Potent inhibitor of cdk4/cyclin D1 (IC50 = 59 nM). Also active against CaM kinase II (IC50 = 25 nM) but displays selectivity over several other kinases in vitro (IC50 values for inhibition of PKA and PKC are > 2 and > 100 μM respectively). Inhibits human cytomegalovirus (HCMV) replication in vitro (IC50 = 200 nM).
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 325.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.07 mL||15.37 mL||30.74 mL|
|5 mM||0.61 mL||3.07 mL||6.15 mL|
|10 mM||0.31 mL||1.54 mL||3.07 mL|
|50 mM||0.06 mL||0.31 mL||0.61 mL|
References are publications that support the biological activity of the product.
Slater et al (1999) Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication. Bioorg.Med.Chem. 7 1067 PMID: 10428375
Zhu et al (2003) Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. Bioorg.Med.Chem.Lett. 13 1231 PMID: 12657252
Sanchez-Martinez et al (2003) Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. Bioorg.Med.Chem.Lett. 13 3835 PMID: 14552791
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.