Antibodies
VER 155008
- 貨號 Cat. No.
- S7150
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
VER 155008
Catalog No.S7150
VER-155008 is a potent inhibitor of the HSP70 family, with IC50 of 0.5 μM and 2.6 μM for HSP70 and Grp78, respectively, exhibits >100-fold selectivity over HSP90.
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Biological Activity
| Description | VER-155008 is a potent inhibitor of the HSP70 family, with IC50 of 0.5 μM and 2.6 μM for HSP70 and Grp78, respectively, exhibits >100-fold selectivity over HSP90. | |||||
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| Targets | HSP70 | Grp78 | ||||
| IC50 | 0.5 μM [1] | 2.6 μM [1] | ||||
| In vitro | VVER-155008 is a potent inhibitor of the HSP70 family of chaperones, with IC50 of 0.5 μM and 2.6 μM for HSP70 and Grp78, respectively, exhibits >100-fold selectivity over HSP90. VER-155008 inhibits the proliferation of human breast and colon cancer cell lines with GI50s in the range 5.3–14.4 μM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells. As a single agent, VER-155008 induces caspase-3/7 dependent apoptosis in BT474 cells and non-caspase dependent cell death in HCT116 cells. [1] VER-155008 binds at Grp78 with KD of 80 nM. [2] | |||||
| In vivo | VER- 155008 demonstrats rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Fluorescence polarisation (FP) assay | Hsc70 (aa 5-381) and Grp78 (ATPase domain) are cloned and expressed as follows. A PCR fragment of Hsc70 corresponding |
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Cell Assay: [1]
| Cell lines | HCT116 |
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| Concentrations | ~40 μM |
| Incubation Time | 24 h |
| Method | Cell cycle analysis. HCT116 cells are exposed to the indicated concentrations of VER-155008 for 24 h. All cells are |
Animal Study: [1]
| Animal Models | BALB/c nu/nu mouse |
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| Dosages | 25 mg/kg |
| Administration | i.v. |
References
Chemical Information
| Molecular Weight (MW) | 556.4 |
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| Formula | C25H23Cl2N7O4 |
| CAS No. | 1134156-31-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
|---|---|---|---|
| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Adenosine, 5’-O-[(4-cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]- |
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