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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 | Price | Availability | Quantity |
---|---|---|---|
5 mg | $52 | In Stock | |
10 mg | $79 | In Stock | |
25 mg | $143 | In Stock | |
50 mg | $233 | In Stock | |
100 mg | $397 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
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 | MLK2:42nM, DLK:150 nM, MLK3:14nM, MLK1:19nM |
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 |
Smiles | CN1CCN(Cc2ccc(cc2)-c2cnc3[nH]cc(-c4ccc5[nH]ccc5c4)c3c2)CC1 |
Relative Density. | 1.256 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 6 mg/mL (14.2 mM) DMSO: 75 mg/mL (177.9 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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