1. PROTAC Apoptosis Autophagy
  2. Ligands for E3 Ligase Autophagy Apoptosis
  3. tDHU, acid

tDHU, acid is a dihydropyrimidinecereblon ligand that contains an E3 ligase ligand and a benzoic acid linker. tDHU, acid can be used as an E3 ubiquitin ligase ligand-Linker conjugate for the development of PROTACs.

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tDHU, acid Chemical Structure

tDHU, acid Chemical Structure

CAS No. : 2377643-37-1

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Based on 1 publication(s) in Google Scholar

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Description

tDHU, acid is a dihydropyrimidinecereblon ligand that contains an E3 ligase ligand and a benzoic acid linker. tDHU, acid can be used as an E3 ubiquitin ligase ligand-Linker conjugate for the development of PROTACs[1].

IC50 & Target

Cereblon

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 50 μM
Compound: tDHU-CO2H
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay
[PMID: 35859867]
HEK293 IC50
> 50 μM
Compound: tDHU-CO2H
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
[PMID: 35859867]
HEK293 IC50
1.94 μM
Compound: tDHU-CO2H
Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
[PMID: 35859867]
Molecular Weight

248.23

Formula

C12H12N2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C)C(N2C(NC(CC2)=O)=O)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 17.5 mg/mL (70.50 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0285 mL 20.1426 mL 40.2852 mL
5 mM 0.8057 mL 4.0285 mL 8.0570 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 4.0285 mL 20.1426 mL 40.2852 mL 100.7131 mL
5 mM 0.8057 mL 4.0285 mL 8.0570 mL 20.1426 mL
10 mM 0.4029 mL 2.0143 mL 4.0285 mL 10.0713 mL
15 mM 0.2686 mL 1.3428 mL 2.6857 mL 6.7142 mL
20 mM 0.2014 mL 1.0071 mL 2.0143 mL 5.0357 mL
25 mM 0.1611 mL 0.8057 mL 1.6114 mL 4.0285 mL
30 mM 0.1343 mL 0.6714 mL 1.3428 mL 3.3571 mL
40 mM 0.1007 mL 0.5036 mL 1.0071 mL 2.5178 mL
50 mM 0.0806 mL 0.4029 mL 0.8057 mL 2.0143 mL
60 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6786 mL
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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.

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tDHU, acid
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HY-W454906
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