API-1
Cat. No.：YN420402
| 产品名称: | API-1 |
| CAS No.: | 36707-00-3 |
| Chemical Name: | 4-amino-5,8-dihydro-5-oxo-8-β-D-ribofuranosyl-pyrido[2,3-d]pyrimidine-6-carboxamide |
| Synonyms: | |
| 分子量: | 337.3 |
| 分子式: | C13H15N5O6 |
| SMILES: | O=C1C2=C(N)N=CN=C2N([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C=C1C(N)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | 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 (apoptosis)。 |
| IC50和靶点: | |
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Kim, D., Sun, M., He, L., et al.A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocationJ. Biol. Chem.285(11),8383-8394(2010)
Ren, H., Koo, J., Guan, B., et al.The E3 ubiquitin ligases β-TrCP and FBXW7 cooperatively mediates GSK3-dependent Mcl-1 degradation induced by the Akt inhibitor API-1, resulting in apoptosisMol. Cancer12,146(2013)
Li, B., Ren, H., Yue, P., et al.The novel Akt inhibitor API-1 induces c-FLIP degradation and synergizes with TRAIL to augment apoptosis independent of Akt inhibitionCancer Prev. Res. (Phila.)5(4),612-620(2012)
