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Cat. No.: HY-173256

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Hyp-dBET1

Hyp-dBET1 is a hypoxia-activated BRD4 PROTAC degrader. The IC₅₀ of Hyp-dBET1 for reducing cell viability under hypoxic conditions is approximately 153 nM to 192 nM, while it shows low activity under normoxic conditions (IC₅₀ of approximately 2.8 μM to 3.8 μM). Hyp-dBET1 induces BRD4 degradation under hypoxic conditions, converts to dBET1 in hypoxic environments, and downregulates the expression level of ZFP-91. Hyp-dBET1 can be used in studies related to breast cancer, cervical cancer and solid tumors.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker (HY-178091)).

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

Formula: C₄₅H₄₂ClN₉O₉S
Molecular Weight:920.39

Storage:

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

Data Sheet (275 KB)

Hyp-dBET1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Hyp-dBET1 is a hypoxia-activated BRD4 PROTAC degrader. The IC₅₀ of Hyp-dBET1 for reducing cell viability under hypoxic conditions is approximately 153 nM to 192 nM, while it shows low activity under normoxic conditions (IC₅₀ of approximately 2.8 μM to 3.8 μM). Hyp-dBET1 induces BRD4 degradation under hypoxic conditions, converts to dBET1 in hypoxic environments, and downregulates the expression level of ZFP-91. Hyp-dBET1 can be used in studies related to breast cancer, cervical cancer and solid tumors^[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker (HY-178091)).

IC₅₀ & Target^[1]

BRD4

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

Hyp-dBET1 (0.05-5.0 μM; 24 h) significantly degrades BRD4 protein in MDA-MB-231 cells under hypoxic conditions, while it exerts no obvious BRD4-degrading effect but downregulates the expression of downstream protein ZFP-91 under normoxic conditions^[1].
Hyp-dBET1 (0.1-100 μM; 72 h) exerts a concentration-dependent effect on reducing cell viability in MDA-MB-231 (with an IC₅₀ value of 3.4 μM under normoxia), HeLa (with IC₅₀ values of 3815 nM and 192 nM under normoxia and hypoxia, respectively), and HEK-293 (with IC₅₀ values of 2870 nM and 153 nM under normoxia and hypoxia, respectively) cells under either hypoxic or normoxic conditions^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0.05, 0.1, 0.2, 0.5, 1.0, 2.0, 5.0 μM
Incubation Time:

24 h
Result:

Significantly degraded the target protein BRD4 under hypoxic conditions.
Failed to effectively degrade the target protein BRD4 under normoxic conditions.
Non-specifically downregulated the expression of the downstream protein ZFP-91 under normoxic conditions.

Chemical Information

Molecular Weight 920.39
Formula C₄₅H₄₂ClN₉O₉S
SMILES

CC1=C(C)C(C(C2=CC=C(Cl)C=C2)=N[C@H]3CC(N(CC4=CC=C([N+]([O-])=O)C=C4)CCCCNC(COC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)=O)=O)=C(S1)N8C3=NN=C8C
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Dutta R, et al. Dual-Action-Only PROTACs. Journal of the American Chemical Society. 2025 Mar 19;147(11):9074-9078. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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Hyp-dBET1

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms