Radicicol – ATP-competitive inhibitor of Hsp90 that bi...

For Research Use Only. Not for human or veterinary use.

Radicicol Product ID: BLK-0500
Structure
CAS	12772-57-5
Molecular Formula	C18H17ClO6
Molecular Weight	364.78
UN (Transport)	UN2811
Price	1mg: USD 36.00 / 5mg: - / 25mg: -
Storage	-20°C
Solubility	1mg/ml ethanol, methanol, DMSO
Synonyms	Monorden
Purity	>95%
Source Organism	Pochonia sp.
Summary	Radicicol Resorcylic acid lactone that inhibits Hsp90.
Details	Radicicol is a fungal secondary metabolite originally identified as an antibiotic and later established as a potent ATP competitive inhibitor of heat shock protein 90 Hsp90. It binds to the N terminal ATP binding pocket of Hsp90 and blocks its chaperone cycle, leading to destabilization and degradation of oncogenic client proteins including Raf 1, HER2, and mutant p53. Structural and biochemical studies confirmed its occupation of the nucleotide binding site and its role in suppressing oncogenic signaling.
Mechanism	ATP-competitive inhibitor of Hsp90 that binds the N-terminal nucleotide pocket, blocking chaperone function.
Primary Target	Hsp90
Pathway	Protein folding pathway; Oncogenic signaling
Chemical Class	Resorcylic acid lactone (RAL)
Discovery Year	1953
Keywords	hsp90 inhibitorresorcylic acid lactoneatp-competitive inhibitoroncogenic client protein degradation inducerfungal macrolidechemical biology probe
References	Delmotte et al., Nature, 1953 DOI: 10.1038/171344a0 Schulte et al., J Biol Chem, 1998 DOI: 10.1074/jbc.273.25.15564 Soga et al., Cancer Res, 1998 DOI: 10.1158/0008-5472.CAN-98-0588 Roe et al., J Med Chem, 1999 DOI: 10.1021/jm990095i Chiosis et al., Mol Cancer Ther, 2001 DOI: 10.1158/1535-7163.MCT-01-0004
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