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Radicicol R-1130

Humicola fuscoatra



Radicicol, a macrocyclic antifungal antibitotic, has been shown to bind to a highly conserved pocket in the Hsp90 (heat shock protein 90) chaperone protein and inhibit its function.

Because HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, and oncogenesis, Radicicol obstructs the proliferation of cultured cancer cells and shows anti-cancer activity in experimental animals.

Radicicol exerts this anti-tumor effect by inhibiting the intrinsic ATPase activity of HSP90, resulting in degradation of HSP90 client proteins via the ubiquitin-proteosome pathway.

Product No: R-1130
Chemical Formula: C18H17CIO6
M.W.: 364.78
CAS No: [12772-57-5]
Handling: Toxic, Hygroscopic
Storage: +4°C

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Literature References

  1. 1. Tago K, Tsukahara F, Naruse M, Yoshioka T, Takano K., Hsp90 inhibitors attenuate effect of dexamethasone on activated NF-kappaB and AP-1. Life Sci. 2004 Mar 5;74(16):1981-92.
  2. 2. Piper PW, Millson SH, Mollapour M, Panaretou B, Siligardi G, Pearl LH, Prodromou C. Sensitivity to Hsp90-targeting drugs can arise with mutation to the Hsp90 chaperone, cochaperones and plasma membrane ATP binding cassette transporters of yeast. Eur J Biochem. 2003 Dec;270(23):4689-95.
  3. 3. Yoshida M, Honda A, Horinouchi S., Morphological reversion of tumor cells by histone deacetylase inhibitors and radicicol, Gan To Kagaku Ryoho (Article in Japanese).1997. Sep; 24(11):1512.
  4. 4. Blagosklonny MV., Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs., Leukemia. 2002. Apr;16(4):455-62.
  5. 5. Maloney A, Workman P., HSP90 as a new therapeutic target for cancer therapy: The story unfolds., Expert Opin Biol Ther. 2002. Jan; 2(1):3-24.
  6. 6. Piper PW., The Hsp90 chaperone as a promising drug target., Curr Opin Investig Drugs. 2001. Nov; 2(11):1606-10.
  7. 7. Richter K, Buchner J., Hsp90: chaperoning Cancer Research., J Cell Physiol 2001 Sep; 188(3):281-90.
  8. 8. Hur E, Kim HH, Choi SM, Kim JH, Yim S, Kwon HJ, Choi Y, Kim DK, Lee MO, Park H., 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. 2002. Nov; 62(5):975-82.
  9. 9. Vogen S, Gidalevitz T, Biswas C, Simen BB, Stein E, Gulmen F, Argon Y., Radicicol-sensitive peptide binding to the N-terminal portion of GRP94. J Biol Chem. 2002. Oct 25; 277(43):40742-50.
  10. 10. Sano M., Radicicol and geldanamycin prevent neurotoxic effects of anti-cancer drugs on cultured embryonic sensory neurons. Neuropharmacology. 2001. Jun;40(7):947-53.
  11. 11. Besant PG, Lasker MV, Bui CD, Turck CW., Inhibition of branched-chain alpha-keto acid dehydrogenase kinase and Sln1 yeast histidine kinase by the antifungal antibiotic radicicol., Mol Pharmacol. 2002. Aug;62(2):289-96.