JQAD1

Research use only, not for human use.

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 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.

Western Blot Analysis Cell Line:MYCN-amplified NB cells Concentration:0.1, 0.5, 1, 3, 5, and 10 μM Incubation Time:24 h Result:Demonstrated a dose-dependent decrease in EP300 expression along with a parallel loss of the H3K27ac modification. Induced selective loss of EP300 expression coincident with cleavage of PARP1, signaling the onset of apoptosis.Western Blot Analysis Cell Line:Kelly NB cells Concentration:1 μM Incubation Time:12, 24, and 36 hours Result:Increased the expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.

Animal Model:NSG mice with Kelly NB cell xenograftsDosage:40 mg/kg Administration:Intraperitoneal injection; daily, for 21 days Result:Suppressed tumor growth and prolonged survival.Animal Model:CD1 miceDosage:10 mg/kg Administration:Intraperitoneal injection (Pharmacokinetic Analysis) Result:Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.

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Chromatin/Epigenetic

Epigenetic Reader Domain

Epigenetic Reader Domain | PROTACs

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2417097-18-6

932.95

C48H52F4N6O9

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (107.19 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years