| Name | URMC-099 |
| 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). |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 6 mg/mL (14.23 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.74 mM), Sonication is recommended.
DMSO : 62.5 mg/mL (148.27 mM), Sonication is recommended.
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| Keywords | VEGFR1/FLT1 | URMC-099 | URMC099 | URMC 099 | Trkreceptor | TrkB | TrkA | Trk receptor | Syk | SGK1 | SGK | ROCK2 | ROCK1 | MLKs | MLK3 | MLK2 | MLK1 | Mixed Lineage Kinase | MEKK2 | LRRK2 | Lck | Insulin Receptor | Inhibitor | inhibit | IGF-1R | IGF1R | HGFR | DNAAlkylation | DNA Alkylation | DLK | cMet/HGFR | c-Met | cMet | CDK2 | CDK1 | BcrAbl | Autophagy | AuroraKinase | Aurora Kinase | Aurora C | Aurora B | Aurora A | Abl1 |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Cysteamine hydrochloride | 2-Chloropyrazine | Guanidine hydrochloride | Hydroxychloroquine | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Diabetic Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | TGF-beta/Smad Compound Library |
United States
