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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

ACK1

ACK1 (Activated Cdc42-associated Kinase 1), also known as TNK2, is a non-receptor tyrosine kinase activated by Cdc42, involved in regulating cell migration, proliferation, and survival. It influences signaling pathways like RAS and NF-kB, and plays a key role in cytoskeletal remodeling and cell adhesion. Overexpression of ACK1 is linked to cancer metastasis, making it a potential therapeutic target for cancer treatment.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsACK1

Vemurafenib

T2382918504-65-1

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

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Cited

AIM-100

T5092873305-35-2

AIM-100 is a Ack1 inhibitor (IC50: 24 nM).

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AZ7550

T135641421373-99-0

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

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GNF-7

T3196839706-07-9

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

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KRCA-0008

T26411472795-20-2

KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.

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Ack1 inhibitor 1

T855832924415-92-7

Ack1 inhibitor 1 is a potent and selective orally active inhibitor of ACK1 kinase, with an IC50 value of 2.1 nM. It effectively inhibits the phosphorylation of ACK1 and the activation of downstream AKT, demonstrating anti-tumor activity [1].

$1,970

10-14 weeks

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(R)-9b

T2017761655527-68-6

(R)-9b is an effective inhibitor of the ACK1 tyrosine kinase (IC50=56 nM) and exhibits anticancer activity. It selectively targets ACK1 but also inhibits kinases in the JAK family, specifically JAK2 and Tyk2. (R)-9b is used in research related to hormone-regulated cancers, such as prostate cancer and breast cancer.