URMC-099, MLK3 inhibitor (TBI4012)

Description

Product Details

Formal Name: 3-(1H-Indol-5-yl)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridine

Molecular Formula: C₂₇H₂₇N₅

Formula Weight: 421.50

CAS Number: 1229582-33-5

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

MLK3 inhibitor

Functions

URMC-099 is a potent (IC50 = 14 nM), brain penetrant mixed-lineage kinase 3 inhibitor (MLK3). It also potently inhibits FLT3 (4 nM in vitro, but 560 nM in vivo), LRRK2 (11 nM), and ABL1 (3 nM). URMC-099 displayed neuroprotective effects in HIV-associated neurocognitive disorders and facilitated microglial amyloid-β degradation and clearance in mouse models. URMC-099 increased CD8+ T cells in mice and increased the CD8+GZMB+ T cell population in blood mononuclear cells isolated from breast cancer patients.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.