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| Product Name: | UCN-01 | | Synonyms: | UCN-01;7-hydroxystaurosporine;KW-2401;(9S)-2,3,10,11,12,13-Hexahydro-3α-hydroxy-10α-methoxy-9-methyl-11α-methylamino-9β,13β-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one;9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lM]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-Methoxy-9-Methyl-11-(MethylaMino)-, (3R,9S,10R,11R,13R)-;KRX-0601;NSC 638850;UNC 01 | | CAS: | 112953-11-4 | | MF: | C28H26N4O4 | | MW: | 482.53044 | | EINECS: | | Product Categories: | | Mol File: | 112953-11-4.mol |
| UCN-01 Chemical Properties |
| Boiling point | 705.7±60.0 °C(Predicted) | | density | 1.63±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: >5mg/mL | | form | Tan solid | | pka | 12.25±0.70(Predicted) | | color | light yellow | | optical activity | [α]20/D 130 to 160°, c = 0.2 in DMSO |
| WGK Germany | 3 | | RTECS | KC6600010 |
| UCN-01 Usage And Synthesis |
| Description | UCN-01 is a synthetic derivative of staurosporine with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM) and cyclin-dependent kinases (IC50s = 300-600 nM for Cdk1 and Cdk2). UCN-01 arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase Chk1 (IC50 = 7 nM), leading to apoptosis. | | Uses | UCN-01 is an indolocarbazole isolated from a high staurosporine-producing Streptomyces culture. UCN-01 inhibits protein kinase C (PKC) and cyclin-dependant kinase 2 (CDK2), resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by the latter agents. | | Uses | UCN 01 is a protein kinase C inhibitor which overrides ZEB1-induced chemoresistance in hepatocellular cancer in human. A cell-permeable Staurosporine derived anticancer agent that inhibits several protein kinases. | | General Description | A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC50 = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC50 = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC50 = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents. | | Biochem/physiol Actions | Cell permeable: yes |
| UCN-01 Preparation Products And Raw materials |
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