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Breast Tumor Kinase (BRK, also known as PTK6) is normally expressed in the differentiating epithelial cells of the intestine, skin, prostate, and oral cavity, where it has been shown to promote cellular differentiation, apoptosis, and more recently to mediate migration/wound healing. In tumors which over express Brk this Src-family, nonreceptor protein-tyrosine kinase has been implicated as a mediator of cancer cell phenotypes, including increased proliferation, survival, and migration. Potential Brk substrates include RNA-binding proteins: Sam68, SLM-1, SLM-2, and PSF; transcription factors: STAT3 and STAT5a/b; and a variety of signaling molecules: p190RhoGAP, paxillin, Akt, IRS-4, BKS/STAP-2, and KAP3A.

Studies have shown that Brk interacts with the ErbB family signaling pathway. Kamalati et al. demonstrated an interaction between Brk and the ErbB family member EGFR and over expression of Brk enhanced EGF-induced proliferation.

There are no or limited specific Brk/PTK6 inhibitors reported to date. Dasatinib, a Src/Abl multi-kinase inhibitor that is approved for chronic myelogenous leukemia (CML), is a potent PTK6/Brk (IC50=9 nM). XMU-MP-2 exhibited target-specific inhibition of BRK kinase activity and disrupted signaling pathways both in vitro and in vivo. BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM), exhibits potent cellular activity with p-SAM68 IC50 of 52 nM, downregulates SNAIL protein and restores E-cadherin expression in TNBC cells.

 

References:

1. Jiang J, et al. Cancer Res. 2017 Jan 1;77(1):175-186.

2. Ito K, et al. Cancer Res. 2016 Aug 1;76(15):4406-17.

3. Zeng H, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5.

4. Shen CH, et al. Cancer Res. 2008 Oct 1;68(19):7779-87.

 

Cat. No. Product Name CAS No. Information
PC-61652

XMU-MP-2

2031152-10-8

XMU-MP-2 is a potent and selective BRK/PTK6 (breast tumor kinase) inhibitor with biochemical IC50 of 3.2 nM; inhibits the autophosphorylation of BRK Y342 in dose-dependent manner (maximum inhibition at 500 nM), abolishes phosphorylation levels of STAT3 Y705 and STAT5 Y694; blocks proliferation and survival of BRK-transformed Ba/F3 cells with IC50 of 29.7 nM; cooperates strongly with HER2 inhibitor or ER blockade to block breast cancer cell proliferation in vitro and in vivo.

PC-35189

BRK inhibitor P21d

1338249-87-8 BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM); exhibits potent cellular activity with p-SAM68 IC50 of 52 nM, downregulates SNAIL protein and restores E-cadherin expression in TNBC cells; suppresses migration of MDA-MB-231 and MMTV-myc cells, sensitizes TNBC cells to anoikis and suppresses metastasis formation.
PC-35188

PF-6689840

1799790-53-6 PF-6689840 (PF6689840) is a potent and selective Type II PTK6/Brk inhibitor with IC50 of 54 nM in biochemical assays; inhibits PTK6 phosphorylation at Y342 in engineered HET293T cells overexpressing PTK6 WT with IC50 of 0.25 uM; demonstrates superior kinase selectivity compared to the Type I inhibitors; inhibits tumor cell growth, which is independent of PTK6 expression levels in cells.
PC-35187

PF-6683324

1799788-94-5 PF-6683324 (PF6683324) is a potent and selective Type II PTK6/Brk inhibitor with IC50 of 76 nM in biochemical assays; inhibits PTK6 phosphorylation at Y342 in engineered HET293T cells overexpressing PTK6 WT with IC50 of 0.7 uM; demonstrates superior kinase selectivity compared to the Type I inhibitors.

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