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Cat. No.: HY-111300

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G3130

G3130 is a reversible HSP90 inhibitor with a K_d 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
화학식: C₁₄H₁₄N₄O₂
분자량:270.29

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

G3130 Chemical Structure

CAS No.: 848952-37-4

Amount: USD 0.00

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One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
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Biological Activity

제품 설명

IC₅₀ & Target

^[1]^[2]

HSP90α

280 nM (Kd, N-terminal ATP-binding domain of purified human Hsp90α)

HER2

All HSP Isoforms :

All EGFR Isoforms :

In Vitro

G3130 (49 nM-25 μM) binds reversibly to the purified N-terminal ATP-binding domain of human Hsp90α, with a K_d 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

CAS No. 848952-37-4
분자량 270.29
화학식 C₁₄H₁₄N₄O₂
SMILES

OC=1C=C(O)C(=CC1C2=NNC=C2C3=CN=CN3)CC
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Kreusch A, et al. Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles. Bioorganic & medicinal chemistry letters. 2005 Mar 01;15(5):1475-8.

[2]. Blagg BS, et al. Hsp90 inhibitors: small molecules that transform the Hsp90 protein folding machinery into a catalyst for protein degradation. Medicinal research reviews. 2006 May;26(3):310-38.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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Species:
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수량:

G3130

All HSP Isoforms

All EGFR Isoforms

Biological Activity

제품 설명

IC50 & Target

In Vitro

Chemical Information

순도&문서

References

Calculators

Help & FAQs

G3130 Related Classifications

HY-111300 Related Classifications

Bioz

Keywords

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