848952-37-4
Chemical Structure
G3130
- CAS No.: 848952-37-4
- Formula:C14H14N4O2
- Molecular Weight:270.29
IUPAC Name: 4-(4-(1H-imidazol-5-yl)-1H-pyrazol-3-yl)-6-ethylbenzene-1,3-diol
InChIKey: ATORUNMAUREKMH-UHFFFAOYSA-N
SMILES: OC=1C=C(O)C(=CC1C2=NNC=C2C3=CN=CN3)CC
Biological Activity: 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[1][2].
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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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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.
