JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.

 

Brand: BCM

 

Signaling Pathways: Chromatin/Epigenetic

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: C[C@@H](C(F)(F)F)N(CC1=CC=C(C=C1)F)C(=O)CN2C(=O)[C@]3(CCC4=C3C=CC(=C4)NC(=O)CCCCCCCCCCCNC5=CC6=C(C=C5)C(=O)N(C6=O)C7CCC(=O)NC7=O)OC2=O  

 

InChIKey: TWCIGBYYSZQAAA-GWWVHQGYSA-N  

 

InChI: InChI=1S/C48H52F4N6O9/c1-29(48(50,51)52)56(27-30-12-14-32(49)15-13-30)41(61)28-57-45(65)47(67-46(57)66)23-22-31-25-34(17-19-37(31)47)54-39(59)11-9-7-5-3-2-4-6-8-10-24-53-33-16-18-35-36(26-33)44(64)58(43(35)63)38-20-21-40(60)55-42(38)62/h12-19,25-26,29,38,53H,2-11,20-24,27-28H2,1H3,(H,54,59)(H,55,60,62)/t29-,38?,47+/m0/s1

 

Attribute
[Chem Name]	12-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]amino]-N-[(5R)-3-[2-[(4-fluorophenyl)methyl-[(2S)-1,1,1-trifluoropropan-2-yl]amino]-2-oxoethyl]-2,4-dioxospiro[1,3-oxazolidine-5,1'-2,3-dihydroindene]-5'-yl]dodecanamide
[Synonym]	JQAD1
[CAS No.]	2417097-18-6
[Formula]	C48H52F4N6O9
[Molecular]	932.97
[Form]	Light yellow to green yellow solid powder
[Storage]	Sealed in dry. -20°C

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