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|
|NCT02826837||Not yet recruiting||Advanced Colorectal Cancer||Taiwan Leader Biotech Corp.||June 1 2020||Phase 1|Phase 2|
|NCT03579888||Not yet recruiting||Acute Lymphoblastic Leukemia|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells|Blasts More Than 5 Percent of Peripheral Blood White Cells|CD19 Positive|Chronic Lymphocytic Leukemia|Minimal Residual Disease|Non-Hodgkin Lymphoma|Small Lymphocytic Lymphoma||M.D. Anderson Cancer Center|Ziopharm Oncology|Precigen Inc||December 2019||Phase 1|
|NCT03106376||Not yet recruiting||Healthy||Mclean Hospital||October 2019||Not Applicable|
|NCT03164447||Not yet recruiting||HIV-1 Infection||United BioPharma||September 2019||Phase 2|Phase 3|
|NCT02873351||Suspended||Age-related Macular Degeneration||Snyder Robert W. M.D. Ph.D. P.C.||September 2019||Phase 2|
|NCT02077621||Not yet recruiting||Cancer|Surgery|Fatigue||PhytoHealth Corporation||July 2019||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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