Home Cytoskeletal Signaling HSP (HSP90) inhibitor - Autophagy inhibitor VER155008

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

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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=>
Click to View More Cell Line Experimental Data
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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