TD-428

Cat. No.: HY-114407: FAQs
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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.

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

TD-428 Chemical Structure

CAS No. : 2334525-50-5

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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

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.

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.

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

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

Handling Instructions (2659 KB)

References

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

TD-428 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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