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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|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|
|NCT03255915||Recruiting||HIV Prevention||Oak Crest Institute of Science|The Miriam Hospital|Johns Hopkins University|University of California Los Angeles|University of California San Diego|Vanderbilt University|The University of Texas Medical Branch Galveston|National Institutes of Health (NIH)|National Institute of Allergy and Infectious Diseases (NIAID)||October 9 2018||Early Phase 1|
|NCT03617081||Recruiting||Diabetes Mellitus Type 2||Novo Nordisk A/S||August 9 2018||Phase 1|
|NCT03609606||Completed||Dyslipidemias|Hypertension||Chong Kun Dang Pharmaceutical||August 9 2018||Phase 1|
|NCT03587207||Active not recruiting||Meningitis Meningococcal||GlaxoSmithKline||July 9 2018||Phase 2|
|NCT03557411||Recruiting||Non-Small-Cell Lung Cancer||Shandong Cancer Hospital and Institute|Jiangsu HengRui Medicine Co. Ltd.||July 9 2018||Phase 2|
|NCT03601052||Recruiting||Keloid||miRagen Therapeutics Inc.||July 9 2018||Phase 2|
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