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  3. TD-428

TD-428 

Cat. No.: HY-114407
Handling Instructions

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.

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

TD-428 Chemical Structure

TD-428 Chemical Structure

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Description

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)

PROTAC

 

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].

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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

879.38

Formula

C₄₃H₄₃ClN₁₀O₇S

SMILES

O=C(NC1=CC(OCCOCCOCCNC2=C3C(N=NN(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)=CC=C1)C[[email protected]]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

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Product Name:
TD-428
Cat. No.:
HY-114407
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TD-428

Cat. No.: HY-114407