JQAD1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JQAD1 是 CRBN 依赖的 PROTAC，选择性靶向 EP300 进行降解。JQAD1 抑制 EP300 表达和 H3K27ac 修饰。JQAD1 诱导细胞凋亡 (apoptosis)。JQAD1 可用于癌症研究。

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 中的溶解度 : 100 mg/mL (107.19 mM; 超声助溶 )

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