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JQAD1

CAS No. : 2417097-18-6

MCE 站：JQAD1

产品活性：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。

研究领域：PROTAC  |  Epigenetics  |  Apoptosis  |  Cell Cycle/DNA Damage

作用靶点：PROTACs  |  Histone Acetyltransferase  |  Apoptosis  |  Caspase  |  PARP

In Vitro: JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, ａnd induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells.
JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly ａnd NGP cells.
JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis.
JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, ａnd PUMA together with the proapoptotic mediator BAX ａnd its inhibitors BCL2 ａnd MCL1.
JQAD1 (0.5 ａnd 1 μM; 24 h) disrupts MYCN expression.
JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin.
JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines.
JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours.

In Vivo: JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts.

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