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URMC-099 | MLK3 inhibitor

CAS:
1229582-33-5
Catalog Number:
10-4012
Activity:
MLK3 inhibitor
Chemical Names:
3-(1H-Indol-5-yl)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridine
Molecular Weight:
421.54
Molecular Formula:
C27H27N5
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

URMC-099 (1229582-33-5) 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).1 URMC-099 displayed neuroprotective effects in HIV-associated neurocognitive disorders2 and facilitated microglial amyloid-β degradation and clearance in mouse models.3,4 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.5

References/Citations:

1) Goodfellow et al. (2013), Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3; J. Med. Chem. 56 8032
2) Marker et al. (2013), The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disorders; J. Neurosc. 33 9998
3) Dong et al. (2016), The mixed-lineage kinase 3 inhibitor URMC-099 facilitates microglial amyloid-β degradation; J. Neuroinflammation 13 184
4) Kiyota et al. (2018), URMC-099 facilitates amyloid-β clearance in a murine model of Alzheimer’s disease; J. Neuroinflammation 15 137
5) Kumar et al. (2020), Mixed lineage kinase 3 inhibition induces T cell activation and cytotoxicity; Proc. Natl. Acad. Sci. USA 9 34567

URMC-099 | MLK3 inhibitor is also available in the Cellular Metabolism Library.
CAS:
1229582-33-5
Catalog Number:
10-4012
Activity:
MLK3 inhibitor
Chemical Names:
3-(1H-Indol-5-yl)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridine
Molecular Weight:
421.54
Molecular Formula:
C27H27N5
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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