2-D08
Based on 12 publication(s) in Google Scholar
2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
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- Pureté: 99.37%
- CAS No.: 144707-18-6
- Formule: C15H10O5
- Masse moléculaire:270.24
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Stockage:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
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Publications Citing Use of MedChemExpress (MCE) 2-D08
More- Nat Commun. 2025 Oct 29;16(1):9554. [Abstract]
- Nat Commun. 2022 Sep 3;13(1):5204. [Abstract]
- Cell Death Differ. 2025 Jun;32(6):1041-1057. [Abstract]
- Oncogene. 2025 May;44(19):1361-1374. [Abstract]
- Sci Signal. 2023 Mar 14;16(776):eabq3362. [Abstract]
- Plant Cell Environ. 2024 Jun 27. [Abstract]
- Life Sci. 2020 Aug 15;255:117859. [Abstract]
- J Virol. 2025 Nov 25:e0164825. [Abstract]
- Andrology. 2025 Jul 2. [Abstract]
- Res Sq. 2026 Mar 5.
- Temple University. 2025.
- bioRxiv. 2021 May 26.
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Activité biologique
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Axl |
2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate[1]. 2-D08 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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 144707-18-6
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Appearance Solid
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Masse moléculaire 270.24
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Formule C15H10O5
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Color Light yellow to yellow
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SMILES
O=C1C=C(C2=CC=C(O)C(O)=C2O)OC3=CC=CC=C13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
Nanomaterial signatures program biomolecular condensates via triphasic separation for chemoplasticity remodeling. [Abstract]2025 Oct 29;16(1):9554. PMID: 41162367 -
Nat Commun
Suppression of ACE2 SUMOylation protects against SARS-CoV-2 infection through TOLLIP-mediated selective autophagy. [Abstract]2022 Sep 3;13(1):5204. PMID: 36057605
2-D08 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 3;13(1):5204. [Abstract]
Immunoblotting of 293 T cells transfected with plasmids of Flag-ACE2 and HA-SUMO3 in the presence of 2-D08 (200 μM; 24 h), ML-792 (10 μM), GA (5 μM), or TAK-981 (5 μM). 2-D08 largely decreased the SUMOylation of ACE2.
2-D08 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 3;13(1):5204. [Abstract]
Protein abundance and mRNA level of ACE2 in Calu-3 cells treated with 2-D08 (100-300 μM; 24h). Protein levels of ACE2 were gradually reduced upon 2-D08 treatments in a dose-dependent manner.
2-D08 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 3;13(1):5204. [Abstract]
293 T cells were transfected with plasmids encoding Flag-ACE2 and HA-TOLLIP, and treatedwith indicated concentrations of 2-D08 (100-200 μM; 24 h). The cells cultured with Baf A1 (0.2 μM) for 6 h were immunoprecipitated with α-FLAG M2 beads and immunoblotted with anti-HA. ACE2-TOLLIP association was increased upon 2-D08 treatment.
2-D08 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 3;13(1):5204. [Abstract]
GSEA analysis of differentially expressed genes (DEGs) in Calu-3 cells infected with SARS-CoV-2 (MOI = 0.5) for 24 h with or without 2-D08 (100 μM) treatment.
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Cell Death Differ
Redox regulation of TRIM28 facilitates neuronal ferroptosis by promoting SUMOylation and inhibiting OPTN-selective autophagic degradation of ACSL4. [Abstract]2025 Jun;32(6):1041-1057. PMID: 39875520 -
Oncogene
SENP1-mediated deSUMOylation of YBX1 promotes colorectal cancer development through the SENP1-YBX1-AKT signaling axis. [Abstract]2025 May;44(19):1361-1374. PMID: 39988696 -
Sci Signal
SUMOylated IL-33 in the nucleus stabilizes the transcription factor IRF1 in hepatocellular carcinoma cells to promote immune escape. [Abstract]2023 Mar 14;16(776):eabq3362. PMID: 36917642 -
Plant Cell Environ
2024 Jun 27. PMID: 38935876 -
Life Sci
Sumoylation enhances the activity of the TGF-β/SMAD and HIF-1 signaling pathways in keloids. [Abstract]2020 Aug 15;255:117859. PMID: 32474020
2-D08 purchased from MedChemExpress. Usage Cited in: Life Sci. 2020 Aug 15;255:117859. [Abstract]
The expression levels of TGF-β/SMAD and HIF-1 signaling pathways-related proteins, including Col III, Smad2, Smad3, Smad4 and HIF-1α are measured by western blotting in HFFs and HKFs. The band intensity ratio of the TGF-β/SMAD and HIF-1 signaling related protein to reference protein is significantly decreased in the 2-D08 group.
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J Virol
SUMOylation-dependent degradation of nucleocapsid is responsible for Pestivirus uncoating. [Abstract]2025 Nov 25:e0164825. PMID: 41288382 -
Andrology
Ubiquitin-mediated immunoglobulin-binding protein 1 degradation promotes autophagy and sperm capacitation in vitro. [Abstract]2025 Jul 2. PMID: 40600667 -
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Solvant et solubilité
DMSO : 66.67 mg/mL (246.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (18.50 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Human lung multi-potent cells at passage 5 are incubated with DMEM+0.5% BSA+penicillin/streptomycin containing either 0.1% DMSO (vehicle) or 2D08 (10 μM) on Permanox culture slides for 6 days. Cells are fixed with 4% PFA for 30 min and then blocked and permeabilized with 10% goat serum and 0.3% Triton-X 100 in PBS for 30 min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Eight- to 10-week-old mice (both male and female) are used for the study. A 5 cm-long glass pipette is buffered with Mineral Oil and then attached to the injection apparatus to take up 10 μL of 2-D08 (30 μM) or NaCl[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kim YS, et al. Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1094-7. [Content Brief]
[2]. Fujino N, et al. Phenotypic screening identifies Axl kinase as a negative regulator of an alveolar epithelial cell phenotype. Lab Invest. 2017 Sep;97(9):1047-1062. [Content Brief]
[3]. Ghosh H, et al. Several posttranslational modifications act in concert to regulate gephyrin scaffolding and GABAergic transmission. Nat Commun. 2016 Nov 7;7:13365. doi: 10.1038/ncomms13365. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | 92.5104 mL |
| 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | 18.5021 mL | |
| 10 mM | 0.3700 mL | 1.8502 mL | 3.7004 mL | 9.2510 mL | |
| 15 mM | 0.2467 mL | 1.2335 mL | 2.4669 mL | 6.1674 mL | |
| 20 mM | 0.1850 mL | 0.9251 mL | 1.8502 mL | 4.6255 mL | |
| 25 mM | 0.1480 mL | 0.7401 mL | 1.4802 mL | 3.7004 mL | |
| 30 mM | 0.1233 mL | 0.6167 mL | 1.2335 mL | 3.0837 mL | |
| 40 mM | 0.0925 mL | 0.4626 mL | 0.9251 mL | 2.3128 mL | |
| 50 mM | 0.0740 mL | 0.3700 mL | 0.7401 mL | 1.8502 mL | |
| 60 mM | 0.0617 mL | 0.3084 mL | 0.6167 mL | 1.5418 mL | |
| 80 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 1.1564 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9251 mL |
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