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URMC-099

🥰Excellent
Catalog No. T6057Cas No. 1229582-33-5

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).

URMC-099

URMC-099

🥰Excellent
Purity: 99.32%
Catalog No. T6057Cas No. 1229582-33-5
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 SizePriceAvailabilityQuantity
5 mg$52In Stock
10 mg$79In Stock
25 mg$143In Stock
50 mg$233In Stock
100 mg$397In Stock
1 mL x 10 mM (in DMSO)$54In Stock
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Purity:99.32%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight421.54
FormulaC27H27N5
Cas No.1229582-33-5
SmilesCN1CCN(Cc2ccc(cc2)-c2cnc3[nH]cc(-c4ccc5[nH]ccc5c4)c3c2)CC1
Relative Density.1.256 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3723 mL11.8613 mL23.7225 mL118.6127 mL
5 mM0.4745 mL2.3723 mL4.7445 mL23.7225 mL
10 mM0.2372 mL1.1861 mL2.3723 mL11.8613 mL
DMSO
1mg5mg10mg50mg
20 mM0.1186 mL0.5931 mL1.1861 mL5.9306 mL
50 mM0.0474 mL0.2372 mL0.4745 mL2.3723 mL
100 mM0.0237 mL0.1186 mL0.2372 mL1.1861 mL

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