1. PROTAC Cell Cycle/DNA Damage
  2. Molecular Glues CDK
  3. dCeMM3

dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.

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dCeMM3 Chemical Structure

dCeMM3 Chemical Structure

CAS No. : 311787-85-6

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Based on 1 publication(s) in Google Scholar

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Description

dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex[1].

In Vitro

dCeMM3 (0.01–100 µM, 3 days) exhibits significant cytotoxicity in wild-type KBM7 cells, and its effect was dependent on UBE2M activity[1].
dCeMM3 (7 µM, 5 hours) significantly reduces Cyclin K levels in KBM7 cells[1].

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

Western Blot Analysis[1]

Cell Line: KBM7 cells
Concentration: 7 µM
Incubation Time: 5 hours
Result: Significantly reduced cyclin K levels.

Cell Viability Assay[1]

Cell Line: KBM7 wild-type (WT) and UBE2M mutant cells
Concentration: 0.01-100 µM
Incubation Time: 3 days
Result: Showed significant cytotoxicity in WT cells but greatly reduced cytotoxicity in UBE2M mutant cells.
Molecular Weight

318.78

Formula

C14H11ClN4OS

CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C(NC1=NC=C(Cl)C=C1)CSC2=NC3=CC=CC=C3N2

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 : 50 mg/mL (156.85 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 3.1370 mL 15.6848 mL 31.3696 mL
5 mM 0.6274 mL 3.1370 mL 6.2739 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (7.84 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 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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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
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 3.1370 mL 15.6848 mL 31.3696 mL 78.4240 mL
5 mM 0.6274 mL 3.1370 mL 6.2739 mL 15.6848 mL
10 mM 0.3137 mL 1.5685 mL 3.1370 mL 7.8424 mL
15 mM 0.2091 mL 1.0457 mL 2.0913 mL 5.2283 mL
20 mM 0.1568 mL 0.7842 mL 1.5685 mL 3.9212 mL
25 mM 0.1255 mL 0.6274 mL 1.2548 mL 3.1370 mL
30 mM 0.1046 mL 0.5228 mL 1.0457 mL 2.6141 mL
40 mM 0.0784 mL 0.3921 mL 0.7842 mL 1.9606 mL
50 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5685 mL
60 mM 0.0523 mL 0.2614 mL 0.5228 mL 1.3071 mL
80 mM 0.0392 mL 0.1961 mL 0.3921 mL 0.9803 mL
100 mM 0.0314 mL 0.1568 mL 0.3137 mL 0.7842 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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dCeMM3
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