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Activated Cdc42-associated tyrosine kinase 1 (ACK1; also known as TNK2, tyrosine kinase non-receptor 2) 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 has been shown to interact with AKT, Androgen receptor or AR, tumor suppressor WWOX, FYN and Grb2. ACK1 has been shown to be critical for progression of PC to hormone therapy insensitive stage called castration resistant prostate cancer or CRPC due to it’s ability to regulate the expression and function of AR in androgen-independent manner.

The ACK1 inhibitor (R)-9bMS sensitized naive and enzalutamide-resistant prostate cancer cells and reduced AR and AR-V7 levels to mitigate CRPC tumor growth.

References:

1.Thaker YR, et al. J Biol Chem. 2017 Apr 14;292(15):6281-6290.

2. Mahajan K, et al. Cancer Cell. 2017 Jun 12;31(6):790-803.e8.

3. Wu X, et al. Oncotarget. 2017 Jan 10;8(2):2971-2983.

4. Jiao X, et al. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6212-7.

 

Cat. No. Product Name CAS No. Information
PC-35146

XMD8-87

1234480-46-6 XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM.
PC-70152

(R)-9b

1655527-68-6 Ack1 inhibitor (R)-9b is a potent and selective ACK1 (TNK2) inhibitor with IC50 of 48 nM.
PC-70151

(R)-9bMS

N/A (R)-9bMS is a potent and selective ACK1 (TNK2) inhibitor with IC50 of 48 nM.
PC-42339

XMD16-5

1345098-78-3 XMD16-5 is a potent Ack1 (TNK2) inhibitor with IC50 of 0.38 uM in ELISA assay.
PC-44307

AIM-100

873305-35-2 AIM-100 (AIM100) is a highly potent inhibitor of Ack1 (TNK2) (IC50=24 nM), selective for Ack1 over ABL1, BTK, Lck and LYN.
PC-35147

Ack1 inhibitor 37

1026493-77-5 Ack1 inhibitor 37 is a potent and selective Ack1 (TNK2) inhibitor with Ki of 0.3 nM, displays high selectivity over related kinases LCK, JAK3, KDR and TIE2 (Ki= 138, 6.5, 380 and 200 nM).

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