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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
pseudokinase
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "pseudokinase" in MCE Product Catalog:
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25 Cited Publications
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GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis .
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25 Cited Publications
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GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis .
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NR162 is a selective CASK (Ca 2+/calmodulin-dependent Ser/Thr kinase) inhibitor with an IC50 of 80 nM and a Kd of 22 nM. NR162 shows about 50-fold selectivity for CASK than TYRO3. NR162 targets the unique GFG motif of CASK and has excellent shape complementarity to the CASK ATP binding pocket. NR162 can be used for the research of neurological diseases .
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BRD0418 is a diversity-oriented synthesis (DOS) molecule that regulates the expression of tribbles pseudokinase 1. BRD0418 has the effect of causing hot lipoprotein metabolism from fat production to clearance. BRD0418 can be used in the study of coronary artery disease (CAD) .
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QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC50=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC50=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) .
Cat. No.: HY-148366
Purity: 98.99%
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NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
Cat. No.: HY-E70873
TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). Tyk2(JH1/JH2) Recombinant Human Active Protein Kinase is a recombinant Tyk2(JH1/JH2) protein that can be used to study Tyk2(JH1/JH2)-related functions .
Cat. No.: HY-18709
CAS No.: 1779493-12-7
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Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
Cat. No.: HY-18710
CAS No.: 914946-88-6
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BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
Cat. No.: HY-169072
CAS No.: 3103327-20-1
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PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research .
Cat. No.: HY-178464
CAS No.: 3065634-19-4
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RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS) .
Cat. No.: HY-E70872
TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). TYK2(JH1) Recombinant Human Active Protein Kinase is a recombinant TYK2(JH1) protein that can be used to study TYK2(JH1)-related functions .
Cat. No.: HY-E70874
TYK2 is a member of the JAK family of non-receptor tyrosine kinases that act together with signal transducer and activator of transcription (STAT) factors in mediating intracellular signal transduction. JAKs are characterized by dual kinase domain: a tyrosine kinase domain (JH1) that is preceded by a pseudokinase domain (JH2). TYK2(JH2) Recombinant Human Active Protein Kinase is a recombinant TYK2(JH2) protein that can be used to study TYK2(JH2)-related functions .
Cat. No.: HY-112783
CAS No.: 1258295-27-0
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TYK2 ligand 4 (Compound 2) is a TYK2 ligand. TYK2 ligand 4 binds to both the kinase domain and pseudokinase domain, and induces an inactive conformation of the kinase domain, thereby preventing ATP binding. TYK2 ligand 4 serves as a tool compound for the development of Deucravacitinib (HY-117287) .
Cat. No.: HY-182344
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MLKL ligand-2 is a mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC ligand with a KD of 9.408 μM. MLKL ligand-2 forms hydrogen bond networks and hydrophobic interactions with specific MLKL residues, and stabilizes MLKL in hepatic cells. MLKL ligand-2 can be used to synthesize PROTAC MLKL Degrader-3 (HY-182343) .
Cat. No.: HY-P701725
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: VRK3; Inactive serine/threonine-protein kinase VRK3; Serine/threonine-protein pseudokinase VRK3; Vaccinia-related kinase 3
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Cat. No.: HY-E70835
Janus kinase 2 (JAK2) initiates signaling from several cytokine receptors and is required for biological responses such as erythropoiesis. JAK2 contains the kinase (JH1) and pseudokinase domains (JH2). JAK2(JH1/JH2) Recombinant Human Active Protein Kinase is a recombinant JAK2(JH1/JH2) protein that can be used to study JAK2(JH1/JH2)-related functions .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
