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Cat. No. Product Name CAS No. Information
PC-70174

CEP-1347

156177-65-0

CEP-1347 (KT-7515) is a potent and selective MLK inhibitor that completely rescues motoneurons and inhibits JNK1 activation with IC50 of 20 nM; has weak inhibitory activity for Trk A and MLCK; promotes motoneuron survival and simultaneously inhibits the JNK1 signaling cascade; inhibits recombinant MLK1/2/3 with IC50 of 23-51 nM; blocks cell death (overexpression of MLK3) in CHO cells; elicits neuroprotective and anti-inflammatory responses in models of neurodegenerative diseases.

Parkinson Disease

Phase 2 Discontinued

PC-43118

URMC-099

1229582-33-5 URMC-099 is a potent, orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3 (MLK3) with IC50 of 14 nM; shows >90% inhibition against 111 kinases in a panel of 442 kinases at 1 uM; URMC-099 likely functions in HIV-1 associated neurocognitive disorders (HAND) preclinical models by inhibiting multiple kinase pathways, including MLK3 and LRRK2 (IC50=11 nM); inhibits LPS-induced TNFα release in microglial cells, HIV-1 Tat-induced release of cytokines in human monocytes and up-regulation of phospho-JNK in Tat-injected brains of mice.
PC-70325

GW 806742X

579515-63-2 A small molecule MLKL (Mixed Lineage Kinase Domain-Like) interactor that binds the MLKL pseudokinase domain (Kd=9.3 uM), retards membrane association to inhibit necroptosis; rescues 50% of wild-type MDFs from TSQ-induced necroptosis with IC50 <50 nM, with >50-fold greater potency than Nec-1; enhances RIPK3-mediated phosphorylation of MLKL (S345 and S347) at 10 uM.
PC-70175

M-443

1820684-31-8 A specific, irreversible inhibitor of MLK-related kinase MRK (ZAK), does not inhibit Bcr-Abl; effectively inhibits MRK downstream signals in primary medulloblastoma cells and prevents cell-cycle arrest induced by IR; also inhibits radiation-induced activation of both p38 and Chk2; achieves a synergistic increase in survival in an animal model of medulloblastoma.
PC-42202

Necrosulfonamide

1360614-48-7 A small molecule covalent inhibitor of mixed lineage kinase domain like protein (MLKL) that specifically blocks necrosis downstream of RIP3 activation; binds within the N-terminal 178 residues of human MLKL; arrests necrosis at a specific step at which RIP3 formed discrete punctae in cells.

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