DKM-2-93-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDKM 2-93Cat. No.: HY-101836CAS No.: 65836-72-8分式: CHClNO分量: 243.69作靶点: E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (615.54 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.1036 mL 20.5179 mL 41.0357 mL5 mM 0.8207 mL 4.1036 mL 8.2071 mL10 mM 0.4104 mL 2.0518 mL 4.1036 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 DKM 2-93是相对选择性的UBA5抑制剂，IC50值为430 M。IC50 & Targ

3、et IC50: 430 M (UBA5), 90 M (PaCa2 cells), 30 M (Panc1 cells) 1体外研究Ubiquitin-like modifier activating enzyme 5 (UBA5) is a novel pancreatic cancer therapeutic target. DKM 2-93impairs pancreatic cancer cell survival through covalently modifying the catalytic cysteine of UBA5, thereby1/2 Master of Sma

4、ll Molecules 您边的抑制剂师www.MedChemEinhibiting its activity as a protein that activates the ubiquitin-like protein UFM1 to UFMylate proteins. DKM 2-93 inhibits PaCa2 and Panc1 cells survival with IC50s of 90 and 30 M, respectively 1.体内研究 DKM 2-93 daily treatment significantly impairs tumor growth of PaC

5、a2 cells in vivo in tumor xenograft studiesin immune-deficient mice without causing any weight loss or overt toxicity 1.PROTOCOLCell Assay 1 PaCa2 and Panc1 cells are treated with 0-1000 M DKM 2-93 for 48 hours. Cell viability is assessed byHoescht stain 1.MCE has not independently confirmed the acc

6、uracy of these methods. They are for reference only.Animal Mice: Mice are subcutaneously injected with PaCa2 cells to initiate the tumor xenograft study and treatmentsAdministration 1 of mice are initiated with vehicle or DKM 2-93 (50 mg/kg ip, once per day) three days after injection of cancercells

7、 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Rep. 2019 Apr 16;27(3):971-986.e9. bioRxiv. June 28, 2018.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Roberts AM, et al. Chemoproteomic Screening of Covalent Ligands Reveals UBA5 As a Novel Pancreatic Cancer Target. ACS ChemBiol. 2017 Apr 21;12(4):899-904.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea