2. PROTAC Epigenetics
  3. Molecular Glues Epigenetic Reader Domain
  4. TMX1

TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.

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TMX1

TMX1 Chemical Structure

CAS No. : 3079093-92-5

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TMX1 Related Antibodies

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Description

TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity[1][2].

IC50 & Target[1]

BRD4 BD2

 

BRD2

 

BRD3

 

In Vitro

TMX1 (0.01-10 μM; 4-24 h) induces proteasome-dependent, DCAF16-mediated degradation of BRD4, with selective activity against the BRD4BD2 domain, achieving ~80% maximal degradation in K562 cells at 16 h[1].
TMX1 (0.5 μM; 5 h) selectively downregulates BRD4 (with minor effects on BRD2 and BRD3) in K562 cells[1].
TMX1 (0.1 μM; 14 days) requires DCAF16 for its induced cellular toxicity in K562 cells[1].
TMX1 (0.01-10 μM; 16 h) induces concentration-dependent degradation of BRD4 in K562 cells after 16 h of treatment[2].
TMX1 (1 μM; 16 h) induced degradation of BRD4_BD2-eGFP in K562-Cas9 cells requires the RBX1-CUL4-DDB1-DCAF16 ubiquitin ligase complex, as demonstrated by a UPS-focused CRISPR screen with treatment at 1 μM for 16 h[2].
TMX1 (1 μM; 16 h) induced BRD4 degradation in K562 cells requires DCAF16 after 16 h of treatment at 1 μM[2].

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

TMX1 Related Antibodies

Western Blot Analysis[2]

Cell Line: K562 cells
Concentration: 0.01-10 μM
Incubation Time: 16 h
Result: Induced concentration-dependent degradation of BRD4, with visible reduction of BRD4 protein levels across all tested concentrations relative to the DMSO control.
Maintained stable actin levels as a loading control.

Western Blot Analysis[2]

Cell Line: DCAF16-knockout K562 cells
Concentration: 1 μM
Incubation Time: 16 h
Result: Abolished TMX1-induced BRD4 degradation in DCAF16-knockout K562 cells, whereas BRD4 degradation was observed in cells transduced with non-targeting sgRNA.

Western Blot Analysis[2]

Cell Line: DCAF16-knockout K562 cells expressing DCAF16 mutants
Concentration: 1 μM
Incubation Time: 16 h
Result: Abolished TMX1-induced BRD4 degradation in cells expressing the DCAF16 C58S mutant, whereas degradation was preserved in cells expressing wild-type DCAF16 or other mutants (C177S, C179S, A53R).
Molecular Weight

476.59

Formula

C26H28N4O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C/C=C/C1=CC=C(C2=N[C@@H](CC(OC(C)(C)C)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (209.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0982 mL 10.4912 mL 20.9824 mL
5 mM 0.4196 mL 2.0982 mL 4.1965 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 (sealed storage, away from moisture and light). 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (5.25 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 (5.25 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
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+
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.57%

SDS (252 KB)

COA (258 KB) HNMR (223 KB) LCMS (96 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 (sealed storage, away from moisture and light). 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 2.0982 mL 10.4912 mL 20.9824 mL 52.4560 mL
5 mM 0.4196 mL 2.0982 mL 4.1965 mL 10.4912 mL
10 mM 0.2098 mL 1.0491 mL 2.0982 mL 5.2456 mL
15 mM 0.1399 mL 0.6994 mL 1.3988 mL 3.4971 mL
20 mM 0.1049 mL 0.5246 mL 1.0491 mL 2.6228 mL
25 mM 0.0839 mL 0.4196 mL 0.8393 mL 2.0982 mL
30 mM 0.0699 mL 0.3497 mL 0.6994 mL 1.7485 mL
40 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3114 mL
50 mM 0.0420 mL 0.2098 mL 0.4196 mL 1.0491 mL
60 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
80 mM 0.0262 mL 0.1311 mL 0.2623 mL 0.6557 mL
100 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5246 mL
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TMX1 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:

TMX13079093-92-5TMX 1TMX-1Molecular GluesEpigenetic Reader DomainBRD3proteasomeGAKBRD4DCAF16BRD2HEK293T cellsK562 cellsBRD4BD2CRL4DCAF16 ubiquitin ligase complexInhibitorinhibitorinhibit

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