Date published: 2025-12-3

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PCI-24781 (CAS 783355-60-2)

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Application:
PCI-24781 is an HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor
CAS Number:
783355-60-2
Purity:
≥98%
Molecular Weight:
397.42
Molecular Formula:
C21H23N3O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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PCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 mumol/L, as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 mumol/L. PCI-24781 is an innovative inhibitor of histone deacetylases (HDACs), a class of enzymes responsible for epigenetic control of gene expression.


PCI-24781 (CAS 783355-60-2) References

  1. Radiosensitization by the histone deacetylase inhibitor PCI-24781.  |  Banuelos, CA., et al. 2007. Clin Cancer Res. 13: 6816-26. PMID: 18006784
  2. PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-kappaB mechanisms and is synergistic with bortezomib in lymphoma cells.  |  Bhalla, S., et al. 2009. Clin Cancer Res. 15: 3354-65. PMID: 19417023
  3. PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells.  |  Rivera-Del Valle, N., et al. 2010. Int J Cell Biol. 2010: 207420. PMID: 20145726
  4. Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells.  |  Yang, C., et al. 2011. Cancer Chemother Pharmacol. 67: 439-46. PMID: 20461381
  5. Histone deacetylase inhibitor PCI-24781 enhances chemotherapy-induced apoptosis in multidrug-resistant sarcoma cell lines.  |  Yang, C., et al. 2011. Anticancer Res. 31: 1115-23. PMID: 21508354
  6. The therapeutic effect of histone deacetylase inhibitor PCI-24781 on gallbladder carcinoma in BK5.erbB2 mice.  |  Kitamura, T., et al. 2012. J Hepatol. 57: 84-91. PMID: 22326466
  7. RuvBL2 is involved in histone deacetylase inhibitor PCI-24781-induced cell death in SK-N-DZ neuroblastoma cells.  |  Zhan, Q., et al. 2013. PLoS One. 8: e71663. PMID: 23977108
  8. RAD51 potentiates synergistic effects of chemotherapy with PCI-24781 and cis-diamminedichloroplatinum on gastric cancer.  |  He, WL., et al. 2014. World J Gastroenterol. 20: 10094-107. PMID: 25110436
  9. PCI-24781 down-regulates EZH2 expression and then promotes glioma apoptosis by suppressing the PIK3K/Akt/mTOR pathway.  |  Zhang, W., et al. 2014. Genet Mol Biol. 37: 716-24. PMID: 25505847
  10. PCI-24781 (abexinostat), a novel histone deacetylase inhibitor, induces reactive oxygen species-dependent apoptosis and is synergistic with bortezomib in neuroblastoma.  |  Sholler, GS., et al. 2013. J Cancer Ther Res. 2: 21. PMID: 25520806
  11. HDAC Inhibitors as Novel Anti-Cancer Therapeutics.  |  De Souza, C. and Chatterji, BP. 2015. Recent Pat Anticancer Drug Discov. 10: 145-62. PMID: 25782916
  12. The histone deacetylase inhibitor PCI-24781 as a putative radiosensitizer in pediatric glioblastoma cell lines.  |  de Andrade, PV., et al. 2016. Cancer Cell Int. 16: 31. PMID: 27095947
  13. PCI-24781 can improve in vitro and in vivo developmental capacity of pig somatic cell nuclear transfer embryos.  |  Jin, L., et al. 2016. Biotechnol Lett. 38: 1433-41. PMID: 27271328
  14. The histone deacetylase inhibitor PCI-24781 impairs calcium influx and inhibits proliferation and metastasis in breast cancer.  |  Yang, T., et al. 2021. Theranostics. 11: 2058-2076. PMID: 33500709

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PCI-24781, 5 mg

sc-364565
5 mg
$182.00

PCI-24781, 50 mg

sc-364565A
50 mg
$1330.00