An orally bioavailable

URMC-099 – 5 mg

Brand:
Cayman
CAS:
1229582-33-5
Storage:
-20
UN-No:
Non-Hazardous - /

URMC-099 is an orally bioavailable, brain-penetrant inhibitor of mixed-lineage kinases (MLKs) with IC50 values of 19, 42, 14, and 150 nM for MLK1, MLK2, MLK3, and the related MLK family member DLK, respectively.{19147} It also inhibits LRRK2 activity with an IC50 value of 11 nM.{19147} In vitro, URMC-099 has been shown to reduce inflammatory cytokine production by HIV-1 Tat-exposed microglia and to prevent destruction and phagocytosis of cultured neuronal axons by these cells.{31033} In rodent models of HIV-associated neurocognitive disorders, URMC-099 demonstrates anti-inflammatory and neuroprotective effects.{31033}  

 

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Description

An orally bioavailable, brain-penetrant inhibitor of MLKs (IC50s = 19, 42, 14, and 150 nM for MLK1, MLK2, MLK3, and the related MLK family member DLK, respectively); also inhibits LRRK2 activity (IC50 = 11 nM); demonstrates anti-inflammatory and neuroprotective effects both in vitro and in vivo

Formal name: 3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine

Synonyms: 

Molecular weight: 421.5

CAS: 1229582-33-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling||Research Area|Immunology & Inflammation|Innate Immunity|Phagocytosis||Research Area|Infectious Disease|Viral Diseases|HIV & AIDS||Research Area|Neuroscience

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