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MEKK (MAP3K)

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Cat. No. Product Name Field of Application Chemical Structure
DC11622 MAP3K14-IN-173 A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation).
DC11610 AKS1-IN-19 A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3.
DC11558 DLK-IN-14 A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM.
DC10781 ASK1-IN-1 Featured ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.
DC9555 Cot inhibitor-2 Cot inhibitor-2 is a COT/Tpl2 inhibitor.
DC10106 GNE-3511 Featured GNE-3511 is a potent and selective zipper kinase (DLK, MAP3K12) inhibitors.
DC8787 NQDI-1 Featured NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.
DC11036 TCASK10 TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM, 30-fold selectivity over ASK2 (IC50=510 nM) and no activity against MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf.
DC9873 Selonsertib(GS-4997) Featured Selonsertib(GS-4997)is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.
DC44947 SM1-71 SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.
DC47890 TAK1-IN-3 TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
DC70429 GDC-0134 GDC-0134 (GDC0134) is a potent, selective, orally available, brain-penetrant inhibitor of dual leucine zipper kinase (DLK, MAP3K12).GDC‐0134 blocks DLK activity in cellular assays and in animal models of neuronal injury.Dual leucine zipper kinase (DLK), which regulates the c‐Jun N‐terminal kinase pathway involved in axon degeneration and apoptosis following neuronal injury, is a potential therapeutic target in amyotrophic lateral sclerosis (ALS).
DC72783 DDO3711 DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.
DC74342 IACS-52825 IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.
DC74343 IKAM-1 IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.
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