For research use only. Not for therapeutic Use.
KRX-0601, also known as UCN-01, is a synthetic derivative of staurosporine with antineoplastic activity. 7-hydroxystaurosporine inhibits many phosphokinases, including the serine/threonine kinase AKT, calcium-dependent protein kinase C, and cyclin-dependent kinases. This agent arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
| Catalog Number | M019098 |
| CAS Number | 112953-11-4 |
| Synonyms | (3R,9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one |
| Molecular Formula | C28H26N4O4 |
| Purity | ≥95% |
| Target | PDK-1 |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| InChI | InChI=1S/C28H26N4O4/c1-28-25(35-3)15(29-2)12-18(36-28)31-16-10-6-4-8-13(16)19-21-22(27(34)30-26(21)33)20-14-9-5-7-11-17(14)32(28)24(20)23(19)31/h4-11,15,18,25,27,29,34H,12H2,1-3H3,(H,30,33)/t15-,18-,25-,27-,28+/m1/s1 |
| InChIKey | PBCZSGKMGDDXIJ-HQCWYSJUSA-N |
| SMILES | CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)C(NC6=O)O)NC)OC |
| Reference | </br>1:UCN-01 enhances cytotoxicity of irinotecan in colorectal cancer stem-like cells by impairing DNA damage response. Signore M, Buccarelli M, Pilozzi E, De Luca G, Cappellari M, Fanciulli M, Goeman F, Melucci E, Biffoni M, Ricci-Vitiani L.Oncotarget. 2016 Jul 12;7(28):44113-44128. doi: 10.18632/oncotarget.9859. PMID: 27286453 Free PMC Article</br>2:Tetra-O-Methyl Nordihydroguaiaretic Acid Broadly Suppresses Cancer Metabolism and Synergistically Induces Strong Anticancer Activity in Combination with Etoposide, Rapamycin and UCN-01. Kimura K, Huang RC.PLoS One. 2016 Feb 17;11(2):e0148685. doi: 10.1371/journal.pone.0148685. eCollection 2016. PMID: 26886430 Free PMC Article</br>3:Caspase-9 mediates Puma activation in UCN-01-induced apoptosis. Nie C, Luo Y, Zhao X, Luo N, Tong A, Liu X, Yuan Z, Wang C, Wei Y.Cell Death Dis. 2014 Oct 30;5:e1495. doi: 10.1038/cddis.2014.461. PMID: 25356864 Free PMC Article</br>4:The phosphoinositide-dependent protein kinase 1 inhibitor, UCN-01, induces fragmentation: possible role of metalloproteinases. Alcántara-Hernández R, Hernández-Méndez A, García-Sáinz JA.Eur J Pharmacol. 2014 Oct 5;740:88-96. doi: 10.1016/j.ejphar.2014.06.057. Epub 2014 Jul 10. PMID: 25016091 </br>5:UCN-01 induces S and G2/M cell cycle arrest through the p53/p21(waf1) or CHK2/CDC25C pathways and can suppress invasion in human hepatoma cell lines. Wu G, Lin N, Xu L, Liu B, Feitelson MA.BMC Cancer. 2013 Mar 28;13:167. doi: 10.1186/1471-2407-13-167. Erratum in: BMC Cancer. 2014;14:216. Feitelson, Mark A [added]. PMID: 23537372 Free PMC Article</br>6:Phase I study of UCN-01 and perifosine in patients with relapsed and refractory acute leukemias and high-risk myelodysplastic syndrome. Gojo I, Perl A, Luger S, Baer MR, Norsworthy KJ, Bauer KS, Tidwell M, Fleckinger S, Carroll M, Sausville EA.Invest New Drugs. 2013 Oct;31(5):1217-27. doi: 10.1007/s10637-013-9937-8. Epub 2013 Feb 27. PMID: 23443507 Free PMC Article</br>7:A phase II study of UCN-01 in combination with irinotecan in patients with metastatic triple negative breast cancer. Ma CX, Ellis MJ, Petroni GR, Guo Z, Cai SR, Ryan CE, Craig Lockhart A, Naughton MJ, Pluard TJ, Brenin CM, Picus J, Creekmore AN, Mwandoro T, Yarde ER, Reed J, Ebbert M, Bernard PS, Watson M, Doyle LA, Dancey J, Piwnica-Worms H, Fracasso PM.Breast Cancer Res Treat. 2013 Jan;137(2):483-92. doi: 10.1007/s10549-012-2378-9. Epub 2012 Dec 15. PMID: 23242585 Free PMC Article</br>8:Celecoxib enhances the radiosensitizing effect of 7-hydroxystaurosporine (UCN-01) in human lung cancer cell lines. Kim YM, Jeong IH, Pyo H.Int J Radiat Oncol Biol Phys. 2012 Jul 1;83(3):e399-407. doi: 10.1016/j.ijrobp.2012.01.001. Epub 2012 Mar 13. PMID: 22417802 </br>9:Determinants of mitotic catastrophe on abrogation of the G2 DNA damage checkpoint by UCN-01. On KF, Chen Y, Ma HT, Chow JP, Poon RY.Mol Cancer Ther. 2011 May;10(5):784-94. doi: 10.1158/1535-7163.MCT-10-0809. Epub 2011 Mar 23. PMID: 21430130 Free Article</br>10:Sodium butyrate with UCN-01 has marked antitumour activity against cervical cancer cells. Decrion-Barthod AZ, Bosset M, Plissonnier ML, Marchini A, Nicolier M, Launay S, Prétet JL, Rommelaere J, Mougin C.Anticancer Res. 2010 Oct;30(10):4049-61. PMID: 21036719 |
