Date published: 2026-2-3

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ICRF-193 (CAS 21416-68-2)

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Alternate Names:
4,4′-(1,2-Dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione
Application:
ICRF-193 is a bisdioxopiperazine which induces apoptosis and erythroid differentiation
CAS Number:
21416-68-2
Purity:
≥95%
Molecular Weight:
282.30
Molecular Formula:
C12H18N4O4
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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ICRF-193, a bisdioxopiperazine, is a catalytic noncleavable complex-forming inhibitor of DNA Topo II (topoisomerase II) that does not produce protein-linked DNA strand breaks. This compound may act to induce erythroid differentiation and apoptosis. Mechanistic studies suggest that ICRF-193 affects the caspase-3 activation/cleavage pathway of cell growth and associates with ATR-dependent inhibition of polo-like kinase (plk) 1 kinase activity and a decrease in cyclin B1 phosphorylation. ICRF-193 is an inhibitor of Topo II beta.


ICRF-193 (CAS 21416-68-2) References

  1. Probing the interaction of the cytotoxic bisdioxopiperazine ICRF-193 with the closed enzyme clamp of human topoisomerase IIalpha.  |  Patel, S., et al. 2000. Mol Pharmacol. 58: 560-8. PMID: 10953049
  2. The catalytic DNA topoisomerase II inhibitor dexrazoxane (ICRF-187) induces differentiation and apoptosis in human leukemia K562 cells.  |  Hasinoff, BB., et al. 2001. Mol Pharmacol. 59: 453-61. PMID: 11179439
  3. Decreased thymosin beta4 in apoptosis induced by a variety of antitumor drugs.  |  Iguchi, K., et al. 1999. Biochem Pharmacol. 57: 1105-11. PMID: 11230797
  4. ICRF-193, a catalytic inhibitor of DNA topoisomerase II, inhibits re-entry into the cell division cycle from quiescent state in mammalian cells.  |  Hossain, MS., et al. 2002. Genes Cells. 7: 285-94. PMID: 11918672
  5. ATR enforces the topoisomerase II-dependent G2 checkpoint through inhibition of Plk1 kinase.  |  Deming, PB., et al. 2002. J Biol Chem. 277: 36832-8. PMID: 12147700
  6. DNA strand breaks induced by the anti-topoisomerase II bis-dioxopiperazine ICRF-193.  |  Hajji, N., et al. 2003. Mutat Res. 530: 35-46. PMID: 14563529
  7. Cell cycle-dependent DNA damage signaling induced by ICRF-193 involves ATM, ATR, CHK2, and BRCA1.  |  Park, I. and Avraham, HK. 2006. Exp Cell Res. 312: 1996-2008. PMID: 16630610
  8. ICRF-193, an anticancer topoisomerase II inhibitor, induces arched telophase spindles that snap, leading to a ploidy increase in fission yeast.  |  Nakazawa, N., et al. 2016. Genes Cells. 21: 978-93. PMID: 27458047
  9. DNA binding activity of the proximal C-terminal domain of rat DNA topoisomerase IIβ is involved in ICRF-193-induced closed-clamp formation.  |  Kawano, S., et al. 2020. PLoS One. 15: e0239466. PMID: 32960919
  10. Development of water-soluble prodrugs of the bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 as potential cardioprotective agents against anthracycline cardiotoxicity.  |  Bavlovič Piskáčková, H., et al. 2021. Sci Rep. 11: 4456. PMID: 33627707
  11. Structure-Activity Relationship Study of Dexrazoxane Analogues Reveals ICRF-193 as the Most Potent Bisdioxopiperazine against Anthracycline Toxicity to Cardiomyocytes Due to Its Strong Topoisomerase IIβ Interactions.  |  Jirkovská, A., et al. 2021. J Med Chem. 64: 3997-4019. PMID: 33750129
  12. Prodrug of ICRF-193 provides promising protective effects against chronic anthracycline cardiotoxicity in a rabbit model in vivo.  |  Kollárová-Brázdová, P., et al. 2021. Clin Sci (Lond). 135: 1897-1914. PMID: 34318878
  13. ICRF-193, an inhibitor of topoisomerase II, demonstrates that DNA replication in sperm nuclei reconstituted in Xenopus egg extracts does not require chromatin decondensation.  |  Takasuga, Y., et al. 1995. Exp Cell Res. 217: 378-84. PMID: 7698239
  14. ICRF-193 modifies etoposide-induced apoptosis in thymocytes.  |  Tanimoto, C., et al. 1995. Acta Med Okayama. 49: 281-6. PMID: 8770236
  15. ICRF-193, a catalytic inhibitor of DNA topoisomerase II, delays the cell cycle progression from metaphase, but not from anaphase to the G1 phase in mammalian cells.  |  Iwai, M., et al. 1997. FEBS Lett. 406: 267-70. PMID: 9136899

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

ICRF-193, 1 mg

sc-200889
1 mg
$341.00

ICRF-193, 5 mg

sc-200889A
5 mg
$927.00