| 货号 | CAS号 |
|---|---|
| P125966-10mg | 372196-77-5 |
| P125966-50mg | 372196-77-5 |
| P125966-100mg | 372196-77-5 |
| 溶解性 | DMSO ≥16mg/mL Water <1.2mg/mL Ethanol ≥4.6mg/mL |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | PIK-75是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，亚型特异性的突变体在Ser773，也有效抑制DNA-PK，IC50为2 nM。 |
| 备注 | PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM. |
| 生化机理 |
PIK-75 Hydrochloride is a hydrochloride salt form of PIK-75, which is a preferential p110α/γ forms of PI3K inhibitor with IC50 of 6, 1300, 76, 510 nM for p110α, p110β, p110γ, p110δ, respectively. PIK-75 is a PI3K p110α specific inhibitor and belongs to the class of imidazo[1, 2-a]pyridines. It inhibited cell proliferation of A375 cells (IC50=58nM) in vitro and reduced tumor growth in a mouse xenograft model. Besides inhibition of PI3Kα, PIK-75 also inhibited DNA-PK with an IC50 of 2 nM, but not mTORC1 and mTORC2. PIK-75-mediated anti-inflammatory effects are associated with dramatic inhibition of AKT phosphorylation, IKK activation and NF-κB transcription. |
| 别名 | PIK 75; 2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐;PIK-75 Hydrochloride; PIK 75;2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride |
