Lyn
Lyn is a Src-family tyrosine kinase that relays immune-cell receptor inputs to regulate proliferation, differentiation, apoptosis, migration, and metabolism[1]. Mechanistically, Lyn phosphorylates ITAM and ITIM signaling motifs, enabling both activating and inhibitory immunoreceptor signaling[1][2]. In B-cell biology, Lyn negatively regulates B-cell receptor signaling, and loss of Lyn in B cells leads to lupus-like autoimmunity in mouse models[3]. Compared with related Lyn isoforms, LynB shows a dominant immunosuppressive function in vivo, whereas LynA is uniquely required to restrain autoimmunity in female mice[4]. For experimental applications, bafetinib/NS-187 is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor used in imatinib-resistant leukemia research[5]. MLR-1023 is an allosteric Lyn kinase activator and insulin receptor potentiator used in glucose-homeostasis models[6].
参考文献:
- [1]. Ingley E. Functions of the Lyn tyrosine kinase in health and disease. Cell Commun Signal. 2012 Jul 17;10(1):21. doi: 10.1186/1478-811X-10-21. PMID: 22805580; PMCID: PMC3464935. et al. Functions of the Lyn tyrosine kinase in health and disease. Cell Commun Signal. 2012 Jul 17;10(1):21. [Content Brief]
- [2]. Xu Y, et al. Lyn tyrosine kinase: accentuating the positive and the negative. Immunity. 2005 Jan;22(1):9-18. [Content Brief]
- [3]. Lamagna C, et al. B cell-specific loss of Lyn kinase leads to autoimmunity. J Immunol. 2014 Feb 1;192(3):919-28. [Content Brief]
- [4]. Brian BF 4th, et al. A dominant function of LynB kinase in preventing autoimmunity. Sci Adv. 2022 Apr 22;8(16):eabj5227. [Content Brief]
- [5]. Kimura S, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood. 2005 Dec 1;106(12):3948-54. [Content Brief]
- [6]. Ochman AR, et al. The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes. J Pharmacol Exp Ther. 2012 Jul;342(1):23-32. [Content Brief]
All Product Categories
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Lyn 関連製品 (8)
関連製品 (8)
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GLPG3312
0 ImagesGLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
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SB1-G-187
0 ImagesSB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
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AP-24567
0 Images製品番号: HY-125142CAS 番号: 943319-87-7AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).
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Antifibrotic agent 1
0 Images製品番号: HY-176194Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model.
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SIK1-IN-1
0 Images製品番号: HY-178014SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN).
