GGTI-2418
| CAS号 | 501010-06-6 | 货号 | BCP30523 |
| 中文名 | GGTI-2418 | ||
| 英文名 | GGTI-2418 | ||
| 中文别名 | |||
| 英文别名 | GGTI2418; GGTI 2418; PTX-100; PTX 100; PTX100;Geranylgeranyl transferase inhibitor-2148; | ||
| 分子式 | C23H31N5O4 | 分子量 | 441.53 |
| 生物活性 | GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways. GGTase I catalyzes the lipid posttranslational modification which is required for the function of Rho GTPases (frequently found aberrantly activated in human cancer). GGTase I inhibitors block Rho function in cancer cells and induce a G1 phase cell cycle arrest by a mechanism involving induction of the CDK inhibitors p21waf and p27kip, CDK2 and CDK4 inhibition and hypophoshorylation of the tumor suppressor Rb. GGTase I inhibitors also induce apoptosis by a mechanism involving downregulation of the expression of survivin and suppression of the activation of PI3K/Akt. | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | Ras/Rho | ||
结构式
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