Thalidomide-4-OH
Based on 1 Customer Validation
Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 5054-59-1
- Formula: C13H10N2O5
- Molecular Weight:274.23
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cereblon |
hHDAC1 |
hHDAC2 |
hHDAC3 |
hHDAC6 |
hHDAC8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NAMALVA | IC50 |
>1 μM
Compound: 24
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Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting
Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting
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[PMID: 23168019] |
| PBMC | IC50 |
>1 μM
Compound: 24
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Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
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[PMID: 23168019] |
| T-cell | EC50 |
>1 μM
Compound: 24
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Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
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[PMID: 23168019] |
Thalidomide may exert anti-angiogenic effect in isolated blood vessels and endothelial cells. Thalidomide-OH is a putative hydroxylated thalidomide metabolite. Thalidomide-OH has weak anti-angiogenic activity (14% mean inhibition of blood vessel density at 100 mg). Thalidomide-OH does not have any anti-proliferative effect against the breast or neuroblastoma cells, but do possess appreciable anti-proliferative activity against the endothelial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 5054-59-1
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Appearance Solid
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Molecular Weight 274.23
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Formula C13H10N2O5
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Color White to gray
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SMILES
OC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O
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Synonyms
Cereblon ligand 2; E3 ligase Ligand 2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (364.66 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (18.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (18.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (291 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6466 mL | 18.2329 mL | 36.4657 mL | 91.1643 mL |
| 5 mM | 0.7293 mL | 3.6466 mL | 7.2931 mL | 18.2329 mL | |
| 10 mM | 0.3647 mL | 1.8233 mL | 3.6466 mL | 9.1164 mL | |
| 15 mM | 0.2431 mL | 1.2155 mL | 2.4310 mL | 6.0776 mL | |
| 20 mM | 0.1823 mL | 0.9116 mL | 1.8233 mL | 4.5582 mL | |
| 25 mM | 0.1459 mL | 0.7293 mL | 1.4586 mL | 3.6466 mL | |
| 30 mM | 0.1216 mL | 0.6078 mL | 1.2155 mL | 3.0388 mL | |
| 40 mM | 0.0912 mL | 0.4558 mL | 0.9116 mL | 2.2791 mL | |
| 50 mM | 0.0729 mL | 0.3647 mL | 0.7293 mL | 1.8233 mL | |
| 60 mM | 0.0608 mL | 0.3039 mL | 0.6078 mL | 1.5194 mL | |
| 80 mM | 0.0456 mL | 0.2279 mL | 0.4558 mL | 1.1396 mL | |
| 100 mM | 0.0365 mL | 0.1823 mL | 0.3647 mL | 0.9116 mL |
Thalidomide-4-OH Related Classifications
HY-103596 Related Classifications
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