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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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TD-428 Related Classifications

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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.

Keywords:

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

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