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JQAD1
Price range: 210 CAD through 2,432 CAD
Products Details
Product Description
– 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.
Web ID
– T41180
Storage Temperature
– -20℃
Shipping
– Blue Ice
Molecular Formula
– C48H52F4N6O9
Citations
– 1. Zhang D, Ma B, Liu D, et al.Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy.EBioMedicine.2024, 105.
References
– Durbin et al (2021) EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma. Cancer Discov.
CAS Number
– 2417097-18-6
Molecular Weight
– C48H52F4N6O9
Compound Purity
– 0.9975
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
Pathway
– PROTAC|||Chromatin/Epigenetic
Product type
– PROTAC
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
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