2. Cell Cycle/DNA Damage Stem Cell/Wnt PROTAC
  3. Casein Kinase Molecular Glues
  4. TMX-4116

TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma.

For research use only. We do not sell to patients.

TMX-4116 Chemical Structure

TMX-4116 Chemical Structure

CAS No. : 2766385-56-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 528 In-stock
Solution
10 mM * 1 mL in DMSO USD 528 In-stock
Solid
5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
100 mg USD 4000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

TMX-4116 Related Antibodies

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Description

TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma[1].

IC50 & Target[1]

CK1α

 

In Vitro

TMX-4116 (compound 16; 1 μM; 4 h) shows a high degradation preference for CK1α in MOLT4 cells[1].
TMX-4116 (250 nM, 4 h) induces primary target degradation of CK1α, while no downregulation of PDE6D, IKZF1, and IKZF3 in MOLT4 cells[1].

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

TMX-4116 Related Antibodies

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 μM
Incubation Time: 4 hours
Result: Showed a high degradation preference for CK1α.

Western Blot Analysis[1]

Cell Line: MOLT4, Jurkat, and MM.1S cells
Concentration: 0 nM, 40 nM, 200 nM, 1 μM
Incubation Time: 4 hours
Result: Showed a high degradation preference for CK1α with the DC50 value less than 200 nM in MOLT4, Jurkat, and MM.1S cells.
Molecular Weight

389.43

Formula

C17H19N5O4S
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(C(N1N=NC(C2=CSC(C(N3CCCC3)=O)=C2OC)=C1)CC4)NC4=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 : 100 mg/mL (256.79 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 2.5679 mL 12.8393 mL 25.6786 mL
5 mM 0.5136 mL 2.5679 mL 5.1357 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: ≥ 2.5 mg/mL (6.42 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.42 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).
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 2.5679 mL 12.8393 mL 25.6786 mL 64.1964 mL
5 mM 0.5136 mL 2.5679 mL 5.1357 mL 12.8393 mL
10 mM 0.2568 mL 1.2839 mL 2.5679 mL 6.4196 mL
15 mM 0.1712 mL 0.8560 mL 1.7119 mL 4.2798 mL
20 mM 0.1284 mL 0.6420 mL 1.2839 mL 3.2098 mL
25 mM 0.1027 mL 0.5136 mL 1.0271 mL 2.5679 mL
30 mM 0.0856 mL 0.4280 mL 0.8560 mL 2.1399 mL
40 mM 0.0642 mL 0.3210 mL 0.6420 mL 1.6049 mL
50 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2839 mL
60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0699 mL
80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8025 mL
100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6420 mL
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TMX-4116 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:

TMX-41162766385-56-0TMX4116TMX 4116Casein KinaseMolecular GluesdegraderMOLT4 cellsJurkat cellsMM.1S cellsmultiple myelomaInhibitorinhibitorinhibit

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