Home Cytoskeletal Signaling HSP inhibitor VER-50589

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VER-50589 HSP inhibitor

Cat.No.S7459

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

Chemical Structure

Molecular Weight: 388.80

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (198.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 388.80 Formula

C19H17ClN2O5

 Storage (From the date of receipt)
CAS No. 747413-08-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCNC(=O)C1=NOC(=C1C2=CC=C(C=C2)OC)C3=CC(=C(C=C3O)O)Cl

Mechanism of Action

Targets/IC50/Ki
HSP90β
21 nM
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. This compound 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.
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.
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.
References

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