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.

Size Price Stock Quantity  
USD 107 In stock
USD 407 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • 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.

    (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.

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

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 NVjBVFNkS3m2b4TvfIlkyqCjc4PhfS=> NELwd25EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUWg{txO Ml32NVkzPTZ3MEi=
human BT474 cells Mo\tSpVv[3Srb36gZZN{[Xl? NF74ZlNDcW6maX7nJIFn\mmwaYT5JJRwKEi|cEewJI52[2ynb4Tp[IUh[mmwZHnu[{Bld22jaX6gbY4hcHWvYX6gRnQ1PzRiY3XscJMtKEmFNUC9NVAvPCEQvF2= MVuyNFYxQDd|OB?=
human HCT116 cells Ml\jSpVv[3Srb36gZZN{[Xl? NVrQ[4VnOjRiaB?= MXXJcohq[mm2aX;uJI9nKEiVUEewJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhWmGoMTDwdo91\WmwIHzleoVteyCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2 M3nxU|E6OjV4NUC4

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
Synonyms C07

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HSP (e.g. HSP90) Signaling Pathway Map

Related HSP (e.g. HSP90) Products

Tags: buy VER155008 | VER155008 supplier | purchase VER155008 | VER155008 cost | VER155008 manufacturer | order VER155008 | VER155008 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID