Ack1 (Activated Cdc42 kinase 1) is an enzyme that in humans is encoded by the TNK2 gene. Ack1 binds to multiple receptor tyrosine kinases e.g. EGFR, MERTK, AXL, HER2 and insulin receptor (IR). Ack1 also interacts with Cdc42Hs in its GTP-bound form and inhibits both the intrinsic and GTPase-activating protein (GAP)-stimulated GTPase activity of Cdc42Hs. Ack1 is a survival kinase and shown to be associated with tumor cell survival, proliferation, hormone-resistance and radiation resistance. Ack1 has emerged as a new cancer target and multiple small molecule inhibitors have been reported.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PC16015 | AIM-100 | 873305-35-2 | Ack1抑制剂,AIM-100是Ack1抑制剂,IC50为24 nM。 |
PL01794 | GNF-7 | 839706-07-9 | GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂,对 Bcr-Abl<sup>WT</sup> 和 Bcr-Abl<sup>T315I</sup> 作用的 IC50 值分别为 133 nM 和 61 nM。GNF-7 对 ACK1 和 GCK 也具有抑制活性,IC50 分别为 25 nM 和 8 nM。GNF-7 可用于血液恶性肿瘤的研究。 |