JQAD1
Product Specifications
CAS Number
2417097-18-6
Target
PROTACs, Apoptosis, Epigenetic Reader Domain, Caspase, PARP, Histone Acetyltransferase
Related Pathways
PROTAC, Apoptosis, Chromatin/Epigenetic, Proteases/Proteasome, DNA Damage/DNA Repair
Purity
0.9975
Bioactivity
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.
Smiles
O=C1[C@@]2(C=3C(CC2)=CC(NC(CCCCCCCCCCCNC=4C=C5C(=CC4)C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=O)=CC3)OC(=O)N1CC(N(CC7=CC=C(F)C=C7)[C@H](C(F)(F)F)C)=O
Molecular Formula
C48H52F4N6O9
Molecular Weight
932.95
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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