9-ING-41是一种强效的糖原合成酶激酶-3(GSK-3)抑制剂,具有抗肿瘤活性,能够诱导细胞凋亡并通过靶向中心体和微管结合 GSK3β 引起有丝分裂前期的细胞周期停滞。
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产品名称 | GSK-3 ↓ ↑ | GSK-3α ↓ ↑ | GSK-3β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD2858 |
+
GSK-3, IC50: 68 nM |
99% | |||||||||||||||||
Bikinin | ✔ | 99%+ | |||||||||||||||||
GSK 3 Inhibitor IX |
++++
GSK-3, IC50: 5 nM |
99%+ | |||||||||||||||||
AZD1080 |
+++
GSK-3α, IC50: 6.9 nM |
++
GSK-3β, IC50: 31 nM |
99%+ | ||||||||||||||||
BIO-acetoxime |
+++
GSK-3α, IC50: 10 nM |
+++
GSK-3β, IC50: 10 nM |
95% | ||||||||||||||||
SB-216763 |
++
GSK-3α, IC50: 34.3 nM |
++
GSK-3β, IC50: ~34.3 nM |
98% | ||||||||||||||||
SB 415286 |
+
GSK-3α, IC50: 78 nM |
+
GSK-3β, IC50: ~78 nM |
99%+ | ||||||||||||||||
CHIR-98014 |
++++
GSK-3α, IC50: 0.65 nM |
++++
GSK-3β, IC50: 0.58 nM |
98% | ||||||||||||||||
LY2090314 |
++++
GSK-3α, IC50: 1.5 nM |
++++
GSK-3β, IC50: 0.9 nM |
99%+ | ||||||||||||||||
CHIR 99021 |
+++
GSK-3α, IC50: 10 nM |
++++
GSK-3β, IC50: 6.7 nM |
99%+ | ||||||||||||||||
TDZD-8 |
+
GSK-3β, IC50: 2 μM |
99%+ | |||||||||||||||||
Indirubin |
+
GSK-3β, IC50: 0.6 μM |
98% | |||||||||||||||||
IM-12 |
++
GSK-3β, IC50: 53 nM |
98% | |||||||||||||||||
TWS119 |
++
GSK-3β, IC50: 30 nM |
99% | |||||||||||||||||
1-Azakenpaullone |
+++
GSK-3β, IC50: 18 nM |
99%+ | |||||||||||||||||
AR-A014418 |
++
GSK-3β, Ki: 38 nM |
99%+ | |||||||||||||||||
Tideglusib |
+
GSK-3β, IC50: 60 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Glycogen synthase kinase-3 (GSK-3), a serine/threonine kinase, is a master regulator of neural progenitor homeostasis, integrating multiple proliferation, and differentiation signals, and thus has been focused on as a potential target in neuroblastoma. 9-ING-41, a potent and selective small-molecule GSK-3 inhibitor, is active in neuroblastoma. In cell viability assay, 9-ING-41 inhibited the growth of SK-N-DZ and SK-N-BE(2) neuroblastoma cells with GI50s among 50–100 nM. 9-ING-41 (0.1–1 µM) inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells[1]. Teretment with low doses of 9-ING-41 for 48 hours specifically induced lymphoma cell apoptosis without affecting normal lymphocytes[2]. In vivo, 9-ING-41 (70 mg/kg) potentiated the effects of CPT-11 (5 mg/kg) in growth inhibition of neuroblastoma xenograft tumors[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.37mL 2.47mL 1.24mL |
24.73mL 4.95mL 2.47mL |
CAS号 | 1034895-42-5 |
分子式 | C22H13FN2O5 |
分子量 | 404.347 |
别名 | Elraglusib |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 50 mg/mL(123.66 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |