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Radicicol CAS 12772-57-5 Antibiotic HSP90 inhibitor molecular chaperone essent

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产品名称: Radicicol CAS 12772-57-5 Antibiotic HSP90 inhibitor molecular chaperone essent
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简单介绍

CAS:12772-57-5Formula:C18H17ClO6MW:364.78Appearance:WhitepowderPurity:100%(HPLC)


Radicicol CAS 12772-57-5 Antibiotic HSP90 inhibitor molecular chaperone essent  的详细介绍

Radicicol is a macrocyclic antifungal antibiotic that inhibits protein tyrosine kinase. Isolated from Monocillium nordinii, it binds to and inhibits Hsp90 at very low concentrations (20nM). Heat shock Protein 90(Hsp90), is a molecular chaperone that mediates the folding of  a number of oncogenic proteins, it is an attractive target for inhibiton by anticancer agents.

Radicicol binds to a highly conserved pocket in the Hsp90 protein and inhibits the intrinsic ATPase activity of Hsp90. Radicicol induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. It suppresses NIH 3T3 cell transformation by diverse oncogenes such as srcras and mos and also suppresses the expression of mitogen-inducible cyclooxygenase-2. As a cell differentiation modulator, radicicol has anti-angiogenic activity in vivo, inhibiting the proliferation of and plasminogen activator production by vascular endothelial cells.

 

Additional Information

SynonymsMonorden
Product #R-1130
CAS #12772-57-5
Chemical Name1aR,2Z,4E,14R,15aR)-8-Chloro-9,11-dihydroxy-14-methyl-1a,14,15,15a-tetrahydro-6H-oxireno[e][2]benzoxacyclotetradecine-6,12(7H)-dione
FormulaC18H17ClO6
MW364.78
AppearanceWhite powder
Purity100% (HPLC)
SolubilityClear colorless solution at 20mg/ml DMSO and 10mg/ml methanol.
Melting Point198‚°C
PreparationPacked under inert gas.
Storage Temp-20°C . Store under desiccating conditions. The product can be stored for up to 12 months.
UseRadicol is used for the treatment of inflammation and endotoxemia. it does this by inhibiting Hsp 90 function by binding in its L-shaped confirmation to its N-terminal ATP pocket. this was found to be done at the ATp of yeast HSP 90.Treatment of Leukemia and Lymphoma. Inhibits intestinal inflammation and leakage in abdominal sepsis.

Additional Information

SMILESCC1CC2C(O2)C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1
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