VER155008

Catalog No.S7751 Synonyms: C07

For research use only.

VER155008 (C07) 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.

VER155008 Chemical Structure

CAS No. 1134156-31-2

Selleck's VER155008 has been cited by 32 publications

Purity & Quality Control

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Biological Activity

Description VER155008 (C07) 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Targets
HSP70 [1]
(Cell-free assay)
HSC70 [1]
(Cell-free assay)
GRP78 [1]
(Cell-free assay)
0.5 μM 2.6 μM 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21 DE3 NI\YUopHfW6ldHnvckBie3OjeR?= NWn4S49wOTBibXnudy=> NEDEbo1KdmirYnn0bY9vKG:oIFfSVFc5KCh{NjD0c{A3OzZicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgRmwzOSCGRUOgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiMUCgcYlveyCkZX\vdoUhTkmWQz3OVmxNVFSJIH\seY9z\XOlZX70JJBmeHSrZHWgZYRlcXSrb36gbY4heHKnc3XuZ4Uhd2ZiMUCgeW0hSUSSIH\vcIxwf2WmIHL5JIZ2enSqZYKgbY5kfWKjdHnvckBnd3JiMjDodpMh[nliZnz1c5Jme2NuIFnDOVA:OC56zszN NEm0VGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUGyPVA2PCd-M{GxNlkxPTR:L3G+
HCT116 Mnm5R5l1d3SxeHnjbZR6KGG|c3H5 NIjsS2REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUZOwG0> M{jXeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkW2OVA5Lz5zOUK1OlUxQDxxYU6=
HCT116 MkDhRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXO0OYlHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEeLNUC9Oe69VQ>? NVn3U4dvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1NlY4PjNpPkKxOVI3PzZ|PD;hQi=>
BT474 M{DaO2Z2dmO2aX;uJIF{e2G7 NI\EfYtDcW6maX7nJIFn\mmwaYT5JJRwKEi|cEewJI52[2ynb4Tp[IUh[mmwZHnu[{Bld22jaX6gbY4hcHWvYX6gRnQ1PzRiY3XscJMtKEmFNUC9NVAvPM7:TR?= M2TZW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkC4O|M5Lz5{ME[wPFc{QDxxYU6=
HCT116 NUPvXFhkTnWwY4Tpc44h[XO|YYm= NHnUNHAzPCCqcoO= Mn7VTY5pcWKrdHnvckBw\iCKU2C3NEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEinMjDwdo91\WmwIHzleoVteyCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2 Mk\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NU[1NFgoRjF7MkW2OVA5RC:jPh?=
HCT116 MWXGeY5kfGmxbjDhd5NigQ>? M2j3[FI1KGi{cx?= M2\1TWlvcGmkaYTpc44hd2ZiSGPQO|AhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCUYX[xJJBzd3SnaX6gcIV3\Wy|IHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4S= NYT0U|VERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOVY2ODhpPkG5NlU3PTB6PD;hQi=>
Assay
Methods Test Index PMID
Western blot Hsp70 / AR 28691182
Immunofluorescence Blimp-1 28842558
Growth inhibition assay Cell viability 28053100
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]

Protocol (from reference)

Kinase Assay:[1] [5]
  • Hsc70, Hsp70 and Grp78 fluorescence 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 modifications. 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:[1]
  • Cell lines: BT474, MB-468, HCT116, and HT29 cells
  • Concentrations: 50 μM
  • Incubation Time: 72 h
  • Method: 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.
Animal Research:[1]
  • Animal Models: HCT116 tumor bearing
  • Dosages: 40 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 556.4
Formula

C25H23Cl2N7O4

CAS No. 1134156-31-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC=C1COCC2C(C(C(O2)N3C4=NC=NC(=C4N=C3NCC5=CC(=C(C=C5)Cl)Cl)N)O)O)C#N

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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