Breast Tumor Kinase
Breast cancer is divided into several clinical subtypes that includ ductal carcinoma in-situ (DCIS), infiltrating ductal carcinoma (IDC), lobular carcinoma in-situ (LCIS), infiltrating lobular carcinoma (LC), as well as into different stages from 0 to IV (based on tumor size and metastatic propensity). BRK (also pronounced “berk”) is a prototypical member of a family of non-receptor tyrosine kinases previously referred to as the FRK/PTK6 or PTK6 family kinases. The mammalian BFKs comprise three members namely, BRK or protein tyrosine kinase 6 (PTK6), FRK(PTK5) and SRMS (src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites or PTK70).
Like their Src family counterparts, members of the BRK family kinases are composed of the classic Src homology 3 (SH3), the Src homology 2 (SH2) and the kinase (SH1) domains. However, unlike Src family kinases (SFKs), the BFKs typically lack membrane-anchoring N-terminal myristoylation and palmitoylation signals, thereby rendering them soluble and potentially widening their accessibility to intracellular substrates. The BFKs are also evolutionarily distinct from SFKs by their unique exon organization. All three mammalian BFK members possess 8 exons interspersed between 7 introns in a conserved/identical manner. Src42a/Dsrc41, a tyrosine kinase belonging to the Drosophila melanogaster species, is the only other off-species relative known to exhibit significant intron-exon splice pattern similarity with the BFKs.
References
1.Goel RK, et al. Biochim Biophys Acta. 2015;1856(1):39–54.
Like their Src family counterparts, members of the BRK family kinases are composed of the classic Src homology 3 (SH3), the Src homology 2 (SH2) and the kinase (SH1) domains. However, unlike Src family kinases (SFKs), the BFKs typically lack membrane-anchoring N-terminal myristoylation and palmitoylation signals, thereby rendering them soluble and potentially widening their accessibility to intracellular substrates. The BFKs are also evolutionarily distinct from SFKs by their unique exon organization. All three mammalian BFK members possess 8 exons interspersed between 7 introns in a conserved/identical manner. Src42a/Dsrc41, a tyrosine kinase belonging to the Drosophila melanogaster species, is the only other off-species relative known to exhibit significant intron-exon splice pattern similarity with the BFKs.
References
1.Goel RK, et al. Biochim Biophys Acta. 2015;1856(1):39–54.
Tyrosine Kinase
Breast Tumor Kinase
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XMU-MP-2
产品货号 : M13159
cas no: 2031152-10-8
XMU-MP-2 是一种有效的选择性 BRK/PTK6(乳腺肿瘤激酶)抑制剂,生化 IC50 为 3.2 nM。 -
PF-6689840
产品货号 : M12729
cas no: 1799790-53-6
PF-6689840 (PF6689840) 是一种有效的选择性 II 型 PTK6/Brk 抑制剂,在生化测定中 IC50 为 54 nM。 -
PF-6683324
产品货号 : M12728
cas no: 1799788-94-5
PF-6683324 (PF6683324) 是一种有效的选择性 II 型 PTK6/Brk 抑制剂,在生化测定中 IC50 为 76 nM。 -
BRK inhibitor P21d
产品货号 : M11355
cas no: 1338249-87-8
BRK 抑制剂 P21d 是一种有效的、选择性的、细胞渗透性的乳腺肿瘤激酶 (Brk、PTK6) 抑制剂,IC50 为 30 nM。