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H2-Gamendazole

Catalog No. T72076 CAS 877768-84-8

H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and/or elongation factor 1 alpha, and is an Hsp90 regulator.

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H2-Gamendazole, CAS 877768-84-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 119.00
5 mg	In stock	$ 333.00
10 mg	In stock	$ 498.00
25 mg	In stock	$ 885.00
50 mg	In stock	$ 1,190.00
100 mg	In stock	$ 1,630.00
1 mL * 10 mM (in DMSO)	In stock	$ 376.00

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Purity: 97.36%

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Description	H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and/or elongation factor 1 alpha, and is an Hsp90 regulator.
Targets&IC50	MCF-7 cells:∼100 μM, ADPKD cells:5–10 μM, ErbB2:50 μM
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.[1] H2-GMZ (50 μM)-treated ADPKD cells showed decreased phosphorylated ERK and decreased hyperphosphorylated retinoblastoma levels through western blot analysis.[1] 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.[1]
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.[1]

Molecular Weight	417.21
Formula	C18H13Cl2F3N2O2
CAS No.	877768-84-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (71.91 mM)

References and Literature

1. Sundar SV, et al. The lonidamine derivative H2-gamendazole reduces cyst formation in polycystic kidney disease. Am J Physiol Renal Physiol. 2022 ; 323(4):F492-F506. 2. Hau RK, et al. Physiological Characterization of the Transporter-Mediated Uptake of the Reversible Male Contraceptive H2-Gamendazole Across the Blood-Testis Barrier. J Pharmacol Exp Ther. 2022 ; 382(3):299-312. 3. Matts RL, et al. A systematic protocol for the characterization of Hsp90 modulators. Bioorg Med Chem. 2011 ; 19(1):684-692.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Exosome Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

H2-Gamendazole 877768-84-8 Cytoskeletal Signaling Metabolism HSP inhibitor inhibit

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