2. PROTAC Autophagy Apoptosis
  3. E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis
  4. Thalidomide-NH-CH2-COOH

Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).

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Thalidomide-NH-CH2-COOH Chemical Structure

Thalidomide-NH-CH2-COOH Chemical Structure

CAS No. : 927670-97-1

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Based on 1 publication(s) in Google Scholar

Thalidomide-NH-CH2-COOH Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1 Aryl Hydrocarbon Receptor

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  • Purity & Documentation

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Description

Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937)[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Thalidomide-NH-CH2-COOH Related Antibodies
Molecular Weight

331.28

Formula

C15H13N3O6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(O)CNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (150.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0186 mL 15.0930 mL 30.1859 mL
5 mM 0.6037 mL 3.0186 mL 6.0372 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. 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: ≥ 1.67 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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).
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: 98.20%

COA (252 KB) HNMR (239 KB) LCMS (118 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. 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 3.0186 mL 15.0930 mL 30.1859 mL 75.4649 mL
5 mM 0.6037 mL 3.0186 mL 6.0372 mL 15.0930 mL
10 mM 0.3019 mL 1.5093 mL 3.0186 mL 7.5465 mL
15 mM 0.2012 mL 1.0062 mL 2.0124 mL 5.0310 mL
20 mM 0.1509 mL 0.7546 mL 1.5093 mL 3.7732 mL
25 mM 0.1207 mL 0.6037 mL 1.2074 mL 3.0186 mL
30 mM 0.1006 mL 0.5031 mL 1.0062 mL 2.5155 mL
40 mM 0.0755 mL 0.3773 mL 0.7546 mL 1.8866 mL
50 mM 0.0604 mL 0.3019 mL 0.6037 mL 1.5093 mL
60 mM 0.0503 mL 0.2515 mL 0.5031 mL 1.2577 mL
80 mM 0.0377 mL 0.1887 mL 0.3773 mL 0.9433 mL
100 mM 0.0302 mL 0.1509 mL 0.3019 mL 0.7546 mL
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Thalidomide-NH-CH2-COOH 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-NH-CH2-COOH927670-97-1E3 Ligase Ligand-Linker ConjugatesAutophagyApoptosisCRBNcereblonThalidomideInhibitorinhibitorinhibit

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