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Technical Data
| Formula | C27H27N5 |
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| Molecular Weight | 421.54 | CAS No. | 1229582-33-5 | |
| Solubility (25°C)* | In vitro | DMSO | 84 mg/mL (199.26 mM) | |
| Ethanol | 6 mg/mL (14.23 mM) | |||
| Water | Insoluble | |||
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* <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.) |
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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. | |||||||||||
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| Targets |
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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] |
Protocol (from reference)
| Animal Study:[2] |
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References
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Selleck's URMC-099 has been cited by 16 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.