G3130
G3130 is a reversible HSP90 inhibitor with a Kd value of 280 nM for the N-terminal ATP-binding domain of purified human Hsp90α. G3130 binds to the adenine site via a multi-hydrogen bond network. G3130 induces the degradation of Hsp90 client protein Her-2 in breast cancer cells. G3130 activates Hsp70 promoter-driven luciferase expression in 293T cells. G3130 can be used in breast cancer-related research.
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- CAS No.: 848952-37-4
- Formule: C14H14N4O2
- Masse moléculaire:270.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
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HSP90α 280 nM (Kd, N-terminal ATP-binding domain of purified human Hsp90α) |
HER2 |
In Vitro
G3130 (49 nM-25 μM) binds reversibly to the purified N-terminal ATP-binding domain of human Hsp90α, with a Kd value of 280 nM[1].
G3130 binds to the adenine-binding pocket of the purified human Hsp90α N-terminal ATP-binding domain via multiple direct hydrogen bonds and water-mediated hydrogen bonds, with its ethyl group occupying a hydrophobic subpocket[1].
G3130 (0.001-100 μM) activates the Hsp70 promoter in human embryonic kidney 293T cells in a concentration-dependent manner in vitro, confirming its Hsp90 inhibitory activity[1].
G3130 binds to the N-terminal domain of human Hsp90α, and its specific structural interactions match the regions targeted by radicicol and geldanamycin[2].
G3130 (3-100 μM) induces degradation of the Her-2 protein in SKBR-3 human breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 848952-37-4
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Masse moléculaire 270.29
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Formule C14H14N4O2
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SMILES
OC=1C=C(O)C(=CC1C2=NNC=C2C3=CN=CN3)CC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
G3130 Related Classifications
HY-111300 Related Classifications
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