GSK1059615
GSK1059615 is inhibitor of pan-PI3K with IC50 values of 0.4nM, 0.6nM, 5nM, 2nM and 12nM for PI3Kα, P13Kβ, P13Kγ, P13Kδ and mTOR, respectively [1].
GSK1059615 is a potent and reversible inhibitor of P13K. It also has inhibition efficacy to the oncogenic mutants of PI3Kα. The thiazolidinedione ring of GSK1059615 forms an interaction with the catalytic lysine (Lys833) within the ATP-binding pocket. In cellular assay, GSK1059615 is reported to induce G1 arrest and apoptosis in a variety of cell lines. Among these, the breast tumor cells display more sensitive. Moreover, GSK1059615 significantly suppresses tumor growth and increases plasma insulin levels in xenograft mice [1, 2].
References:
[1] Carnero A. Novel inhibitors of the PI3K family. 2009.
[2] Knight S D, Adams N D, Burgess J L, et al. Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Medicinal Chemistry Letters, 2010, 1(1): 39-43.
| Storage | Store at -20°C |
| M.Wt | 333.36 |
| Cas No. | 958852-01-2 |
| Formula | C18H11N3O2S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥8.33 mg/mL in DMSO with gentle warming |
| Chemical Name | (5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione |
| SDF | Download SDF |
| Canonical SMILES | C1=CC2=NC=CC(=C2C=C1C=C3C(=O)NC(=O)S3)C4=CC=NC=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 values of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. | |||||
| Targets | PI3Kα | PI3Kβ | PI3Kδ | PI3Kγ | mTOR | |
| IC50 | 0.4 nM | 0.6 nM | 2 nM | 5 nM | 12 nM | |
Quality Control & MSDS
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Chemical structure
