Ack1
ACK1 (Activated CDC42 kinase 1) is an enzyme that in humans is encoded by the TNK2 gene. TNK2 gene encodes a non-receptor tyrosine kinase, ACK1, that 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. This binding is mediated by a unique sequence of 47 amino acids C-terminal to an SH3 domain. The protein may be involved in a regulatory mechanism that sustains the GTP-bound active form of Cdc42Hs and which is directly linked to a tyrosine phosphorylation signal transduction pathway. CK1 or TNK2 has been shown to interact with AKT, Androgen receptor or AR, a tumor suppressor WWOX, FYN and Grb2. ACK1 interaction with its substrates resulted in their phosphorylation at specific tyrosine residues.
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GNF 7是Ras signaling 抑制剂， 抑制 Ack1，GCK。
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AIM 100是活性的，选择性 Ack1 (TNK2) 抑制剂。
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XMD8-87是有效的TNK2抑制剂，对D163E和R806Q突变型TNK2的IC50值分别为38 nM和113 nM。
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KRCA 0008是活性的 Ack1，ALK dual 抑制剂， 口服有效。
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