API-1 是一种有效的 Akt/PKB 抑制剂，与 PH 结构域结合并抑制 Akt 膜易位。 API-1 有效降低 Akt 的磷酸化水平，IC50 为 ~0.8 μM。 API-1 对 PKB 具有选择性，不抑制 PKC 和 PKA 的激活。 API-1 还通过与 TNF 相关的凋亡诱导配体 (TRAIL) 协同作用来诱导细胞凋亡。
| Cas No. | 36707-00-3 |
| 化学名 | 4-amino-5,8-dihydro-5-oxo-8-β-D-ribofuranosyl-pyrido[2,3-d]pyrimidine-6-carboxamide |
| Canonical SMILES | O=C1C2=C(N)N=CN=C2N([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C=C1C(N)=O |
| 分子式 | C13H15N5O6 |
| 分子量 | 337.3 |
| 溶解度 | DMSO : 5.8 mg/mL (15.45 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | API-1 is an inhibitor of Akt that reduces the level of phosphorylated Akt (IC50 = ~0.8 uM in OVCAR3 cells) by binding to Akt and blocking its translocation to the cell membrane. It reduces cell proliferation in various cancer cell lines, induces apoptosis, and, at a dose of 10 mg/kg per day, decreases tumor growth in a mouse xenograft model. API-1 inhibition of Akt leads to proteasomal degradation of the downstream mediator Mcl-1. Likely independent of Akt binding, API-1 inhibits cell growth (IC50s = 2-5 uM) and induces apoptosis in non-small cell lung and head and neck squamous cancer (NSCLC and HNSCC) cell lines with concomitant increases in caspase-3, -8, and -9 cleavage. It reduces the levels of cellular FLICE-inhibitory protein (c-FLIP), an important regulator of apoptosis, through ubiquitin- and proteasome-mediated degradation. It also has a synergistic effect on apoptosis in combination with TRAIL/APO-2L.The information regarding the reduction in phosphorylated Akt levels, IC50 value, translocation, cell proliferation, and xenograft tumor growth was drawn from a paper that has been retracted; however, the information specified in the retraction statement has not been included. |
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