Radicicol | HSP90 inhibitor

CAS:
12772-57-5
Catalog Number:
10-2102
Activity:
HSP90 inhibitor
Chemical Name:
(1aR,2Z,4E,14R,15aR)-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
Alternate Names:
Monorden
Molecular Weight:
364.78
Molecular Formula:
C18H17ClO6
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 8 mg/ml).
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

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1 mg$50.00
5 mg$200.00

Radicicol (12772-57-5) inhibits heat shock protein 90 (HSP90) activity by binding to the ATP-binding pocket.1 In cells HSP90 client proteins such as Raf kinase2, HIF-1α3 and estrogen receptor4 are destabilized and proteolytically degraded. Radicicol inhibits expression of COX-2 without affecting COX-1 expression in LPS-stimulated macrophages (IC50=27 nM).5 Inhibits angiogenesis.6

References/Citations:

1) Schulte et al. (1999), Interaction of radicicol with members of the heat shock protein 90 family of molecular chaperones; Mol. Endocrinol., 13 1435
2) Soga et al. (1998), Radicicol leads to selective depletion of Raf kinase and disrupts K-Ras-activated aberrant signaling pathway; J. Biol. Chem., 273 822
3) Hur et al. (2002) Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1alpha/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heat-shock protein inhibitor radicicol; Mol. Pharmacol., 62 975
4) Lee et al. (2002) Radicicol represses the transcriptional function of the estrogen receptor by suppressing the stabilization of the receptor by heat shock protein 90; Mol. Cell. Endocrinol., 188 47
5) Chanmugam et al. (1995) Radicicol, a protein tyrosine kinase inhibitor, suppresses the expression of mitogen-inducible cyclooxygenase in macrophages stimulated with lipopolysaccharide and in experimental glomerulonephritis; J. Biol. Chem., 270 5418
6) Oikawa et al. (1993) Radicicol, a microbial cell differentiation modulator, inhibits in vivo angiogenesis; Eur. J. Pharmacol., 241 221

CAS:
12772-57-5
Catalog Number:
10-2102
Activity:
HSP90 inhibitor
Chemical Name:
(1aR,2Z,4E,14R,15aR)-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
Alternate Names:
Monorden
Molecular Weight:
364.78
Molecular Formula:
C18H17ClO6
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 8 mg/ml).
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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