LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。
| CAS No. | 154447-36-6 |
| 生物活性 | LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator. |
| 分子式 | C19H17NO3 |
| 分子量 | 307.34 |
| 储存条件 | Powder -20℃ 3 years |
| 溶解性数据 | DMSO : 50 mg/mL (162.69 mM; Need ultrasonic) Ethanol : 50 mg/mL (162.69 mM; Need ultrasonic) |
| 体内研究 | LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden. LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats. |
| 体外研究 | LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion. LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent. LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration. LY294002 (5, 10, 100 µM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 µM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels. |
| 文献 | Buqi Huoxue Tongnao prescription protects against chronic cerebral hypoperfusion via regulating PI3K/AKT and LXRα/CYP7A1 signaling pathways |
| 纯度及产品资料 | 98% |
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