URMC-099

Catalog No.S7343

For research use only.

URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.

URMC-099 Chemical Structure

CAS No. 1229582-33-5

Selleck's URMC-099 has been cited by 9 Publications

Purity & Quality Control

Choose Selective Mixed Lineage Kinase Inhibitors

Biological Activity

Description URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Targets
Abl1 [1]
(Cell-free assay)
LRRK2 [1]
(Cell-free assay)
MLK3 [1]
(Cell-free assay)
MLK1 [1]
(Cell-free assay)
VEGFR1/FLT1 [1]
(Cell-free assay)
Click to View More Targets
6.5 nM 11 nM 14 nM 19 nM 39 nM
In vitro

URMC-099 inhibits LPS-induced TNFα release in microglial cells, and HIV-1 Tat-induced release of cytokines in human monocytes. [1] URMC-099 prevents destruction and phagocytosis of cultured neuronal axons by microglia cells. [2] URMC-099 reduces fMLP-induced chemotaxis of wild-type neutrophil in vitro. [3]

Assay
Methods Test Index PMID
Immunofluorescence LC3B 28134625
In vivo In mice, URMC-099 shows excellent pharmacokinetic properties and improved CNS penetration. [1] In vivo, URMC-099 (10 mg/kg i.p.) reduces inflammatory cytokine production, protects neuronal architecture, and alters the morphologic and ultrastructural response of microglia to HIV-1 Tat exposure. [2] URMC099 significantly reduces recruitment of neutrophils into the peritoneum by fMLP in wild-type mice. [3]

Protocol (from reference)

Animal Research:[2]
  • Animal Models: Mice exposed to HIV-1 Tat
  • Dosages: 10 mg/kg twice a day
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 421.54
Formula

C27H27N5

CAS No. 1229582-33-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC=C4C5=CC6=C(C=C5)NC=C6)N=C3

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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