2417097-18-6
2417097-18-6 structure
- Name: JQAD1
- Chemical Name: JQAD1
- CAS Number: 2417097-18-6
- Molecular Formula: C48H52F4N6O9
- Molecular Weight: 932.95
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2023-05-12 10:16:01
- Modify Date: 2025-08-20 23:33:44
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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[1].
| Name | JQAD1 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| In Vitro | JQAD1在对照组 Kelly NB 细胞而不是 CRBN 敲除细胞中抑制 EP300 的表达，抑制 H3K27ac 修饰，并诱导凋亡[1]。 JQAD1 (0.5 or 1 μM; 6-96 h) 处理导致早期时间依赖性诱导亚 G1 峰，表明 Kelly 和 NGP细胞凋亡死亡[1]。 JQAD1 (1 μM; 12-36 h) 诱导 Kelly NB 细胞凋亡[1]。 JQAD1 (0.5 μM; 24 h) 处理的细胞表现出促凋亡的 BH3 效应物 BIM、BID 和 PUMA 以及促凋亡介质 BAX 及其抑制剂 BCL2 和 MCL1 的上调[1]。 JQAD1 (0.5 and 1 μM; 24 h) 破坏 MYCN 表达[1]。 JQAD1 (0.5 μM; 24 h) 导致染色质上 H3K27ac 缺失[1]。 JQAD1 (1.2 nM-20 μM; 5 days) 具有广泛的 CRBN 依赖的跨癌细胞系抗肿瘤活性[1]。 JQAD1 以时间依赖的方式诱导 EP300 降解，最早在 16 小时[1]。 Western Blot Analysis[1] 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[1] 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. |
| In Vivo | JQAD1 (40 mg/kg; i.p.; 每日一次, 持续 21 天) 抑制 Kelly NB 细胞异种移植的 NSG 小鼠的肿瘤生长[1]。 Animal Model: NSG mice with Kelly NB cell xenografts[1] Dosage: 40 mg/kg Administration: Intraperitoneal injection; daily, for 21 days Result: Suppressed tumor growth and prolonged survival. Animal Model: CD1 mice[1] Dosage: 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. |
| References |
| Molecular Formula | C48H52F4N6O9 |
|---|---|
| Molecular Weight | 932.95 |