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

Name: Thalidomide-4-OH
Brand: MedChemExpress
SKU: HY-103596
Rating: 4.5 (1 reviews)

Cat. No.: HY-103596 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 5054-59-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Thalidomide-4-OH:

Thalidomide-5-OH Get quote

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View All Ligands for E3 Ligase Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
NAMALVA	IC₅₀	> 1 μM Compound: 24	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	[PMID: 23168019]
PBMC	IC₅₀	> 1 μM Compound: 24	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	[PMID: 23168019]
T-cell	EC₅₀	> 1 μM Compound: 24	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	[PMID: 23168019]

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.

Molecular Weight

274.23

Formula

C₁₃H₁₀N₂O₅

CAS No.

5054-59-1

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	3.6465 mL	18.2327 mL	36.4655 mL
5 mM	0.7293 mL	3.6465 mL	7.2931 mL
10 mM	0.3647 mL	1.8233 mL	3.6465 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (275 KB) SDS (557 KB)

COA (253 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Marks MG, et al. Effects of putative hydroxylated thalidomide metabolites on blood vessel density in the chorioallantoic membrane (CAM) assay and on tumor and endothelial cell proliferation. Biol Pharm Bull. 2002 May;25(5):597-604. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6465 mL	18.2327 mL	36.4655 mL	91.1637 mL
	5 mM	0.7293 mL	3.6465 mL	7.2931 mL	18.2327 mL
	10 mM	0.3647 mL	1.8233 mL	3.6465 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	3.6465 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	1.1395 mL
	100 mM	0.0365 mL	0.1823 mL	0.3647 mL	0.9116 mL

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

Customer Review

Other Forms of Thalidomide-4-OH:

Thalidomide-4-OH Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Ligands for E3 Ligase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Thalidomide-4-OH Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Thalidomide-4-OH Related Classifications

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