dlk

DLK-IN-1 is a selective oral active inhibitor of bisleucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM. DLK-IN-1 is active in the Alzheimer's disease model, retains excellent CNS permeability, and after multiple days of administration, its concentration

DN-1289 is an orally available, blood-brain barrier-crossing, selective and potent inhibitor with an IC50 value of 17 nM for di-leucine zipper kinase (DLK) and 40 nM for leucine zipper-bearing kinase (LZK).DN-1289 significantly inhibited optic nerve crush (ONC)-induced p-c-Jun in a mouse model.

IACS-52825 is a selective and potent dual leucine zipper kinase (DLK) inhibitor that reverses para-mechanical aberrant pain in a CIPN mouse model for the study of neurological disorders.

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).

GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

GDC-0134, a dual leucine zipper kinase (DLK) inhibitor, exhibits brain penetration properties. It inhibits DLK to prevent neuronal degeneration and block JNK activation, potentially treating amyotrophic lateral sclerosis (ALS). It has been assessed in a phase 1 study aimed at treating ALS patients.

KAI-11101 is an inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. It effectively suppresses paclitaxel-induced cJun phosphorylation (IC50=95 nM), thereby inhibiting the activation of the MAPK pathway. KAI-11101 exhibits blood-brain barrier permeability, allowing for further exploration of its neuroprotective properties.