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^[1]. (Pink: CBP/p300 ligand (HY-183817); Blue: Cereblon ligand (HY-183818); Black: linker).

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.

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.

962.05

C₅₀H₅₇F₂N₁₁O₇

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

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

• [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.