H2-Gamendazole

SKU: orb1745148

Description

H2-Gamendazole is a novel small molecule Hsp90 regulator and inhibitor of heat shock proteins and elongation factor 1 alpha. It is a research compound investigated for its dual applications in male contraception via spermatogenesis inhibition and in cancer therapy, as evidenced by in vitro and in vivo studies.

Research Area

Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 877768-84-8
• MW: 417.21
• Purity: 97.39% (May vary between batches)
• Formula: C₁₈H₁₃Cl₂F₃N₂O₂
• SMILES: C(N1C=2C(C(CCC(O)=O)=N1)=CC=C(C(F)(F)F)C2)C3=C(Cl)C=C(Cl)C=C3
• Target: Others,CFTR,HSP
• Solubility: DMSO:30 mg/mL (71.91 mM)

Bioactivity

• Target IC50:
  ErbB2:50 μM|MCF-7 cells:∼100 μM|ADPKD cells:5–10 μM
• In Vivo:
  H2-Gamendazole (20 mg/kg ; intraperitoneal injections) was effective in slowing postnatal cyst formation and kidney enlargement in the ---Pkd1flox/flox: Pkhd1-Cre mouse model.
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• In Vitro:
  H2-Gamendazole (H2-GMZ ; 0-100 μM) was effective in rapidly blocking forskolin-induced, Cl-mediated short-circuit currents in human ADPKD cells, and it significantly inhibited both cAMP- and epidermal growth factor-induced proliferation of ADPKD cells. H2-GMZ (50 μM)-treated ADPKD cells showed decreased phosphorylated ERK and decreased hyperphosphorylated retinoblastoma levels through western blot analysis. H2-GMZ (50 μM ; 24、48、72 h) treatment also decreased ErbB2, Akt, and cyclin-dependent kinase 4 and it decreased levels of the cystic fibrosis transmembrane conductance regulator Cl channel protein.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HSP90

Compound Identifiers

PubChem CID

44176633