3109024-12-3
Chemical Structure
PROTAC CBP/p300/BRD4 Degrader-1
- CAS. Nr.: 3109024-12-3
- Formula:C41H42F3N7O7
- Molecular Weight:801.81
InChIKey: ROJZCTYTVQNTGW-UHFFFAOYSA-N
SMILES: O=C1N(C(C2=C1C=CC(N3CCC(CC3)C(N4CCC(CC4)C5=NC6=CC=C(C=C6N5CCOC(F)(F)F)C(C=C7C)=CN(C7=O)C)=O)=C2)=O)C(C(N8)=O)CCC8=O
Biological Activity: PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer[1].
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PROTAC CBP/p300/BRD4 Degrader-1 | PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer. | |||||||||||||||||||||
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