PROTAC CBP/P300 Degrader-1

• CAT Number: I044621
• CAS Number: 2484739-48-0
• Molecular Formula: C46H53F2N11O6
• Molecular Weight: 893.98
• Purity: ≥95%
• Synonyms: 3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-1-[1-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexanoyl]piperidin-4-yl]-N-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
• InChI: InChI=1S/C46H53F2N11O6/c1-49-46(65)56-21-16-35-33(26-56)42(57-18-7-8-27-22-31(28-24-51-54(2)25-28)32(41(47)48)23-37(27)57)53-59(35)29-14-19-55(20-15-29)39(61)11-4-3-5-17-50-34-10-6-9-30-40(34)45(64)58(44(30)63)36-12-13-38(60)52-43(36)62/h6,9-10,22-25,29,36,41,50H,3-5,7-8,11-21,26H2,1-2H3,(H,49,65)(H,52,60,62)
• InChIKey: KOXRGDZBEAJAKE-UHFFFAOYSA-N
• SMILES: CNC(=O)N1CCC2=C(C1)C(=NN2C3CCN(CC3)C(=O)CCCCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)N7CCCC8=CC(=C(C=C87)C(F)F)C9=CN(N=C9)C

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines[1].
PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC50=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%)[1].
PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell lines (IC50s ranging from 0.1-141.4 nM for HEL, NOMO-1, MOLM-13, HL-60, MEG-01, MM.IS, MM.1R, NCL-H929, RPM-8226, AMO-1, WSU-DLCL2, Karpas-422, Pfeiffer, SU-DHL-1, LNCap clone FGC, VCap; 22RV1, NCI-H520, NCI-H703, LK-2, MCE-7, and SK-BR-3 cells)[1].

Reference

[1]. Jing Liu, et al. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use. WO2020173440A1.