Home Cytoskeletal Signaling HSP (HSP90) inhibitor VER-50589 For research use only.

VER-50589

VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.

VER-50589 Chemical Structure

VER-50589 Chemical Structure

CAS No. 747413-08-7

Purity & Quality Control

Batch: S745901 DMSO]77 mg/mL]false]Ethanol]77 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

VER-50589 Related Products

Signaling Pathway

HSP (HSP90) Signaling Pathways

HSP (HSP90) Signaling Pathway

Biological Activity

Description VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Targets
HSP90β [1]
21 nM
In vitro
In vitro VER-50589 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 143 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-50589 causes induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5, which further result in cell cycle arrest and apoptosis. [1]
Kinase Assay Fluorescence Polarization Assay
Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.
Cell Research Cell lines Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT
Concentrations ~10 μM
Incubation Time 4 days
Method Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method.
In Vivo
In vivo In HCT116 human colon cancer xenografts, VER-50589 (100 mg/kg i.p.) results in a statistically significant reduction of ∼30% in tumor volume and weight, as well as induction of HSP72 and depletion of ERBB2 and C-RAF. [1]
Animal Research Animal Models HCT116 human colon cancer xenografts
Dosages ~100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 388.80 Formula

C19H17ClN2O5
CAS No. 747413-08-7 SDF Download VER-50589 SDF
Smiles CCNC(=O)C1=NOC(=C1C2=CC=C(C=C2)OC)C3=CC(=C(C=C3O)O)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (198.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 77 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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