Catalog No.S8696 Synonyms: 2',3',4'-trihydroxy flavone
Molecular Weight(MW): 270.24
2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
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Choose Selective SUMO Inhibitors
|Description||2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.|
2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate. It decreases the ratio of p-Axl to t-Axl in a dose-dependent manner. Suppression of Axl kinase activity by 2D08 disrupts the cytoskeleton and actin filaments with re-organization at cellular junctions as shown by F-actin staining with phalloidin and increased expression of ZO-1 at cellular junctions. It also promotes translocation of β-catenin to cellular junctions and causes an upregulated E-cadherin. 2D08 significantly decreases the migration ability in lung multi-potent cell lines in a dose-dependent manner.
In Vitro Biochemical Kinase Assay:IC50 values of the Axl kinase inhibitor (2D08) are determined using kinase-mediated phosphorylation of poly-GAT by AlphaScreen luminescence detection technology. The inhibitor is tested at eight points of dilution in duplicate.
|In vitro||DMSO||54 mg/mL (199.82 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03097796||Suspended||Hematologic Diseases|Stem Cell Transplants||Pulmotect Inc.|National Heart Lung and Blood Institute (NHLBI)|Cancer Prevention Research Institute of Texas||December 2020||Phase 1|
|NCT02826837||Not yet recruiting||Advanced Colorectal Cancer||Taiwan Leader Biotech Corp.||June 1 2020||Phase 1|Phase 2|
|NCT03883217||Not yet recruiting||Parkinson Disease||Virginia Commonwealth University|Michael J. Fox Foundation for Parkinson''s Research||April 2020||Phase 2|
|NCT03861377||Not yet recruiting||Hemodynamic Instability|Anesthesia General|Anesthesia Intravenous||Helse Fonna||March 2020||Phase 4|
|NCT03883763||Not yet recruiting||Spinal Anesthesia|Vascular Surgery||Cristália Produtos Químicos Farmacêuticos Ltda.||March 1 2020||Phase 3|
|NCT03469284||Not yet recruiting||Diseases of Oral Cavity Salivary Glands and Jaws||M.D. Anderson Cancer Center||February 25 2020||Early Phase 1|
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