2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Ack1

Ack1

Activated Cdc42 kinase 1; TNK2

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15290
    AIM-100
    		Inhibitor 99.95%
    AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.
    AIM-100
  • HY-10943
    GNF-7
    		Inhibitor 99.70%
    GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
    GNF-7
  • HY-12331
    KRCA-0008
    		Inhibitor
    KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.
    KRCA-0008
  • HY-162254
    EGFR/ACK1-IN-1
    		Inhibitor
    EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity.
    EGFR/ACK1-IN-1
  • HY-113787
    (R)-9b
    		Inhibitor
    (R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC50=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer.
    (R)-9b
  • HY-149989
    Ack1 inhibitor 1
    		Inhibitor
    Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.
    Ack1 inhibitor 1
  • HY-160635
    Ack1 inhibitor 2
    		Inhibitor
    Ack1 inhibitor 2 (Example 259) is an Ack1 inhibitor (IC50: 0.46 μM).
    Ack1 inhibitor 2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity