2. PROTAC Apoptosis Autophagy
  3. Ligands for E3 Ligase Autophagy Apoptosis
  4. Thalidomide-4-OH

Thalidomide-4-OH  (Synonyms: Cereblon ligand 2; E3 ligase Ligand 2)

Cat. No.: HY-103596 Purity: 99.85%
COA Handling Instructions

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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.

Thalidomide-4-OH Chemical Structure

Thalidomide-4-OH Chemical Structure

CAS No. : 5054-59-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Thalidomide-4-OH:

Thalidomide-4-OH Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

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Description

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[1].

IC50 & Target

Cereblon

 

In Vitro

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.

Thalidomide-4-OH Related Antibodies
Molecular Weight

274.23

Formula

C13H10N2O5
CAS No.
Appearance

Solid

Color

White to gray

SMILES

OC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 36.5 mg/mL (133.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6466 mL 18.2329 mL 36.4657 mL
5 mM 0.7293 mL 3.6466 mL 7.2931 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (9.12 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.85%

COA (253 KB) LCMS (87 KB)

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
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Thalidomide-4-OH Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Thalidomide-4-OH5054-59-1Cereblon ligand 2 E3 ligase Ligand 2Cereblon ligand2Cereblon ligand-2Ligands for E3 LigaseAutophagyApoptosisE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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