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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
267 Results for "
kinase domains
" in MedChemExpress (MCE) Product Catalog:
Products (267)
267 Results for "kinase domains" in MCE Product Catalog:
1221
1221 Publications Verification
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator .
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114 Cited Publications
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GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury .
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114 Cited Publications
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GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury .
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Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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100 Cited Publications
Cat. No.: HY-50898A
CAS No.: 388082-77-7
Synonyms: GW572016 ditosylate; GW2016 ditosylate
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Lapatinib ditosylate (GW572016 ditosylate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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100 Cited Publications
Cat. No.: HY-50898B
CAS No.: 388082-78-8
Synonyms: GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
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Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
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Quinones Labiatae Terpenoids Samanea saman (Jacq.) Merr. Diterpenoids Plants Disease Research Fields Naphthalene Quinones Cancer
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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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23 Cited Publications
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NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM .
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Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .
9
5,6-Dichlorobenzimidazole riboside (DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain kinases, including casein kinase II and cell cycle-dependent kinases (CDK). 5, 6-dichlorobenzimidazole riboside has antitumor activity. 5, 6-dichlorobenzimidazole riboside can induce apoptosis .
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9 Cited Publications
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BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC) . BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM .
8
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GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. GSK-843 can be used for the research of inflammation .
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7 Cited Publications
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DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC) .
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BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
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4 Cited Publications
Cat. No.: HY-18937
CAS No.: 1354825-58-3
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WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation .
4
4 Cited Publications
Cat. No.: HY-52101A
CAS No.: 821794-92-7
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FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
4
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
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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
