially the HSP90 inhibitors, making it become an important target for anticancer therapy due to its antiapoptotic and oncogenic functions. VER-155008 is a potent inhibitor for Hsp70, Hsc70 and Grp78 with IC50 values of 0.5μM, 2.6 μM and 2.6μM (measured by fluorescence polarisation (FP) assay), respectively. In celluar study, exposure to VER-155008 at 40μM showed a similar response like treatment with HSP90 inhibitor 17-AAG in BT474 or HCT116 cells, like induction of the degradation of HSP90 client protein Her2 and Raf-1, except no induction of HSP70 protein observed. Apoptosis to different extent can be observed in BT474, MDA-MB-468, HCT116 or HT29 cells exposure to VER-155008 at concentration of 0.5μM or 20μM for 24h. Complete colony forming ability of HCT116 or HT29 cells following a 48h-exposure to VER-155008 at concentration>40μM. Combined treatment with VER-155008 at varying concentration to HSP90 inhibitors, 0.5μM VER-82160 or 0.5μM 17-AAG for 24h, could dose-dependently elevate the potency of this two HSP90 to induce cell apoptosis. These suggest that the best use of a small molecule Hsc70/Hsp70 inhibitor, VER-155008, will be in combination with an Hsp90 inhibitor^[1].
作用机制VER-155008 and bind in the ATPase pocket of Hsp70 and inhibit its intrinsic ATPase activity.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human BT474 cells	-	Function assay	-	Binding affinity to Hsp70 nucleotide binding domain in human BT474 cells, IC50=10.4 μM	20608738
human HCT116 cells	-	Cytotoxic assay	-	Cytotoxicity against human HCT116 cells by SRB assay, GI50=5 μM	19256508
human HCT116 cells	-	Function assay	24 h	Inhibition of HSP70 in human HCT116 cells assessed as reduction of Raf1 protein levels after 24 hrs by Western blot	19256508

动物研究
剂量
Mice^[1] (i.v.): 25 mg/kg, 40 mg/kg

给药途径
i.v.

动物药代数据
Animal Mice^[1]
Dose 25 mg/kg
Administration i.v.
T_1/2 0.6 h
CL 49 ml/min/kg
参考文献

[1] Massey AJ, Williamson DS, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7973 mL
- 8.9863 mL
- 17.9727 mL
- 5 mM
- 0.3595 mL
- 1.7973 mL
- 3.5945 mL
- 10 mM
- 0.1797 mL
- 0.8986 mL
- 1.7973 mL

技术信息

CAS号

1134156-31-2

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H23Cl2N7O4

运输

蓝冰

分子量

556.40

别名

C07

溶解度

DMSO	105.0 mg/mL (188.7 mM)
Water	insoluble

动物实验配方

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靶点	Description	IC50
HSP70		IC50:0.5μM
HSPA8		IC50:2.6μM
GRP78		IC50:2.6μM

VER-155008 Catalog No. CSN13116

靶点选择性

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