ACK1
Activated Cdc42 (cell division cycle 42)-associated tyrosine kinase (ACK1; EC 2.7.10.2), also called TNK2 (tyrosine kinase, non-receptor, 2) is activated in response to multiple cellular signals, including cell adhesion, growth factor receptors and heterotrimeric GPCR-signaling. interaction of the SH3 (Src homology 3) domain with the EBD (EGFR-binding domain) in ACK1 forms an auto-inhibition of the kinase activity. Release of this auto-inhibition is a key step for activation of ACK1. Mutation of the SH3 domain caused activation of ACK1, independent of cell adhesion, suggesting that cell adhesion-mediated activation of ACK1 is through releasing the auto-inhibition. ACK is amplified and overexpressed in multiple cancers, and associated with tumour progression through promoting cell growth and migration[1].
[1] Q. Lin et al. The activation mechanism ofACK1 (activated Cdc42-associated tyrosine kinase 1). Biochem. J. 2012, 445, 255-264.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2031 | AIM 100 | Specific inhibitor of Ack1 tyrosine kinase (also known as TNK2) | €95.00 | |
| 2294 | KRCA 0008 | Potent and selective dual ALK/ACK1 inhibitor with good drug-like properties | €95.00 | |
| 2762 | XMD 8-87 | Potent and selective inhibitor of Ack1 tyrosine kinase (also known as TNK2) | €95.00 | |