Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

539644 UCN-01

A cell-permeable Staurosporine derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases.

UCN-01 : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V

Primary Target: PKCα, 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
539644
Purchase on Sigma-Aldrich

Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
112953-11-4C₂₈H₂₆N₄O₄

Products

RéférenceConditionnement Qté
539644-500UG Ampoule plast. 500 μg
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
Global Trade Item Number
Référence GTIN
539644-500UG 04055977194821

Documentation

UCN-01 FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

UCN-01 Certificats d'analyse

TitreNuméro de lot
539644

Références bibliographiques

Aperçu de la référence bibliographique
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.
Fiche technique

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 Protect from light
+2°C to +8°C
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.

Produits & Applications associés

Catégories

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