Date published: 2025-10-15

1-800-457-3801

SCBT Portrait Logo
Seach Input

CCT 018159 (CAS 171009-07-7)

5.0(1)
Write a reviewAsk a question

Alternate Names:
4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethyl-1,3-benzenediol
Application:
CCT 018159 is a cell-permeable compound that inhibits Hsp90 ATPase
CAS Number:
171009-07-7
Purity:
≥98%
Molecular Weight:
352.4
Molecular Formula:
C20H20N2O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

QUICK LINKS

CCT 018159 is a cell-permeable pyrazoloresorcinol compound that inhibits heat shock protein 90 (Hsp90) ATPase activity (IC50 = 3.2 muM and 6.6 muM against human HSP 90 beta and yeast Hsp90, respectively) by targeting the enzyme′s N-terminal ATP binding site. CCT 018159 exhibits no detectable effects against human HSP 70 or topoisomerase II even at concentrations as high as 100 μM and inhibits a panel of 20 studied kinases only at much higher concentrations. Unlike 17-AAG, the antitumor activity of CCT 018159 is not affected by the expression of NQ01/DT-diaphorase or P-glycoprotein. The mean cellular GI value of CCT 018159 across a panel of human cancer cell lines, including melanoma, was 5.3 mumol/L, and it caused cell cytostasis associated with a G arrest and induced apoptosis. Additionally, CCT 018159 inhibited essential endothelial and tumor cell functions related to invasion and angiogenesis.


CCT 018159 (CAS 171009-07-7) References

  1. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.  |  Cheung, KM., et al. 2005. Bioorg Med Chem Lett. 15: 3338-43. PMID: 15955698
  2. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.  |  Dymock, BW., et al. 2005. J Med Chem. 48: 4212-5. PMID: 15974572
  3. 4-Amino derivatives of the Hsp90 inhibitor CCT018159.  |  Barril, X., et al. 2006. Bioorg Med Chem Lett. 16: 2543-8. PMID: 16480864
  4. Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors.  |  Smith, NF., et al. 2006. Mol Cancer Ther. 5: 1628-37. PMID: 16818523
  5. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.  |  Sharp, SY., et al. 2007. Cancer Res. 67: 2206-16. PMID: 17332351
  6. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues.  |  Sharp, SY., et al. 2007. Mol Cancer Ther. 6: 1198-211. PMID: 17431102
  7. Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition.  |  Beloueche-Babari, M., et al. 2010. Oncotarget. 1: 185-97. PMID: 21037799
  8. HSP90 inhibitors enhance differentiation and MITF (microphthalmia transcription factor) activity in osteoclast progenitors.  |  van der Kraan, AG., et al. 2013. Biochem J. 451: 235-44. PMID: 23379601
  9. Inhibition of heat shock protein 90 decreases ACTH production and cell proliferation in AtT-20 cells.  |  Sugiyama, A., et al. 2015. Pituitary. 18: 542-53. PMID: 25280813
  10. Potential role of Hsp90 in rat islet function under the condition of high glucose.  |  Yang, X., et al. 2016. Acta Diabetol. 53: 621-8. PMID: 26997509
  11. Histone deacetylase activity mediates acquired resistance towards structurally diverse HSP90 inhibitors.  |  Chai, RC., et al. 2017. Mol Oncol. 11: 567-583. PMID: 28306192
  12. RETSAT associates with DDX39B to promote fork restarting and resistance to gemcitabine based chemotherapy in pancreatic ductal adenocarcinoma.  |  Tu, Q., et al. 2022. J Exp Clin Cancer Res. 41: 274. PMID: 36109793
  13. Advances in lung adenocarcinoma: A novel perspective on prognoses and immune responses of CENPO as an oncogenic superenhancer.  |  Shi, T., et al. 2023. Transl Oncol. 34: 101691. PMID: 37207381

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CCT 018159, 5 mg

sc-202526
5 mg
$91.00