GLPBio

TD-428

Catalog No.: GC34319Purity:>98%
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
Cas No.: 2334525-50-5
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Description

TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM[1].

TD-428, the BRD4 degrader with TD-106, is highly specific for BET proteins. TD-428 (0.01, 0.1, 1, 10, 100, 1000, and 10000 nM; 72?hours) inhibits the proliferation of 22RV1 cells with a CC50?of??20.1?nM[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, 100nM, 1000 nM, and 10?μM|Incubation Time:|12?hours|Result:|Induced the degradation of BET proteins.

[1]. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.

Chemical Properties

CAS No.
2334525-50-5
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
Molecular Formula
C43H43ClN10O7S
Molecular Weight
879.38
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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