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Organic compounds in which a hydrogen atom or more has been replaced by a halogen atom in an alkane molecule (saturated hydrocarbon chain). Halogen atoms include bromine, chlorine, fluorine, and iodine. Compounds may be in closed ring configurations.
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X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). It is a less potent inhibitor of MET (IC50=0.69 nM) and displays potent anti-tumor activity.
Potent and highly specific ALK tyrosine kinase inhibitor
Less potent inhibitor of MET
Displays potent anti-tumor activity
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GluN1 (356-385) is an antigenic peptide against N-methyl-D-aspartate receptor (NMDAR) encephalitis. It reduces the density of surface NMDAR clusters in hippocampal neurons and can be used to study the pathogenesis of anti-NMDAR encephalitis.
Antigenic peptide against N-methyl-D-aspartate receptor encephalitis
Reduces density of surface NMDAR clusters
Suitable for studying anti-NMDAR encephalitis pathogenesis
Inhibitor of ionotropic glutamate receptors
Active immunization agent
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GluN1 (356-385) is an antigenic peptide against N-methyl-D-aspartate receptor (NMDAR) encephalitis. It reduces the density of surface NMDAR clusters in hippocampal neurons and can be used to study the pathogenesis of anti-NMDAR encephalitis.
Antigenic peptide against NMDAR encephalitis
Reduces density of surface NMDAR clusters in hippocampal neurons
Used to study pathogenesis of anti-NMDAR encephalitis
Related to peptide and derivatives, and peptide epitopes
Applicable to neurological, eye or ear disease
Associated with membrane transporter/ion channel, neuronal signaling, and iGluR pathways
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BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. It is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
Orally bioavailable.
Highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE).
IC50 of 20 nM for HNE.
Nominated as a chemical probe via the Structural Genomics Consortium (SGC).
Ki value for MNE is 700 nM.
4th generation inhibitor of HNE.
More than 2,000-fold selectivity in a panel of 21 serine proteases.
Reveals significant efficacy in preclinical models of ALI and lung emphysema, demonstrating anti-inflammatory and anti-remodeling mode of action.
Shown significant beneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice.
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A perfluoroalkyl substance; chronic topical administration on the EAr increases liver and kidney weight in mice at 25 µl of a 3.75-15% v/v on the EAr; induces multifocal hepatocyte necrosis and centrilobular hepatocyte hypertrophy at 7.5% v/v; increases serum cholesterol and ALP levels at 15% v/v; decreases serum urea nitrogen levels; has been found in marine life and as a contaminant in surface water
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X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) with an IC50 of 0.61 nM. It is also a less potent inhibitor of MET (IC50=0.69 nM) and exhibits potent anti-tumor activity.
Effective in inhibiting the growth of various cancer cell lines, including H3122 lung cancer cells (IC50: 77 nM), H2228 lung cancer cells (IC50: 57 nM), and SUDHL-1 lymphoma cells (IC50: 32 nM).
Also inhibits SY5Y neuroblastoma cells, MKN-45 gastric carcinoma cells, HepG2 cells, and PC-9 lung cancer cell lines.
Demonstrates substantial bioavailability and moderate half-lives in vivo.
Significantly delays tumor growth in H3122 xenografts at a dose of 50 mg/kg bid, appearing well-tolerated without affecting mouse weight or causing compound-related toxicity.
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Also available in 1 mg 2 mg 5 mg 25 mg 50 mg 100 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration X-396 binds to and inhibits ALK kinase ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. purity: 98%
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