539644 UCN-01

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₈H₂₆N₄O₄ 112953-11-4

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539644-500UG
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      Plastic ampoule 500 μg
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      Description
      OverviewA 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 µM 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 µM for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (> 15 µM), 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.
      Catalogue Number539644
      Brand Family Calbiochem®
      Synonyms7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V
      References
      ReferencesReinhardt, H.C., et al. 2007. Cancer Cell 11, 175.
      Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221.
      Sato, S., et al. 2002. Oncogene 21, 1727.
      Patel, V., et al. 2002. Clin. Cancer Res. 8, 3549.
      Leclerc, S., et al. 2001. J. Biol. Chem. 276, 251.
      Busby, E.C., et al. 2000. Cancer Res. 60, 2108.
      Hsueh, C.T., et al. 1998. Clin. Cancer Res. 4, 2201.
      Akiyama, T., et al. 1997. Cancer Res. 57, 1495.
      Seynaeve, C.M., et al. 1994. Mol. Pharmacol. 45, 1207.
      Takahashi, I., et al. 1987, J. Antibiot. 40, 1782.
      Product Information
      CAS number112953-11-4
      ATP CompetitiveY
      FormWhite to beige solid
      Hill FormulaC₂₈H₂₆N₄O₄
      Chemical formulaC₂₈H₂₆N₄O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPKCα, PKCβ, PKCγ, PKCδ PKCε, Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2, PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA
      Primary Target IC<sub>50</sub>IC50 = 29 nM, 34 nM, 30 nM, 590 nM, 530 nM, 7 nM, 27 nM, 50 nM, 50 nM, 150 nM, 1.04 µM, 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 µM, respectively for primary targets in the order listed
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      UCN-01 SDS

      Title

      Safety Data Sheet (SDS) 

      UCN-01 Certificates of Analysis

      TitleLot Number
      539644

      References

      Reference overview
      Reinhardt, H.C., et al. 2007. Cancer Cell 11, 175.
      Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221.
      Sato, S., et al. 2002. Oncogene 21, 1727.
      Patel, V., et al. 2002. Clin. Cancer Res. 8, 3549.
      Leclerc, S., et al. 2001. J. Biol. Chem. 276, 251.
      Busby, E.C., et al. 2000. Cancer Res. 60, 2108.
      Hsueh, C.T., et al. 1998. Clin. Cancer Res. 4, 2201.
      Akiyama, T., et al. 1997. Cancer Res. 57, 1495.
      Seynaeve, C.M., et al. 1994. Mol. Pharmacol. 45, 1207.
      Takahashi, I., et al. 1987, J. Antibiot. 40, 1782.

      Brochure

      Title
      PKC Pathway Poster PDF ( 676 KB )
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision22-June-2009 RFH
      Synonyms7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V
      DescriptionA 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 µM 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 µM for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (> 15 µM), 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.
      FormWhite to beige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number112953-11-4
      Chemical formulaC₂₈H₂₆N₄O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml) or Ethanol (1 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesReinhardt, H.C., et al. 2007. Cancer Cell 11, 175.
      Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221.
      Sato, S., et al. 2002. Oncogene 21, 1727.
      Patel, V., et al. 2002. Clin. Cancer Res. 8, 3549.
      Leclerc, S., et al. 2001. J. Biol. Chem. 276, 251.
      Busby, E.C., et al. 2000. Cancer Res. 60, 2108.
      Hsueh, C.T., et al. 1998. Clin. Cancer Res. 4, 2201.
      Akiyama, T., et al. 1997. Cancer Res. 57, 1495.
      Seynaeve, C.M., et al. 1994. Mol. Pharmacol. 45, 1207.
      Takahashi, I., et al. 1987, J. Antibiot. 40, 1782.

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      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Tyrosine Kinase (PTK) Inhibitors
      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Kinase G (PKG; cGMP-Dependent Protein Kinase) Inhibitors
      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Glycogen Synthase Kinase (GSK) Inhibitors
      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Cell Cycle/Cell Division > Cyclin-Dependent Kinase (Cdk) Inhibitors
      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Kinase C (PKC) Inhibitors