Fyn
Fyn is a Src family tyrosine kinase represented in brain by the neuronal isoform p59FynB, where Src and Fyn constitute the two main tyrosine kinases involved in neuronal growth and myelination[1]. Mechanistically, Fyn participates in Src-family signaling modules that regulate inflammation, apoptosis, neuroinflammation, and epileptogenesis in experimental systems[2][3]. In pulmonary endothelial inflammation models, fyn knockdown increased caspase-3 activity, reduced viable cell numbers, and intensified LPS-induced lung injury in fyn−/− mice, identifying Fyn as a negative regulator of inflammation-induced apoptosis[2]. In temporal lobe epilepsy models, the Fyn-PKCδ pathway linked status epilepticus to neuroinflammation and epileptogenesis, while saracatinib reduced seizures, gliosis, neurodegeneration, phosphorylated Fyn/Src-419, PKCδ-tyr311, nitrooxidative stress, and proinflammatory cytokines[3]. Compared with related isoforms, Fyn showed an opposite endothelial apoptosis phenotype to Yes, because yes knockdown lowered caspase-3 activity and increased viable cells under cytomix stimulation[2]. For experimental applications, saracatinib functions as a Src/Fyn tyrosine kinase inhibitor for probing epileptogenesis-associated neuroinflammatory and nitrooxidative pathways[3].
References:
- [1]. Rouer E. Les isoformes neuronales des tyrosines kinases Src, et al. Les isoformes neuronales des tyrosines kinases Src, Fyn et Lck : rôle particulier de la p56lckN dans la survie neuronale [Neuronal isoforms of Src, Fyn and Lck tyrosine kinases: A specific role for p56lckN in neuron protection]. C R Biol. 2010 Jan;333(1):1-10. French. [Content Brief]
- [2]. Jin Y, et al. The Src family tyrosine kinase, fyn, is a negative regulator of inflammation-induced apoptosis in the lung. FASEB J. 2014;28(1 Suppl):1176.6.
- [3]. Sharma S, et al. Mechanisms of disease-modifying effect of saracatinib (AZD0530), a Src/Fyn tyrosine kinase inhibitor, in the rat kainate model of temporal lobe epilepsy. Neurobiol Dis. 2021 Aug;156:105410. [Content Brief]
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Fyn 관련 제품 (11)
관련 제품 (11)
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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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Papaveroline hydrochloride
0 ImagesPapaveroline hydrochloride is an orally active Fyn tyrosine kinase inhibitor. Papaveroline hydrochloride stably binds to the active site of Fyn tyrosine kinase via hydrogen bonding and hydrophobic interactions, thereby inhibiting kinase activity associated with the pathogenesis of Alzheimer's disease. Papaveroline hydrochloride can be used for the research of Alzheimer's disease.
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ARN25699
0 ImagesCat. No.: HY-183584ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies.
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c-Met-IN-32
0 ImagesCat. No.: HY-189651c-Met-IN-32 is an orally active c-Met inhibitor with an IC50 of 18 nM, blocking autophosphorylation and downstream PI3K/AKT and RAS/ERK signaling pathways. c-Met-IN-32 inhibits MER, FYN, and SRC kinases. c-Met-IN-32 induces apoptosis, inhibits migration and invasion, suppresses the proliferation of MET-amplified cancer cells, and exhibits selectivity against non-MET-dependent cancer cell lines. c-Met-IN-32 can be used for research on non-small cell lung cancer.
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Fyn-IN-1
0 ImagesCat. No.: HY-180938CAS No.: 3107638-80-9
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Antifibrotic agent 1
0 ImagesCat. No.: 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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WAY-637493
0 ImagesCat. No.: HY-169640CAS No.: 791600-64-1
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BMS-243117
0 ImagesCat. No.: HY-120622CAS No.: 225521-80-2
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ON012380
0 ImagesCat. No.: HY-10365CAS No.: 592543-24-3ON012380 is a kinase inhibitor with an IC50 of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia.
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