URMC-099

Catalog No.S7343

URMC-099 Chemical Structure

Molecular Weight(MW): 421.54

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.

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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.
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)
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]

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

Animal Research:[2]
+ Expand
  • Animal Models: Mice exposed to HIV-1 Tat
  • Formulation: Saline
  • Dosages: 10 mg/kg twice a day
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.26 mM)
Ethanol 6 mg/mL (14.23 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 421.54
Formula

C27H27N5

CAS No. 1229582-33-5
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID