Gamendazole

Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research[1][2].

Product Specifications

CAS Number

[877773-32-5]

UNSPSC

12352005

Target

Akt; EGFR; HSP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; JAK/STAT Signaling; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/gamendazole.html

Purity

99.44

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(/C=C/C1=NN(C2=C1C=CC(C(F)(F)F)=C2)CC3=CC=C(C=C3Cl)Cl)O

Molecular Formula

C18H11Cl2F3N2O2

Molecular Weight

415.19

References & Citations

[1]Joseph S Tash, et al. Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates Il1a transcription in rat Sertoli cells. Biol Reprod. 2008 Jun;78 (6) :1139-52.|[2]Joseph S. Tash. Gamendazole: A Potent Antispermatogenic Contraceptive Agent with Novel Targets Hsp90β and eEF1A. Biology of ReproductionIF, Volume 78, Issue Suppl_1, 1 May 2008, Page 91.