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

For research use only. We do not sell to patients.

Gamendazole Chemical Structure

Gamendazole Chemical Structure

CAS No. : 877773-32-5

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Based on 1 publication(s) in Google Scholar

Gamendazole Related Antibodies

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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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Description

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

 

Molecular Weight

415.19

Formula

C18H11Cl2F3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (120.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4085 mL 12.0427 mL 24.0854 mL
5 mM 0.4817 mL 2.4085 mL 4.8171 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4085 mL 12.0427 mL 24.0854 mL 60.2134 mL
5 mM 0.4817 mL 2.4085 mL 4.8171 mL 12.0427 mL
10 mM 0.2409 mL 1.2043 mL 2.4085 mL 6.0213 mL
15 mM 0.1606 mL 0.8028 mL 1.6057 mL 4.0142 mL
20 mM 0.1204 mL 0.6021 mL 1.2043 mL 3.0107 mL
25 mM 0.0963 mL 0.4817 mL 0.9634 mL 2.4085 mL
30 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0071 mL
40 mM 0.0602 mL 0.3011 mL 0.6021 mL 1.5053 mL
50 mM 0.0482 mL 0.2409 mL 0.4817 mL 1.2043 mL
60 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0036 mL
80 mM 0.0301 mL 0.1505 mL 0.3011 mL 0.7527 mL
100 mM 0.0241 mL 0.1204 mL 0.2409 mL 0.6021 mL
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Gamendazole Related Classifications

Help & FAQs
  • 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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