MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, provide specificity for stimulus-dependent activation of MAP2K-MAPK pathways through unique protein-protein interactions and phosphorylation of signaling effectors.TAK1, ASK1, A-Raf, and C-Raf are MAP3Ks with highly divergent gene numbers and structures.
A three-step sequential phosphorylation cascade made up of MAPK, MAP2K, and MAP3K is known as the MAPK system. The MAPK family includes the proteins ERK, p38 MAPK, and JNK, all of which are known to be activated by mechanical stimuli. The activation of multiple MAP3Ks provides the spatiotemporal regulation of the MAPK pathways, which induces a wide range of physiological responses necessary for determining cell fate, such as cytokine production, survival, differentiation, and apoptosis. MAP3Ks serve as "platforms to integrate MAPK signaling."
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V3102 | ASK1-IN-1 | 1262041-49-5 | ASK1-IN-1 is a potent inhibitor of the apoptosis signal regulating kinase 1 (ASK1) inhibitor (Compound 4 from patent WO2016025474A1). |
|
V87074 | ASK1-IN-6 | 2407451-82-3 | ASK1-IN-6 (Compound 32) is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with IC50 of 25 nM. |
|
V74395 | AZ-TAK1 | 1413440-36-4 | AZ-TAK1 is an ATP-competitive, small molecule inhibitor of TAK1 that dephosphorylates TAK1, p38, and IκB-α in lymphoma cells. |
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V87076 | CS17919 | 2379346-41-3 | CS17919 is a potent, selective and orally active ASK1 inhibitor with IC50 of 22.52 nM. |
|
V51189 | DDO-3711 | 2673364-10-6 | PP5-recruiting phosphatase recruitment chimeras (PHORCs) |
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V74397 | IACS-52825 | 2640376-72-1 | IACS-52825 is a potent and specific DLK inhibitor (antagonist) with a Kd of 1.3 nM that may be utilized to study chemotherapy-induced peripheral neuropathy. |
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V83375 | JT21-25 | 2996864-57-2 | |
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V35537 | SM1-71 | 2088179-99-9 | SM1-71 is a potent TAK1 inhibitor (antagonist) with a Ki of 160 nM and 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. |
|
V74396 | SW083688 | 422281-45-6 | SW083688 is a potent and selective TAOK2 (Thousand-And-One Kinase 2) inhibitor (IC50 = 1.3 umol/L). |
|
V74399 | TAK1-IN-2 | 2763213-98-3 | TAK1-IN-2 is a potent and specific TAK1 inhibitor (antagonist) with IC50> value of 2 nM. |
|
V74398 | TAK1-IN-3 | 494772-87-1 | TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor. |
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V87075 | TAK1-IN-5 | TAK1-IN-5 (Compound 26) is a transforming growth factor-β activated kinase (TAK1) inhibitor with an IC50 of 55 nM. | |
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V2973 | Selonsertib | 1448428-04-3 | Selonsertib (Also known as GS-4997) is a highly selective and potent once-daily orally available inhibitor of ASK1 (apoptosis signal-regulating kinase 1) with a pIC50 of 8.3±0.07. |
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