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Cat. No.: HY-139294

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PROTAC BRD4 Degrader-15

PROTAC BRD4 Degrader-15 is a BRD4 PROTAC degrader with a DC₅₀ of 2.1 nM. PROTAC BRD4 Degrader-15 forms a ternary complex with BRD4 and VHL ubiquitin ligase to induce degradation. PROTAC BRD4 Degrader-15 inhibits the transcription level of the MYC gene. PROTAC BRD4 Degrader-15 suppresses human megakaryocytopoiesis and exhibits antigen-dependent tumor growth inhibition in xenograft models of prostate cancer and acute myeloid leukemia. PROTAC BRD4 Degrader-15 can be used in studies related to prostate cancer and acute myeloid leukemia.
(Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-184712)).

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

CAS No.: 2417370-67-1
Formula: C₅₇H₆₂F₂N₁₀O₁₀S₂
Molecular Weight:1149.29

Storage:

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

Data Sheet (287 KB)

PROTAC BRD4 Degrader-15 Chemical Structure

CAS No.: 2417370-67-1

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

PROTAC BRD4 Degrader-15 is a BRD4 PROTAC degrader with a DC₅₀ of 2.1 nM. PROTAC BRD4 Degrader-15 forms a ternary complex with BRD4 and VHL ubiquitin ligase to induce degradation. PROTAC BRD4 Degrader-15 inhibits the transcription level of the MYC gene. PROTAC BRD4 Degrader-15 suppresses human megakaryocytopoiesis and exhibits antigen-dependent tumor growth inhibition in xenograft models of prostate cancer and acute myeloid leukemia. PROTAC BRD4 Degrader-15 can be used in studies related to prostate cancer and acute myeloid leukemia^[1]. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-184712)).

IC₅₀ & Target

^[1]

BRD4

2.1 nM (DC₅₀)

BRD4 BD2

8.1 nM (IC₅₀)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC50	15 nM	Suppression of MYC gene transcript levels in human MV4-11 AML cells incubated for 4 h. Suppression of MYC gene transcript levels in human MV4-11 AML cells incubated for 4 h.	33596073
EOL1	DC₅₀	2.1 nM	Reduction of BRD4 protein levels in EOL-1 cells incubated for 4 h. Reduction of BRD4 protein levels in EOL-1 cells incubated for 4 h.	33596073
HL-60	IC50	4.2 nM	Inhibition of HL-60 AML cell proliferation incubated for 6 days. Inhibition of HL-60 AML cell proliferation incubated for 6 days.	33596073

In Vitro

PROTAC BRD4 Degrader-15 (compound 13) inhibits MYC gene transcription levels by 98% at maximum efficacy in MV4-11 acute myeloid leukemia cells, with an IC₅₀ of 15 nM; it degrades up to 98% of BRD4 protein in EOL-1 cells, with a DC₅₀ of 2.1 nM^[1].
PROTAC BRD4 Degrader-15 (6 days) inhibits the proliferation of PC3-S1 prostate cancer cells with an IC₅₀ of 91 nM, and suppresses the proliferation of HL-60 acute myeloid leukemia (AML) cells with an IC₅₀ of 4.2 nM^[1].
PROTAC BRD4 Degrader-15 (1-1000 nM; 4-22 h) can passively diffuse into PC3-S1 cells^[1].

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

In Vivo

PROTAC BRD4 Degrader-15 (compound 13) (10 mg/kg; intravenous injection; single administration) exerts dose-dependent tumor growth inhibition in mice bearing PC3-S1 prostate cancer xenografts or HL-60 acute myeloid leukemia xenografts^[1].

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

Chemical Information

CAS No. 2417370-67-1
Molecular Weight 1149.29
Formula C₅₇H₆₂F₂N₁₀O₁₀S₂
SMILES

O=C1C2=C3C(C4=CC(CS(C)(=O)=O)=C(C(NCCOC5=CC(CCOCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)=O)=CC(N)=C5)=O)C=C4N(C9=C(C=C(C=N9)F)F)CC3=CN2)=CN1C
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 (287 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]. Dragovich PS, et al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. Journal of medicinal chemistry. 2021 Mar 11;64(5):2576-2607. [Content Brief]

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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.

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100 mg

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