URMC-099

Catalog No.S7343 Batch:S734303

Print

Technical Data

Formula

C27H27N5
Molecular Weight 421.54 CAS No. 1229582-33-5
Solubility (25°C)* In vitro DMSO 84 mg/mL (199.26 mM)
Ethanol 11 mg/mL (26.09 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.25mg/ml 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 95% Corn oil
0.7mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Targets
Abl1 [1]
(Cell-free assay)		 LRRK2 [1]
(Cell-free assay)		 MLK3 [1]
(Cell-free assay)		 MLK1 [1]
(Cell-free assay)		 VEGFR1/FLT1 [1]
(Cell-free assay)		 View More
6.5 nM 11 nM 14 nM 19 nM 39 nM
In vitro URMC-099 inhibits LPS-induced TNFα release in microglial cells, and HIV-1 Tat-induced release of cytokines in human monocytes. [1] URMC-099 prevents destruction and phagocytosis of cultured neuronal axons by microglia cells. [2] URMC-099 reduces fMLP-induced chemotaxis of wild-type neutrophil in vitro. [3]
In vivo In mice, URMC-099 shows excellent pharmacokinetic properties and improved CNS penetration. [1] In vivo, URMC-099 (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. [2] URMC099 significantly reduces recruitment of neutrophils into the peritoneum by fMLP in wild-type mice. [3]

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Mice exposed to HIV-1 Tat

  • Dosages

    10 mg/kg twice a day

  • Administration

    i.p.

Selleck's URMC-099 has been cited by 15 publications

PP1γ regulates neuronal insulin signaling and aggravates insulin resistance leading to AD-like phenotypes [ Cell Commun Signal, 2023, 21(1):82] PubMed: 37085815
TrkA expression directs the anti-neoplastic activity of MLK3 inhibitors in triple-negative breast cancer [ Oncogene, 2023, 42(14):1132-1143.] PubMed: 36813855
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
Systematic analysis of the MAPK signaling network reveals MAP3K-driven control of cell fate [ Cell Syst, 2022, 13(11):885-894.e4] PubMed: 36356576
Antiviral drug screen identifies DNA-damage response inhibitor as potent blocker of SARS-CoV-2 replication [ Cell Rep, 2021, 35(1):108940] PubMed: 33784499
Mixed Lineage Kinase 3 mediates PKG1α impact on cardiac function and controls blood pressure through separate mechanisms. [ JCI Insight, 2021, 6(18)e149075] PubMed: 34324442
Mixed Lineage Kinase 3 mediates PKG1α impact on cardiac function and controls blood pressure through separate mechanisms [ JCI Insight, 2021, 149075] PubMed: 34324442
Synergism between the phosphatidylinositol 3-kinase p110β isoform inhibitor AZD6482 and the mixed lineage kinase 3 inhibitor URMC-099 on the blockade of glioblastoma cell motility and focal adhesion formation [ Cancer Cell Int, 2021, 21(1):24] PubMed: 33407478
Rationalized inhibition of mixed lineage kinase 3 and CD70 enhances life span and antitumor efficacy of CD8 + T cells [ J Immunother Cancer, 2020, 8(2):e000494] PubMed: 32759234

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.