| Name | GW843682X |
| Description | GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM). |
| In vitro | GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X inhibits the proliferation of U937 cells with an EC50 of 120 nM[1]. GW843682X (0.06-1 μM) has inhibitory activities against the proliferation of acute leukemia cells and potentiates the anti-proliferative activity of vincristine. GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells[2]. GW843682X is effective in inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53 (IC50 = 0.14 μM). GW843682X (3 μM) causes strong G2-M arrest in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 2 mg/mL (4.19 mM), Sonication is recommended.
DMSO : 30 mg/mL (62.83 mM), Sonication is recommended.
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| Keywords | VEGFR2 | Polo-like Kinase (PLK) | PLK3 | PLK1 | PDGFRβ | PDGFR1β | GW843682X | GW-843682 | GW 843682 | CDK2/CyclinA | CDK2/cyclin A | AuroraKinase | Aurora Kinase | Aurora A |
| Inhibitors Related | Ribociclib | 2-Chloropyrazine | Kojic acid | Sorafenib | Pyridoxine | Abemaciclib | Nintedanib esylate | 2,4,6-Trihydroxybenzoic acid | Chloramphenicol | Palbociclib | Lenvatinib | Pazopanib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
