| Name | CAN508 |
| Description | CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.] |
| In vitro | The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (22.91 mM), Sonication is recommended. DMSO : 250 mg/mL (1145.63 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | HT-29 | esophageal | Cyclin dependent kinase | cells | CDK9/cyclin T1 | CDK | CAN-508 | CAN508 | CAN 508 | ATP-competitive | adenocarcinoma |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | PF07104091 | Abemaciclib | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Multi-Target Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | High-Efficiency Gene Editing Small Molecule Library |