Signaling Pathway

Ack1

Ack1

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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.

Ack1 Inhibitors & Modulators (2)

Product Name Catalog No. Brief Description
AIM-100

HY-15290

AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.

KRCA-0008

HY-12331

KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.