Date published: 2025-10-10

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UCN-01 (CAS 112953-11-4)

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Alternate Names:
7-hydroxystaurosporine
Application:
UCN-01 is a selective inhibitor of protein kinase C
CAS Number:
112953-11-4
Purity:
>95%
Molecular Weight:
482.53
Molecular Formula:
C28H26N4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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UCN-01 is a Staurosporine (sc-3510) analogue that acts as a selective inhibitor of protein kinase C and is reported to potently inhibit MK2. The compound may act to induce UCN-01 G1 phase accumulation, dephosphorylate Rb and CDK2 proteins, and induce CDK inhibitor p21/Cip1/WAF1/Sdi1 in A431 (sc-2201) cells with mutated p53. Additionally, UCN-01 has been demonstrated to suppress protein expression of thymidylate synthase and E2F-1, inhibit DNA damage checkpoint kinase hChk1, and interrupt the PDK1-Akt survival signaling pathway. UCN-01 has also been noted to inhibit cell proliferation in HNSCC cells. It effectively suppresses the activity of various kinases, such as Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM), and cyclin-dependent kinases (with IC50 values ranging from 300-600 nM for Cdk1 and Cdk2).


UCN-01 (CAS 112953-11-4) References

  1. The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.  |  Busby, EC., et al. 2000. Cancer Res. 60: 2108-12. PMID: 10786669
  2. UCN-01 suppresses E2F-1 mediated by ubiquitin-proteasome-dependent degradation.  |  Hsueh, CT., et al. 2001. Clin Cancer Res. 7: 669-74. PMID: 11297263
  3. Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine).  |  Sato, S., et al. 2002. Oncogene. 21: 1727-38. PMID: 11896604
  4. Antitumor activity of UCN-01 in carcinomas of the head and neck is associated with altered expression of cyclin D3 and p27(KIP1).  |  Patel, V., et al. 2002. Clin Cancer Res. 8: 3549-60. PMID: 12429646
  5. Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.  |  Jiang, X., et al. 2004. Mol Cancer Ther. 3: 1221-7. PMID: 15486189
  6. Hemodynamic regulation of myosin heavy chain gene expression. Studies in the transplanted rat heart.  |  Klein, I., et al. 1992. J Clin Invest. 89: 68-73. PMID: 1729282
  7. UCN-01 (7-hydroxystaurosporine) induces apoptosis and G1 arrest of both primary and metastatic oral cancer cell lines in vitro.  |  Otsubo, A., et al. 2007. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 103: 391-7. PMID: 17321452
  8. UCN-01, a selective inhibitor of protein kinase C from Streptomyces.  |  Takahashi, I., et al. 1987. J Antibiot (Tokyo). 40: 1782-4. PMID: 3429345
  9. Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.  |  Seynaeve, CM., et al. 1994. Mol Pharmacol. 45: 1207-14. PMID: 8022414
  10. G1 phase accumulation induced by UCN-01 is associated with dephosphorylation of Rb and CDK2 proteins as well as induction of CDK inhibitor p21/Cip1/WAF1/Sdi1 in p53-mutated human epidermoid carcinoma A431 cells.  |  Akiyama, T., et al. 1997. Cancer Res. 57: 1495-501. PMID: 9108451
  11. 7-Hydroxystaurosporine (UCN-01) causes redistribution of proliferating cell nuclear antigen and abrogates cisplatin-induced S-phase arrest in Chinese hamster ovary cells.  |  Bunch, RT. and Eastman, A. 1997. Cell Growth Differ. 8: 779-88. PMID: 9218872
  12. 7-Hydroxystaurosporine (UCN-01) induces apoptosis in human colon carcinoma and leukemia cells independently of p53.  |  Shao, RG., et al. 1997. Exp Cell Res. 234: 388-97. PMID: 9260909
  13. UCN-01 suppresses thymidylate synthase gene expression and enhances 5-fluorouracil-induced apoptosis in a sequence-dependent manner.  |  Hsueh, CT., et al. 1998. Clin Cancer Res. 4: 2201-6. PMID: 9748140

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

UCN-01, 500 µg

sc-202376
500 µg
$246.00