2. PROTAC Cell Cycle/DNA Damage
  3. Ligands for Target Protein for PROTAC CDK
  4. TMX-3013

TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).

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

TMX-3013

TMX-3013 Chemical Structure

CAS No. : 2488761-18-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
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Based on 1 publication(s) in Google Scholar

TMX-3013 Related Antibodies

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View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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  • Purity & Documentation

  • References

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Description

TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs)[1][2][3].

IC50 & Target[3]

CDK1

0.9 nM (IC50)

CDK2

<0.5 nM (IC50)

CDK4

24.5 nM (IC50)

CDK5

0.5 nM (IC50)

CDK6

15.6 nM (IC50)

In Vitro

TMX-6PEG-CA, a TMX3013-based covalent RIPTAC, selectively inhibits the viability of HaloTag-FKBP-expressing 293_HFL cells with a GI50 of 0.050 μM[1].
TMX-6PEG-FKBP, a TMX3013-based non-covalent RIPTAC, selectively inhibits the viability of HaloTag-FKBP-expressing 293_HFL cells with a GI50 of 0.011 μM[1].
TMX-3013 is a non-covalent picomolar CDK2 inhibitor that functions as the CDK2 homing ligand for the generation of NASA-based acylation probes[2].
TMX-3013 potently inhibits CDK2/cyclin A (<0.5 nM IC50), CDK1/cyclin B (0.9 nM IC50), and CDK5/p25 (0.5 nM IC50), with reduced potency against CDK4/cyclin D1 (24.5 nM IC50) and CDK6/cyclin D1 (15.6 nM IC50) in biochemical assays[3].

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

TMX-3013 Related Antibodies
Molecular Weight

481.30

Formula

C17H14BrFN6O3S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

NC(C1=C(C=CC=C1NC2=NC(NC3=CC=C(C=C3)S(N)(=O)=O)=NC=C2Br)F)=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 (207.77 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 2.0777 mL 10.3885 mL 20.7771 mL
5 mM 0.4155 mL 2.0777 mL 4.1554 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
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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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)

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 2.0777 mL 10.3885 mL 20.7771 mL 51.9427 mL
5 mM 0.4155 mL 2.0777 mL 4.1554 mL 10.3885 mL
10 mM 0.2078 mL 1.0389 mL 2.0777 mL 5.1943 mL
15 mM 0.1385 mL 0.6926 mL 1.3851 mL 3.4628 mL
20 mM 0.1039 mL 0.5194 mL 1.0389 mL 2.5971 mL
25 mM 0.0831 mL 0.4155 mL 0.8311 mL 2.0777 mL
30 mM 0.0693 mL 0.3463 mL 0.6926 mL 1.7314 mL
40 mM 0.0519 mL 0.2597 mL 0.5194 mL 1.2986 mL
50 mM 0.0416 mL 0.2078 mL 0.4155 mL 1.0389 mL
60 mM 0.0346 mL 0.1731 mL 0.3463 mL 0.8657 mL
80 mM 0.0260 mL 0.1299 mL 0.2597 mL 0.6493 mL
100 mM 0.0208 mL 0.1039 mL 0.2078 mL 0.5194 mL
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TMX-3013 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-30132488761-18-6TMX3013TMX 3013Ligands for Target Protein for PROTACCDKTarget Protein-binding MoietyCyclin dependent kinaseneuronal functionCDK1293_GFPL cellscell cycle regulation293_HFL cellsCDK9cyclin-dependent kinase activityCDK5CDK2cell cycle progressionInhibitorinhibitorinhibit

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