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URMC-099 Mixed Lineage Kinase inhibitor

Name: URMC-099
Brand: Selleck Chemicals
SKU: S7343
Rating: 5 (14 reviews)

Cat.No.S7343

URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. This compound also inhibits ABL1 with IC50 of 6.8 nM. It induces Autophagy.

Chemical Structure

Molecular Weight: 421.54

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	ERK p38 MAPK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1
Other Mixed Lineage Kinase Inhibitors	Necrosulfonamide GW806742X GNE-3511

Chemical Information, Storage & Stability

Molecular Weight	421.54	Formula	C₂₇H₂₇N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1229582-33-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC=C4C5=CC6=C(C=C5)NC=C6)N=C3

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.250mg/ml (10.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Abl1 (Cell-free assay) 6.5 nM LRRK2 (Cell-free assay) 11 nM MLK3 (Cell-free assay) 14 nM MLK1 (Cell-free assay) 19 nM VEGFR1/FLT1 (Cell-free assay) 39 nM MLK2 (Cell-free assay) 42 nM SGK (Cell-free assay) 67 nM TrkA (Cell-free assay) 85 nM Aurora A (Cell-free assay) 108 nM ROCK2 (Cell-free assay) 111 nM Aurora B (Cell-free assay) 123 nM DLK (Cell-free assay) 150 nM c-Met (Cell-free assay) 177 nM IR (Cell-free assay) 200 nM SGK1 (Cell-free assay) 201 nM TrkB (Cell-free assay) 217 nM Aurora C (Cell-free assay) 290 nM IGF-1R (Cell-free assay) 307 nM LCK (Cell-free assay) 333 nM MEKK2 (Cell-free assay) 661 nM Syk (Cell-free assay) 731 nM ROCK1 (Cell-free assay) 1030 nM CDK1 (Cell-free assay) 1125 nM CDK2 (Cell-free assay) 1180 nM
In vitro	URMC-099 inhibits LPS-induced TNFα release in microglial cells, and HIV-1 Tat-induced release of cytokines in human monocytes. This compound prevents destruction and phagocytosis of cultured neuronal axons by microglia cells. It reduces fMLP-induced chemotaxis of wild-type neutrophil in vitro.
In vivo	In mice, URMC-099 shows excellent pharmacokinetic properties and improved CNS penetration. In vivo, this compound (10 mg/kg i.p.) reduces inflammatory cytokine production, protects neuronal architecture, and alters the morphologic and ultrastructural response of microglia to HIV-1 Tat exposure. It significantly reduces recruitment of neutrophils into the peritoneum by fMLP in wild-type mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24044867/ [2] https://pubmed.ncbi.nlm.nih.gov/23761895/ [3] https://pubmed.ncbi.nlm.nih.gov/24389043/

Applications

Methods	Biomarkers	Images	PMID
Immunofluorescence	LC3B		28134625

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