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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
2510 Results for "
ERK1/2 substrate-docking domains
" in MedChemExpress (MCE) Product Catalog:
Products (2510)
2510 Results for "ERK1/2 substrate-docking domains" in MCE Product Catalog:
1199
1199 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 [1]. 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 .
407
407 Cited Publications
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PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy [1] .
334
334 Cited Publications
Cat. No.: HY-18749
CAS No.: 305834-79-1
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SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt [1] .
314
314 Cited Publications
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Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) [1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
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193
193 Cited Publications
Cat. No.: HY-50846
CAS No.: 942183-80-4
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SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naive and MAPK inhibitor-resistant cells containing BRAF or RAS mutations [1].
159
159 Cited Publications
Synonyms: PD0325901; PD325901
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts [1] .
143
143 Cited Publications
Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride
Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis [1] .
143
143 Cited Publications
Cat. No.: HY-50896
CAS No.: 183321-74-6
Synonyms: CP-358774; NSC 718781; OSI-774
Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions [1] .
111
111 Cited Publications
Cat. No.: HY-19696
CAS No.: 14605-22-2
Synonyms: Tauroursodeoxycholic acid; TUDCA; UR 906
Target:
110
110 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 [1] .
110
110 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 [1] .
98
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib can penetrate the blood brain barrier (BBB) [1] .
98
98 Cited Publications
Cat. No.: HY-50706A
CAS No.: 943332-08-9
Synonyms: AZD6244 sulfate; ARRY-142886 sulfate
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Selumetinib (AZD6244) sulfate is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) sulfate inhibits ERK1/2 phosphorylation. Selumetinib sulfate can penetrate the blood brain barrier (BBB) [1] .
95
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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 [1].
95
95 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 [1].
95
95 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 [1].
64
64 Cited Publications
Cat. No.: HY-18234A
CAS No.: 103476-89-7
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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
