MAP3K
MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, modulate many biological processes, such as growth, development and various environmental stresses. Based on the sequence of their kinase catalytic domain, MAP3Ks are classified into three groups: the MEKK-like, ZIK-like and Raf-like families. Raf-like MAP3Ks constitute largest MAP3K subfamily. Raf-like MAP3Ks play roles in response to biotic and abiotic stresses.
MAP3Ks often bind to both MAP4Ks and MAP2Ks in the same pathway. For example, MEKK1 (MAP3K1) binds to both the MAP4K NIK and the MAP2K MKK4, while NSY-1 (MAP3K) binds to the MAP2K SEK-1. MAP3Ks activates MAP2Ks by phosphorylation of a serine and/or threonine, and MAP2Ks activate MAPKs by dual phosphorylation of a Thr-X-Tyr motif.
Targets for MAP3K
Products for MAP3K
- Cat.No. Product Name Information
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GC13944
(5Z)-7-Oxozeaenol
FR148083,L-783,279,LL-Z 1640-2
TAK1 mitogen-activated protein kinase kinase kinase (MAPKKK) inhibitor
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GC79474
(E/Z)-ASK1-IN-4
(E/Z)-ASK1-IN-4 is an isomer of ASK1-IN-4.
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GC19041
ASK1-IN-1
ASK1-IN-1 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.
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GC62426
ASK1-IN-2
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM.
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GC12151
B-Raf inhibitor
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GC43304
Compound 43 TAO Kinase Inhibitor
Compound 43 TAO kinase inhibitor is an ATP-competitive inhibitor of the thousand-and-one amino acid kinases TAOK1 and TAOK2 (IC50s = 11 and 15 nM, respectively).
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GC35734
Cot inhibitor-1
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM.
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GC35735
Cot inhibitor-2
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
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GC30913
DLK-IN-1
DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM.
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GC19173
GNE-3511
GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.
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GC70391
GNE-8505
GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
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GC13514
NG25
NG25 is a potent and cell-permeable inhibitor of transforming growth factor-β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), with IC50 values of 149nM and 21.7nM, respectively.
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GC17577
NQDI 1
A selective inhibitor of ASK1
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GC63144
PF-05381941
PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
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GC36898
Phosphocreatine
Phosphocreatine is a high-energy phosphate compound that is abundant in muscle and brain.
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GC12124
Selonsertib (GS-4997)
GS-4977, GS-4997
Selonsertib (GS-4997) (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
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GC62675
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.
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GC62497
TAK1-IN-2
TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.
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GC69984
TAK1-IN-4
TAK1-IN-4 (Compound 14) is a TAK1 inhibitor.
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GC32687
Takinib
EDHS-206
A TAK1 inhibitor
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GC79478
TAO Kinase-IN-3
TAO Kinase-IN-3 is a potent pan- TAOK ( Thousand-And-One Kinase ) inhibitor that specifically binds to and inhibits the kinase activities of TAOK1, TAOK2 and TAOK3 with K d values of <0.17 nM, 0.34 nM, and 0.17 nM, respectively.
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GC14853
TC ASK 10
ASK1 inhibitor
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GC45067
Tpl2 Kinase Inhibitor
c-Cot Kinase Inhibitor, MAP3K8 Kinase Inhibitor, Tumor Progression Locus 2 Kinase Inhibitor
Tpl2 Kinase Inhibitor (TKI) is a cell-permeable naphthyridine compound that acts as a potent reversible and ATP-competitive inhibitor of Tpl2 kinase.
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GC49150
Tpl2 Kinase Inhibitor (hydrochloride)
c-Cot Kinase Inhibitor, MAP3K8 Kinase Inhibitor, Tumor Progression Locus 2 Kinase Inhibitor
A Tpl2 inhibitor