877773-32-5
Chemical Structure
Gamendazole
- CAS No.: 877773-32-5
- Formula:C18H11Cl2F3N2O2
- Molecular Weight:415.19
IUPAC Name: (E)-3-(1-(2,4-dichlorobenzyl)-6-(trifluoromethyl)-1H-indazol-3-yl)acrylic acid
InChIKey: KYYQMVUKYQCSQY-AATRIKPKSA-N
SMILES: O=C(/C=C/C1=NN(C2=C1C=CC(C(F)(F)F)=C2)CC3=CC=C(C=C3Cl)Cl)O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Gamendazole | 99.44% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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.
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