p110β Selective Inhibitors
Information
TGX-221 is ap110β-specific inhibitor withIC50of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
In vitro
The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform.
In vivo
As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups.
Cell Data
cell lines：OPM-2/GFP, KMS-11, RPMI 8226, and NCI-H929 cells
Concentrations：~20 μM
Incubation Time：24-72 hours
Powder Purity:≥95%
| CAS | 663619-89-4 |
|---|---|
| Concentração | 10mM in DMSO |
| Sinónimos | 7-methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one |
| Especificações e pureza | Moligand™, 10mM in DMSO |
| Condições de armazenamento de armazenamento | Store at -80°C |
| Enviado em | Dry ice packs + Cold packs |
| Product Description | Information TGX-221 is ap110β-specific inhibitor withIC50of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. In vivo As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. cell lines：OPM-2/GFP, KMS-11, RPMI 8226, and NCI-H929 cells Concentrations：~20 μM Incubation Time：24-72 hours Powder Purity:≥95% |
| Solubilidade | Solubility (25°C) In vitro DMSO: 92 mg/mL (199.46 mM); Ethanol: 92 mg/mL (199.46 mM); Water: Insoluble; |
