受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H27N5 |
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分子量 | 421.54 | CAS No. | 1229582-33-5 | |
Solubility (25°C)* | 体外 | DMSO | 84 mg/mL (199.26 mM) | |
Ethanol | 84 mg/mL (199.26 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | 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. |
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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] |
キナーゼアッセイ | Biochemical assay for the inhibition of kinase activity for MLK3 | |
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Myelin basic protein (20 μM final concentration) is dissolved in 20 mM Hepes (pH 7.5) containing 10 μM MgCl2, 1 μM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 μM Na3VO4, 2 mM DTT, and 1% DMSO. Activated MLK3 is added and mixed (20 nM final concentration), and inhibitors are added in DMSO. 33P-ATP (specific activity 500 μCi/μL) is delivered into the reaction mixture to initiate the reaction (ATP concentration: 10 μM) and the mixture is incubated at room temperature for 20 minutes. % Activity is determined using a proprietary HOTSPOT™ microfluidic filter binding technology. | ||
動物実験 | 動物モデル | Mice exposed to HIV-1 Tat |
投薬量 | 10 mg/kg twice a day | |
投与方法 | i.p. |
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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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。