Mixed lineage kinases (MLKs) control the c-Jun N-terminal kinase (JNK), mitogen activated protein kinase (MAPK), and extracellular signal-regulated kinase (ERK) signaling cascades. They are mitogen activated protein kinase kinases (MAPKKKs) with features of both serine-threonine and tyrosine kinases.
The most abundantly expressed member of the MLK family, MLK3 (MAP3K11), is found in neurons as well as other cell types. Stress, such as that caused by reactive oxygen species, ceramide, and TNF, activates MLK3 on a cellular level. It is triggered at the molecular level by Cdc42 and Rac, which engage MLK3 and can dimerize it via a leucine zipper interface, leading to autophosphorylation and enzyme activation.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2799 | GNE-3511 | 1496581-76-0 | GNE-3511 is a novel, highly potent and selective zipper kinase (e.g. DLK, MAP3K12) inhibitor with IC50 of 0.107 uM for DLK. |
|
V4944 | GW806742X | 579515-63-2 | GW806742X is a novel and potent inhibitor of Mixed Lineage Kinase Domain-Like protein (MLKL) which binds the MLKL pseudokinase domain with aKdvalue of 9.3 μM and has anti-necroptosis activity. |
|
V76946 | GW806742X hydrochloride | GW806742X HCl is an ATP mimetic and a potent MLKL inhibitor that binds to the MLKL pseudokinase domain with a Kd of 9.3 μM. | |
|
V74095 | MLK-IN-1 | 1627729-62-7 | MLK-IN-1 is a potent brain-penetrating specific MLK-3 inhibitor, compound 68 obtained from patent US20140256733A1. |
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V83497 | MLK-IN-2 | 2614255-51-3 | |
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V74098 | MLKL-IN-1 | 2837019-30-2 | MLKL-IN-1 is a covalent MLKL inhibitor (antagonist) with Kd of 50 μM. |
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V74097 | MLKL-IN-2 | 899759-16-1 | MLKL-IN-2 is an inhibitor (blocker/antagonist) of MLKL. |
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V80790 | MLKL-IN-3 | MLKL-IN-3 (compound 66) is a potent inhibitor of MLKL (mixed lineage kinase domain-like protein). | |
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V74099 | MLKL-IN-5 | 2755872-58-1 | MLKL-IN-5 is a potent MLKL inhibitor that mediates necroptosis. |
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V79876 | MLKL-IN-6 | MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). | |
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V87088 | MLKL-IN-7 | MLKL-IN-7 (compound 9) is a MLKL inhibitor, exhibits anti-necroptotic activity in HT-29 cells with IC50 value of 148.4 nM. | |
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V2915 | Necrosulfonamide | 1360614-48-7 | Necrosulfonamide is a potent and highly specific and potent necrosis inhibitor which blocks mixed lineage kinase domain-like protein (MLKL). |
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V34662 | Necrosulfonamide HCl | 432531-71-0 | NecrosulfonamideHCl is a potent andcell-permeable MLKL (mixed lineage kinase domain-like) inhibitor. |
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V74096 | Necrosulfonamide-d4 | 1795144-22-7 | Necrosulfonamide-d4 is the deuterated form of Necrosulfonamide. |
|
V15905 | TC13172 | 2093393-05-4 | TC13172 (TC-13172) is a mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor with single nanomolar potency. |
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