Radicicol

SKU
R-1130
  • CAS:12772-57-5
  • Formula:C18H17ClO6
  • MW:364.78 Da
  • Appearance:White powder
  • Purity:≥99% (HPLC)

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Product Name Qty
Radicicol
1 mg
$75.48
Radicicol
5 mg
$280.50

Description

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.

 

Not for human therapeutic use or for medicinal purposes. For research applications only.

More Information
Alternate Name/Synonyms
Monorden; Radicolol; Radisicol
SKU
R-1130
CAS #
12772-57-5
Chemical Name
(4R,6R,8R,9Z,11E)-16-chloro-17,19-dihydroxy-4-methyl-3,7-dioxatricyclo[13.4.0.06,8]nonadeca-1(15),9,11,16,18-pentaene-2,13-dione
Chemical Formula
C18H17ClO6
Molecular Weight
364.78 Da
Appearance
White powder
Purity
≥99% (HPLC)
Solubility
20 mg/mL DMSO and 10 mg/mL methanol
Melting Point
198°C
Preparation
Packed under inert gas
Storage Temp
-20°C, desiccated
THERAPEUTIC AREA
Inflammatory Disorders
USE
Radicicol is used for the treatment of inflammation and endotoxemia. Inhibits Hsp90 by binding in its L-shaped confirmation to its N-terminal ATP pocket. This is done at the ATP binding site of yeast Hsp90. Treatment of leukemia and lymphoma. Inhibits intestinal inflammation and leakage in abdominal sepsis. Radicicol enhances regeneration of muscle by attenuating NF-kB activation and increasing myogenic differentiation.
PACKING GROUP
3
HAZARD CLASS
6.1
Handling
Use only in area provided with appropriate exhaust ventilation. Keep away from heat and source of ignition. Empty containers pose a fire risk, evaporate residue under fume hood. Ground all equipment containing material. Do not breathe dust.
Certificate of Analysis 1
Certificate of Analysis 2
Certificate of Analysis 3
GHS PICTOGRAMS
Handling Use only in area provided with appropriate exhaust ventilation. Keep away from heat and source of ignition. Empty containers pose a fire risk, evaporate residue under fume hood. Ground all equipment containing material. Do not breathe dust.
Packing Group 3
Citations Lysine deacetylases Hda1 and Rpd3 regulate Hsp90 function thereby governing fungal drug resistance
A novel probe to assess cytosolic entry of exogenous proteins
Nontoxic antimicrobials that evade drug resistance
Hsp90-mediated cytosolic refolding of exogenous proteins internalized by dendritic cells
Dosage compensation can buffer copy-number variation in wild yeast
Hsp90 orchestrates transcriptional regulation by Hsf1 and cell wall remodelling by MAPK signalling during thermal adaptation in a pathogenic yeast
Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding
Role of heat shock protein 90 and endothelial nitric oxide synthase during early anesthetic and ischemic preconditioning
Dual Roles for Yeast Sti1/Hop in Regulating the Hsp90 Chaperone Cycle
Cooperative regulation of the interferon regulatory factor-1 tumor suppressor protein by core components of the molecular chaperone machinery
Measurement of nanomolar dissociation constants by titration calorimetry and thermal shift assay - radicicol binding to Hsp90 and ethoxzolamide binding to CAII
ATP Acyl Phosphate Reactivity Reveals Native Conformations of Hsp90 Paralogs and Inhibitor Target Engagement
Heat shock protein-90 inhibitors enhance antigen expression on melanomas and increase T cell recognition of tumor cells
Hsp21 potentiates antifungal drug tolerance in Candida albicans
Thermodynamics of radicicol binding to human Hsp90 alpha and beta isoforms
Mutations that increase both Hsp90 ATPase activity in vitro and Hsp90 drug resistance in vivo
Synthesis-enabled understanding of the mechanism of action of amphotericin B and the development of increased therapeutic derivatives
Understanding Genome Structure and Response to Perturbation
Exploiting fitness trade-offs to prevent antifungal drug resistance
Targeting the adaptability of heterogeneous aneuploids
Mechanism of Long-Range Chromosome Motion Triggered by Gene Activation
The genetic basis of aneuploidy tolerance in wild yeast
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