All AbMole products are for research use only, cannot be used for human consumption.
SU9516 is a selective cdk2 inhibitor and support the theory that compounds that inhibit cdk2 are viable resources in the development of new antineoplastic agents. SU9516 is 9-fold and 1.8-fold more selective for cdk2 than cdk4 and cdk1, respectively. Treatment with SU9516 (5 μM) inhibited (P ≤ 0.05) both cdk2-specific (27–64%) and cdk4-specific (26–49%) phosphorylation of pRb in SW480 cells at all (24, 48, and 72 h) time points. RKO cells remained blocked in G2-M at 20 h post-serum induction and -addition of SU9516. SU9516 produced a dose-dependent G1 accumulation in EGF-stimulated cells.Treatment with 5 microM SU9516 prevented dissociation of pRb from E2F1 in all cell lines (HT-29>RKO>SW480). Treatment effects were time-dependent, demonstrating greater inhibition at 48 hr versus 24hr in HT-29 cells. Furthermore, E2F species were sequestered in complexes with p107, p130, DP-1, and cyclins A and E. After a 24-hr treatment with 5 microM SU9516, cyclin D1 and cdk2 levels decreased by 10-60%. Exposure of U937 and other leukemia cells to SU9516 concentrations > or =5 microM rapidly (i.e., within 4 h) induced cytochrome c release, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1.
| Cell Experiment | |
|---|---|
| Cell lines | RKO cells and SW480 cells |
| Preparation method | Seeding RKO cells and SW480 cells in replicates in 96-well plates at 1 × 104 cells/well and allowing to attach overnight. adding SU9516 in concentrations from 0.05 μM to 50.00 μM for 24 h, then washing the cells twice with PBS, and replenishing cells with complete media. Fixing the cells at 0, 4, and 7 days post-drug removal and assaying for protein levels using a modified SRB cytotoxicity assay.Fixing the cells in 10% trichloroacetic acid for 1 h, washing in distilled H2O, and staining in 0.4% SRB/acetic acid for 30 min. Then washing the cells in 0.1% acetic acid, solubilizing in 10 mM Tris (pH 9), and analyzing on a Bio-Rad 360 microplate reader at 595 nm. Repeating all experiments at least three times. |
| Concentrations | ~50 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 241.25 |
| Formula | C13H11N3O2 |
| CAS Number | 377090-84-1 |
| Solubility (25°C) | DMSO 100 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CDK Products |
|---|
| (E/Z)-Zotiraciclib citrate
(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor. |
| Abemaciclib metabolites M2
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50 values of 1.2 and 1.3 nM, respectively. |
| CDK9-IN-1
CDK9-IN-1 is a novel, selective CDK9 inhibitor, with an IC50 of 39 nM for CDK9/CycT1, it can be used for the research of HIV infection. |
| XO44
XO44 (PF-6808472) is a broad-spectrum covalent kinase probe. |
| ML 315
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
