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2-D08

Cat. No. M9828
2-D08 Structure
Synonym:

2D08; 2',3',4'-trihydroxyflavone

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 100  USD100 In stock
25mg USD 220  USD220 In stock
50mg USD 355  USD355 In stock
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Quality Control & Documentation
Biological Activity

2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate. 2-D08 is also an inhibitor of Axl with IC50 of 0.49 nM. 2-D08 decreases the ratio of p-Axl to t-Axl in a dose-dependent manner.

Chemical Information
Molecular Weight 270.24
Formula C15H10O5
CAS Number 144707-18-6
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage 2-8°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Naoya Fujino, et al. Lab Invest. Phenotypic screening identifies Axl kinase as a negative regulator of an alveolar epithelial cell phenotype

[2] Himanish Ghosh, et al. Nat Commun. Several posttranslational modifications act in concert to regulate gephyrin scaffolding and GABAergic transmission

[3] Yeong Sang Kim, et al. Bioorg Med Chem Lett. Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation

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Keywords: 2-D08, 2D08; 2',3',4'-trihydroxyflavone supplier, E1/E2/E3 Enzyme, inhibitors, activators


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