dBRD4-BD1

Cat. No.: HY-151593: FAQs
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dBRD4-BD1 is a selective and durable BRD4 degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.

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

dBRD4-BD1 Chemical Structure

CAS No. : 2839318-19-1

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Description

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1^[1].

In Vitro

dBRD4-BD1 (64 pM-25 nM; 24 h) degrades BDR4 in a dose-dependent manner^[1].
dBRD4-BD1 (5 μM; 0-72 h) increases the protein level of BRD2 and BRD3^[1].

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

Western Blot Analysis^[1]

Cell Line:	MM.1S cells
Concentration:	25, 5, 1, 0.2, 0.04, 0.008, 0.0016 nM and 320 pM, 64 pM
Incubation Time:	24 hours
Result:	Degraded BDR4 in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	MM.1S cells
Concentration:	5 μM
Incubation Time:	0, 0.5, 1, 2, 4, 8, 12, 24, 30, 36, 48, 72 hours
Result:	Increased the protein amount of BRD2 and BRD3 without decreasing cMyc protein level in 4 hr period.

Molecular Weight

967.00

Formula

C₅₀H₅₃F₃N₈O₉

CAS No.

2839318-19-1

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCC(NCCOCCOCCN4CCC(CC4)N5C=NC(C6=CC=C(C(F)(F)F)C=C6)=C5C7=CC=NC(OC8=CC(C(C)C)=CC=C8C)=N7)=O)=CC=C3)=O)=O

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]. Divakaran A, et al. Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. ACS Med Chem Lett. 2022 Sep 29;13(10):1621-1627. [Content Brief]

dBRD4-BD1 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:

dBRD4-BD12839318-19-1PROTACsEpigenetic Reader DomainBETselectivedurableInhibitorinhibitorinhibit

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