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Cat. No.: HY-184453

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PROTAC CBP/EP300 degrader-1

PROTAC CBP/EP300 Degrader-5 is a CBP and EP300 PROTAC degrader. PROTAC CBP/EP300 Degrader-5 relies on the ubiquitin-proteasome pathway to preferentially induce ubiquitination and degradation of EP300 rather than CBP. PROTAC CBP/EP300 Degrader-5 induces G1 phase cell cycle arrest and triggers Apoptosis. PROTAC CBP/EP300 Degrader-5 is applicable to research related to EP300-dependent malignant tumors.
(Pink: EP300 and CBP ligand (HY-184454); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140213)).

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

Formula: C₄₆H₅₀N₁₀O₉
Molecular Weight:886.95

Storage:

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

PROTAC CBP/EP300 degrader-1 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

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

Description

PROTAC CBP/EP300 Degrader-5 is a CBP and EP300 PROTAC degrader. PROTAC CBP/EP300 Degrader-5 relies on the ubiquitin-proteasome pathway to preferentially induce ubiquitination and degradation of EP300 rather than CBP. PROTAC CBP/EP300 Degrader-5 induces G1 phase cell cycle arrest and triggers Apoptosis. PROTAC CBP/EP300 Degrader-5 is applicable to research related to EP300-dependent malignant tumors^[1]. (Pink: EP300 and CBP ligand (HY-184454); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140213)).

IC₅₀ & Target^[1]

EP300

CBP

All PROTACs Isoforms :

All Histone Acetyltransferase Isoforms :

In Vitro

PROTAC CBP/EP300 Degrader-5 (Compound 25a) (10 μM) inhibits EP300 enzyme activity by 25.1% in a cell-free biochemical assay^[1].
PROTAC CBP/EP300 Degrader-5 engages cellular CRBN with an EC₅₀ of 0.62 μM in HEK293T cells^[1].
PROTAC CBP/EP300 Degrader-5 potently and preferentially degrades EP300 (90.8% maximal degradation) over CBP (59.6% maximal degradation) in REH B-ALL cells^[1].
PROTAC CBP/EP300 Degrader-5 (5 μM) mediates EP300 degradation via the ubiquitin-proteasome pathway in REH B-ALL cells, as shown by concentration-dependent rescue of EP300 expression with MG132 (0.1-1 μM) co-treatment^[1].
PROTAC CBP/EP300 Degrader-5 (1-5 μM; 75 h) causes a significant, dose-dependent reduction in REH B-ALL cell proliferation^[1].
PROTAC CBP/EP300 Degrader-5 (5 μM; 24 h) induces apoptosis in REH B-ALL cells, as shown by a significant increase in caspase 3/7 activity^[1].
PROTAC CBP/EP300 Degrader-5 (1-5 μM) causes G₁ cell cycle arrest in REH B-ALL cells, as shown by significant, dose-dependent accumulation of G₁-phase cells and reduction of S+G₂/M-phase cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

REH B-ALL cells
Concentration:

1-5 μM
Incubation Time:

25 h, 50 h, 75 h
Result:

Induced a significant, dose-dependent reduction in viable cell number over the 75 h assay period, with greater inhibition observed at the higher 5 μM concentration.

Apoptosis Analysis^[1]

Cell Line:

REH B-ALL cells
Concentration:

1-5 μM
Incubation Time:

24 h
Result:

Increased caspase 3/7 activity significantly after treatment with 5 μM, indicating induction of apoptosis.

Chemical Information

Molecular Weight 886.95
Formula C₄₆H₅₀N₁₀O₉
SMILES

O=C([C@@H]1N(C(C2(C3=CC=C(OCC4=CN(CCOCCOCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)N=N4)C=C3)CCCC2)=O)CCC1)NC8=CC=CC9=C8C=NN9
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]. Tan K, et al. Targeting histone acetyltransferases EP300/CBP by novel proline-based PROTAC degraders[J]. ACS Medicinal Chemistry Letters, 2026.

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

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PROTAC CBP/EP300 degrader-1

All PROTACs Isoforms

All Histone Acetyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC CBP/EP300 degrader-1 Related Classifications

HY-184453 Related Classifications