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Cat. No. Product Name CAS No. Information
PC-60092

DLK-IN-14

1620574-24-4

A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM; displays no significant inhibitory activity against a panel of 220 kinases (<70% inhibition at 1 uM); reduces JNK phosphorylation (p-JNK) in HEK293 cells with IC50 of 0.195 uM, reduces p-MKK4 and p-JNK in models of chronic neurodegeneration.

PC-45794

Tpl2-IN-34

915363-56-3

A potent, selective Tpl2 (cot/MAP3K8) inhibitor with IC50 of 1.6 nM; dispalys 6875-fold selectivity over EGFR. P38, Src, CAMKII, MK2, PKA, and PKC (IC50>10 uM); inhibits LPS-induced TNF-α production in whole blood with IC50 of 0.3 uM; shows good efficacy in inhibiting TNF-alpha production in a LPS-stimulated rat inflammation model; orally active.

PC-45565

Selonsertib

1448428-04-3

Selonsertib (GS-4997) is a highly selective and potent, ATP-competetive inhibitor of ASK1 (Apoptosis Signal-regulating Kinase 1, MAP3K5) with potential anti-inflammatory, antineoplastic and anti-fibrotic activities; orally bioavailable.

Steatohepatitis

Phase 3 Clinical

PC-35427

GS-444217

1262041-49-5 GS-444217 (GS444217) is a potent, selective, ATP-competitive, orally available inhibitor of ASK1 with Kd/IC50 of 4.1/2.87 nM; displays >53-fold selectivity over DYRK1A and 104-fold over RSK4 in a panel of 442 kinases; strongly suppresses the activation of ASK1, p38, and JNK in the kidney resulting in decreased death of parenchymal cells, inflammation, and fibrosis;abrogates p38 MAPK activation in diabetic kidneys but has no effect upon hypertension in Nos3(-/-) mice; dose dependently reduced pulmonary arterial pressure and reduced RV hypertrophy in pulmonary arterial hypertension (PAH) models; also reduces the progressive inflammation and fibrosis in the kidney and halted decline of glomerular filtration rate in models of kidney disease, causes regression of fibrosis combined with RAS inhibitor enalapril.
PC-35394

TCASK10

1005775-56-3 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; blocks downstream JNK1/p38 phosphorylation in cells, dose-dependently reduces mitogen (FBS, PDGF and EGF)-induced airway smooth muscle (ASM) growth, also prevents TGFb1-induced migration of ASM cells in vitro.
PC-43286

GNE-3511

1496581-76-0 GNE-3511 is a potent, selective, orally bioavailable, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of <0.5 nM, displays >100-fold selectivity over MKK4/7, JNK1/2/3, MLK1/2/3; inhibits p-JNK with IC50 of 30 nM, displays concentration-dependent protection of neurons from degeneration in vitro (DRG IC50=107 nM) and demonstrates dose-dependent activity in multiple animal models of neurodegenerative disease.
PC-62818

TAOK inhibitor 63

850467-91-3 TAOK inhibitor 63 is a novel potent, selective, ATP-competitive TAO Kinase (TAOK) inhibitor with IC50 of 19 and 39 nM against TAOK1 (MAP3K16) and TAOK2 (MAP3K17), respectively; increases the mitotic population, the percentages of mitotic cells displaying amplified centrosomes and multipolar spindles, induces cell death, and inhibits cell growth in centrosome-amplified SKBR3 or BT549 breast cancer cell models.

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