2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. TD-428

TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.

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TD-428 Chemical Structure

TD-428 Chemical Structure

CAS No. : 2334525-50-5

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Based on 1 publication(s) in Google Scholar

TD-428 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM[1]. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation[1].

IC50 & Target[1]

BRD4

0.32 nM (DC50)

Cereblon

 

Cellular Effect
Cell Line Type Value Description References
CWR22R CC50
20.1 nM
Compound: TD-428; 21b
Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
[PMID: 30684871]
In Vitro

TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1[1].
TD-428 (0.01-10,000 nM; 72 hours) inhibits the proliferation of 22RV1 cells with a CC50 of 20.1 nM[1].
TD-428 (1 nM-10 μM; 12 hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins[1].

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

TD-428 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: 22RV1 cells
Concentration: 0.01, 0.1, 1, 10, 100, 1000, and 10000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation with a CC50 of 20.1 nM.

Western Blot Analysis[1]

Cell Line: U266 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM, and 10 μM
Incubation Time: 12 hours
Result: Induced the degradation of BRD4, IKZF1, IKZF3 proteins.
Molecular Weight

879.38

Formula

C43H43ClN10O7S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(NC1=CC(OCCOCCOCCNC2=C3C(N=NN(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)=CC=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
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 (113.72 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 1.1372 mL 5.6858 mL 11.3716 mL
5 mM 0.2274 mL 1.1372 mL 2.2743 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.

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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 1.1372 mL 5.6858 mL 11.3716 mL 28.4291 mL
5 mM 0.2274 mL 1.1372 mL 2.2743 mL 5.6858 mL
10 mM 0.1137 mL 0.5686 mL 1.1372 mL 2.8429 mL
15 mM 0.0758 mL 0.3791 mL 0.7581 mL 1.8953 mL
20 mM 0.0569 mL 0.2843 mL 0.5686 mL 1.4215 mL
25 mM 0.0455 mL 0.2274 mL 0.4549 mL 1.1372 mL
30 mM 0.0379 mL 0.1895 mL 0.3791 mL 0.9476 mL
40 mM 0.0284 mL 0.1421 mL 0.2843 mL 0.7107 mL
50 mM 0.0227 mL 0.1137 mL 0.2274 mL 0.5686 mL
60 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
80 mM 0.0142 mL 0.0711 mL 0.1421 mL 0.3554 mL
100 mM 0.0114 mL 0.0569 mL 0.1137 mL 0.2843 mL
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TD-428 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:

TD-4282334525-50-5TD428TD 428PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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