Powder: -20°C for 3 years | In solvent: -80°C for 1 year
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 52.00 | |
10 mg | In stock | $ 79.00 | |
25 mg | In stock | $ 143.00 | |
50 mg | In stock | $ 233.00 | |
100 mg | In stock | $ 397.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 54.00 |
Description | URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM). |
Targets&IC50 | MLK1:19nM, MLK3:14nM, DLK:150 nM, MLK2:42nM |
In vitro | URMC-099, administered intraperitoneally (i.p.) at a dosage of 10 mg/kg, demonstrates the ability to reduce the production of inflammatory cytokines within the body, protect neuronal structures, and alter the morphology and ultrastructural response of microglia to exposure to HIV-1 Tat. In mice, URMC-099 exhibits favorable pharmacokinetics and enhanced Central Nervous System (CNS) penetration. Additionally, URMC-099 significantly reduces the infiltration of neutrophils into the peritoneum of wild-type mice in response to fMLP. |
In vivo | URMC-099 reduces chemotaxis in wild-type neutrophils induced by fMLP in vitro. Moreover, URMC-099 inhibits the release of TNFα in microglia triggered by lipopolysaccharides, as well as the release of cytokines in human monocytes stimulated by HIV-1 Tat. Additionally, URMC-099 prevents the destruction and phagocytosis of cultured neuronal axons by microglia. |
Kinase Assay | HDAC IC50 Profiling: The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company's standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds. |
Molecular Weight | 421.54 |
Formula | C27H27N5 |
CAS No. | 1229582-33-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 6 mg/mL (14.2 mM)
DMSO: 75 mg/mL (177.9 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
URMC-099 1229582-33-5 Angiogenesis Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair MAPK Metabolism Stem Cells Tyrosine Kinase/Adaptors MEK LRRK2 IGF-1R Bcr-Abl Syk CDK ROCK MLK VEGFR DNA Alkylation Trk receptor SGK c-Met/HGFR Src Aurora Kinase inhibit MLKs URMC099 URMC 099 Inhibitor Mixed Lineage Kinase inhibitor