VER155008

Catalog No.S7751 Synonyms: C07

VER155008 Chemical Structure

Molecular Weight(MW): 556.4

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.

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Cited by 9 Publications

3 Customer Reviews

  • (D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM).

    Neuroscience, 2014, 281C:164-177.. VER155008 purchased from Selleck.

    RD cells were pre-treated with Ver-155008 for 2 hours at indicated concentration following an infection of EV-A71 at MOI of 10 for 9 hours. Proteins levels of VP0/2 by western blot.

    Antiviral Res, 2018, 150:39-46. VER155008 purchased from Selleck.

  • C, HSP70 protein levels after 1000 ng/mL LPS treatment combined with or without HSP70 inhibitor VER155008 for 48 h using western blot analysis, respectively. D, HSP70 protein levels after heat stress treatment combined with or without HSP70 inhibitor VER155008 for 3 h using western blot analysis.

    Cell Signal, 2017, 30:130-141. VER155008 purchased from Selleck.

Purity & Quality Control

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Biological Activity

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
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
human HCT116 cells MnLPR5l1d3SxeHnjxsBie3OjeR?= MoTVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13IN88US=> MoDhNVkzPTZ3MEi=
human BT474 cells M{nGUmZ2dmO2aX;uJIF{e2G7 MYTCbY5lcW6pIHHm[olvcXS7IITvJGh{eDdyIH71Z4xmd3SrZHWgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iQmS0O|Qh[2WubIOsJGlEPTB;MUCuOEDPxE1? NGftbo8zODZyOEezPC=>
human HCT116 cells MlroSpVv[3Srb36gZZN{[Xl? MXqyOEBp MXTJcohq[mm2aX;uJI9nKEiVUEewJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhWmGoMTDwdo91\WmwIHzleoVteyCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2 M2HP[lE6OjV4NUC4

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Hsp70 / AR; 

PubMed: 28691182     


LNCaP95 cells were treated with VER155008 (25 μM) for the indicated times. Protein extracts (15 μg) were subjected to Western blotting.

28691182
Immunofluorescence
Blimp-1; 

PubMed: 28842558     


SUDHL-2 cells or RJ-Lym1 cells were treated with MG132 (1 μM) or VER155008 (30 μM) for 24 h, stained with a Blimp-1 antibody (red) and DAPI (blue), and then observed under a confocal microscope. Scale bar: 5 μm.

28842558
Growth inhibition assay
Cell viability; 

PubMed: 28053100     


Vero cells were treated with the indicated concentrations of VER155008 for 96 h, and then cell viability was determined and calculated as a percentage of the viability of cells treated with DMSO. 

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

Kinase Assay:[1] [5]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: HCT116 tumor bearing
  • Formulation: 10% DMSO/5% Tween 80/85% Saline (v/v/v)
  • Dosages: 40 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (179.72 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 556.4
Formula

C25H23Cl2N7O4
CAS No. 1134156-31-2
Storage powder
in solvent
Synonyms C07

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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.

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HSP (e.g. HSP90) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID