Lck
Lck (lymphocyte-specific protein tyrosine kinase) is a Src-family non-receptor tyrosine kinase that functions as a central initiator of T-cell activation and antigen receptor signaling through phosphorylation-dependent intracellular signal transduction mechanisms[1][2]. Mechanistically, Lck operates at the proximal stage of the T-cell receptor (TCR) signaling pathway, where it phosphorylates immunoreceptor tyrosine-based activation motifs (ITAMs) and promotes downstream signaling events required for T-cell activation, differentiation, and immune responses[2][3]. Genetic studies demonstrated that loss of functional Lck disrupts TCR-mediated signaling and impairs cellular responsiveness, establishing its essential role in lymphocyte biology and experimental models of immune deficiency[4]. Disease relevance is supported by evidence linking LCK deficiency to severe immunological dysfunction, while dysregulated Lck signaling has also been investigated in hematologic malignancies and other immune-associated disorders[1][4]. Compared with related Src-family kinases, particularly Fyn, Lck has a more dominant role in initiating proximal TCR signaling, whereas Fyn contributes to overlapping but nonessential signaling functions in many T-cell activation contexts[3][5]. Structurally, Lck contains SH2, SH3, and catalytic kinase domains that coordinate activation-state regulation through phosphorylation-dependent conformational changes[2]. For experimental applications, Lck remains a widely used target for kinase inhibition studies and mechanistic analyses of T-cell signaling networks, making it a valuable tool for immune signaling research and therapeutic target validation[6].
References:
- [1]. Uniprotkb.
- [2]. Rossy J, et al. How does the kinase Lck phosphorylate the T cell receptor? Spatial organization as a regulatory mechanism. Front Immunol. 2012 Jun 19;3:167. [Content Brief]
- [3]. Lck gene information from NCBI.
- [4]. Straus DB, et al. Genetic evidence for the involvement of the lck tyrosine kinase in signal transduction through the T cell antigen receptor. Cell. 1992 Aug 21;70(4):585-93. [Content Brief]
- [5]. Wikipedia.
- [6]. Elkamhawy A, et al. New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights. J Enzyme Inhib Med Chem. 2021 Dec;36(1):1574-1602. [Content Brief]
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Lck Related Products (25)
Related Products (25)
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Antibodies (1)
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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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Velzatinib
0 ImagesSynonyms: M4205; IDRX-42
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PRT062607 Hydrochloride
0 ImagesSynonyms: P505-15 Hydrochloride
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AZM475271
0 ImagesSynonyms: M475271AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026).
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N-Deshydroxyethyl Dasatinib
0 ImagesCat. No.: HY-107447CAS No.: 910297-51-7Synonyms: N-Deshydroxyethyl BMS-354825N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
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Lck-IN-6
0 ImagesCat. No.: HY-112448CAS No.: 918870-43-6
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WH-4-023 (GMP)
0 ImagesCat. No.: HY-12299GCAS No.: 837422-57-8Synonyms: Dual LCK/SRC inhibitor (GMP)WH-4-023 GMP is WH-4-023 (HY-12299) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. WH-4-023 (Dual LCK/SRC inhibitor) is a Lck/Src dual target inhibitor with functions in stem cell maintenance and differentiation regulation. WH-4-023 blocks epithelial-mesenchymal transition, supports the self-renewal of porcine embryonic stem cells, and inhibits their differentiation into mesoderm and endoderm. WH-4-023 is a key component of 3i/LAF medium, and enables the stable establishment and long-term maintenance of porcine pre-gastrulation epiblast stem cell lines. Removal of WH-4-023 reduces the expression of pluripotency factors in porcine and human extended pluripotent stem cells. WH-4-023 can be applied to relevant studies such as non-small cell lung cancer resistant to EGFR-TKIs.
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SB 220025
0 ImagesSB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
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PRT062607 acetate
0 ImagesSynonyms: P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
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Lck-IN-5
0 ImagesLck-IN-5 (example C10) is a potent and selective lymphocyte-specific protein tyrosine kinase (LCK) inhibitor. Lck-IN-5 selectively disrupts the interaction between the SH3 domain of LCK and the RK motif of CD3ε, thereby impairing LCK recruitment to the TCR. Lck-IN-5 modulates the activity of CD3ε-containing CAR and TRuC T cells, attenuating cytokine production and promoting a central-memory-like phenotype associated with enhanced persistence. Lck-IN-5 can be used for autoimmune diseases and graft-versus-host disease research.
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BMS-279700
0 ImagesCat. No.: HY-114980CAS No.: 240814-54-4BMS-279700 is an orally active Src-family kinase p56Lck inhibitor. BMS-279700 can block the production of proinflammatory cytokines (IL-2 and TNFα). BMS-279700 can inhibit T cell proliferation. BMS-279700 can be used for the researches of inflammation and immunology.
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SJ11646
0 ImagesCat. No.: HY-175281CAS No.: 2933135-82-9SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
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Lck-IN-2
0 ImagesCat. No.: HY-163278CAS No.: 2615173-24-3Lck-IN-2 (compound 12a) is an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck) with IC50 of 10.6 nM. Lck-IN-2 reveals efficacy in colon cancer cells with GI50s of 0.24-1.26 μM. Lck-IN-2 exhibits an apoptotic effect in Colo201 cells.
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