2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. HSP Akt EGFR
  4. Gamendazole

Gamendazole 是一种吲唑羧酸 (ICA)，一种具有口服活性的，选择性 HSP90AB1 (HSP90BETA) 和 EEF1A1 (eEF1A) 抑制剂。Gamendazole 与 HSP90 的 C 端核苷酸结合口袋结合，导致 AKT1 和 ERBB2 下调，但稳定 HSP90 异源复合物。Gamendazole 特异性抑制 EEF1A1 的肌动蛋白捆绑功能，但不与核苷酸对接口袋结合，也不抑制 EEF1A1 的核糖体充电或蛋白质翻译功能。Gamendazole 是一种可以抗精子发生的化合物，具有抗生育作用，有用于可逆性非激素男性避孕药研究的潜力。

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Gamendazole Chemical Structure

Gamendazole Chemical Structure

CAS No. : 877773-32-5

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Gamendazole 相关抗体

Top Publications Citing Use of Products

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Akt Akt1 Akt2 Akt3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

HSP90AB1

 

EEF1A1

 

Akt1

 

ErbB2

 

分子量

415.19

Formula

C18H11Cl2F3N2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Gamendazole 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gamendazole877773-32-5HSPAktEGFRHeat shock proteinsPKBProtein kinase BEpidermal growth factor receptorErbB-1HER1indazole carboxylic acidICAHSP90AB1EEF1A1AKT1ERBB2antispermatogenicantifertilitycontraceptive agentInhibitorinhibitorinhibit

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