URMC-099
- CAS NO.:1229582-33-5
- Empirical Formula: C27H27N5
- Molecular Weight: 421.54
- MDL number: MFCD28168077
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-30 18:52:02
What is URMC-099?
Description
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
The Uses of URMC-099
URMC-099 is an orally bioavailable MLK3 inhibitor used in the treatment of Parkinson’s disease and HIV-1 associated neurocognitive disorders.
References
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
Properties of URMC-099
Density | 1.256±0.06 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | Soluble in DMSO (>25 mg/ml) |
form | solid |
pka | 13.49±0.40(Predicted) |
color | Off-white |
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. |
Safety information for URMC-099
Computed Descriptors for URMC-099
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