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VER-155008

🥰Excellent
Catalog No. T7010Cas No. 1134156-31-2
Alias VER155008

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.

VER-155008

VER-155008

🥰Excellent
Purity: 99.55%
Catalog No. T7010Alias VER155008Cas No. 1134156-31-2
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.
Pack SizePriceAvailabilityQuantity
2 mg$39In Stock
5 mg$63In Stock
10 mg$85In Stock
25 mg$166In Stock
50 mg$297In Stock
100 mg$492In Stock
200 mg$688In Stock
1 mL x 10 mM (in DMSO)$77In Stock
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Purity:99.55%
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Product Introduction

Bioactivity
Description
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.
Targets&IC50
GRP78:2.6 μM, HSP70:0.5 μM, HSC70:2.6 μM
In vitro
VER-155008 inhibits the proliferation of human breast and colon cancer cell lines BT474, MB-468, HCT116, and HT29 with GI50s in the range 5.3-14.4 μM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells.[1] In the 8505C and FRO cells, VER-155008 reduces the cell viability and elevates the percentage of dead cells in a time- and dose- dependent manner.[2] VER-155008 causes a dose-dependent inhibition of cytokine-dependent AML cell proliferation.[3] VER-155008?shows an effective inhibition of cell proliferation in A549 and H1975 cells. [4]
In vivo
In HCT116 tumor bearing mice, VER-155008 (25 or 40 mg/kg, i.v.) demonstrates rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level.[1]
Kinase Assay
Hsc70, Hsp70 and Grp78 ?uorescence polarisation (FP) assay: The FP assay for Hsp70 is conducted in aqueous buffer consisting of 100 mM Tris pH 7.4, 150 mM KCl and 5 mM CaCl2, in a final assay volume of 100 μl, using 96 well black polystyrene high bind plates with a Fusion plate reader. N6-(6-amino)hexyl-ATP-5-FAM and the in-house protein preparation of GST-HSP70 3-382 have final concentrations in the assay of 20 nM and 400 nM, respectively. Compounds are tested as 10-point IC50s, with a final DMSO concentration of 5%. Assay mixtures are incubated for 3 h prior to reading on the Fusion (ex 485 nm; em 535 nm). The data is fitted using a 4 parameter logistical data model by XLFit 4. The FP assay for Hsc70 and Grp78 is carried out as described for Hsp70 using the same N6 -(6-amino)hexyl-ATP-5-FAM as the FP probe with the following modi?cations. For Hsc70, the protein and probe concentrations are 0.3 μM and 20 nM, respectively with a 30 min incubation at 22℃ while for Grp78, the protein and probe concentrations are 2 μM and 10 nM, respectively with a 2 h incubation at 22℃. The KD for the FAM-ATP probe was 0.24 μM for Hsc70 and 2 μM for Grp78.
Cell Research
All cell lines are grown in DMEM/10% FCS with GlutaMAX-I in a humidified atmosphere of 5% CO2 in air. Cell proliferation is determined using the sulforhodamine B (SRB) assay.(Only for Reference)
AliasVER155008
Chemical Properties
Molecular Weight556.4
FormulaC25H23Cl2N7O4
Cas No.1134156-31-2
SmilesNc1ncnc2n([C@@H]3O[C@H](COCc4ccc(cc4)C#N)[C@@H](O)[C@H]3O)c(NCc3ccc(Cl)c(Cl)c3)nc12
Relative Density.1.63 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: <1 mg/mL (Insoluble)
DMSO: 55.6 mg/mL (100 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7973 mL8.9863 mL17.9727 mL89.8634 mL
5 mM0.3595 mL1.7973 mL3.5945 mL17.9727 mL
10 mM0.1797 mL0.8986 mL1.7973 mL8.9863 mL
20 mM0.0899 mL0.4493 mL0.8986 mL4.4932 mL
50 mM0.0359 mL0.1797 mL0.3595 mL1.7973 mL
100 mM0.0180 mL0.0899 mL0.1797 mL0.8986 mL

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