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Cat. No.: HY-183802

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PROTAC CBP/P300 Degrader-4

PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC₅₀ of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies.
(Pink: CBP/p300 ligand (HY-183817); Blue: Cereblon ligand (HY-183818); Black: linker).

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

Formula: C₅₀H₅₇F₂N₁₁O₇
Molecular Weight:962.05

Storage:

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

PROTAC CBP/P300 Degrader-4 Chemical Structure

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Fluorescent Dye

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

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

Biological Activity

Description

PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC₅₀ of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies^[1]. (Pink: CBP/p300 ligand (HY-183817); Blue: Cereblon ligand (HY-183818); Black: linker).

IC₅₀ & Target^[1]

CBP

10.2 nM (DC₅₀)

p300

17.4 nM (DC₅₀)

All PROTACs Isoforms :

All Histone Acetyltransferase Isoforms :

In Vitro

PROTAC CBP/P300 Degrader-4 (Compound 28) binds with comparable potency to p300 and CBP bromodomains, and potently binds CRBN^[1].
PROTAC CBP/P300 Degrader-4 (24 h) potently and non-selectively degrades both p300 and CBP proteins in U2OS cells, with DC₅₀ values of 17.4 nM and 10.2 nM respectively^[1].
PROTAC CBP/P300 Degrader-4 (0.01-1 μM; 6 h) forms stable ternary complexes with both p300-CRBN and CBP-CRBN in HEK293 cells with equivalent potency^[1].
PROTAC CBP/P300 Degrader-4 (0.01 μM; 6 h) induces ubiquitination of both p300 and CBP in HEK293 cells, relying on p300^K1050 and CBP^K1086 as key ubiquitination sites^[1].
PROTAC CBP/P300 Degrader-4 (0.01-1 μM; 6 h) recruits the proteasomal subunit PSMD3 to both p300 and CBP in HEK293 cells with equivalent potency^[1].
PROTAC CBP/P300 Degrader-4 (3 nM; 24 h) selectively ubiquitinates p300^K1050 and CBP^K1086 in TMD8 cells^[1].

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

In Vivo

PROTAC CBP/P300 Degrader-4 (Compound 28) (0.05-0.1 mg/kg; i.p.; b.i.d.; up to 6 days) is not tolerated in NCI-H929 multiple myeloma xenografts, resulting in severe toxicity and early mortality^[1].

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

Animal Model:

SCID-beige (female, 2-3 months old)^[1]
Dosage:

0.05 mg/kg; 0.1 mg/kg
Administration:

i.p.; b.i.d.
Result:

Caused severe toxicity, including one death and additional moribund animals by day 6 of treatment.

Chemical Information

Molecular Weight 962.05
Formula C₅₀H₅₇F₂N₁₁O₇
SMILES

O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C(C=N6)=CN6CC(N[C@@H]7CC[C@H](CC7)NC(C8=CC(N(CCC(N9)=O)C9=O)=C%10C(C=CC=C%10)=C8OC)=O)=O)=C5)=C3C1)NC
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]. Asem MS, et al. Discovery of a paralog-selective p300 protein degrader with potent anti-cancer activity in hematological malignancies. Nat Commun. Published online May 6, 2026. [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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC CBP/P300 Degrader-4

All PROTACs Isoforms

All Histone Acetyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC CBP/P300 Degrader-4 Related Classifications

HY-183802 Related Classifications