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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 5 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
O=C(C1=CC=NC=C1)/C=C/C2=CN=CC=C2
InChI
1S/C13H10N2O/c16-13(12-5-8-14-9-6-12)4-3-11-2-1-7-15-10-11/h1-10H/b4-3+
InChI key
UOWGYMNWMDNSTL-ONEGZZNKSA-N
应用
3PO已用作6-磷酸果糖-2-激酶/果糖-2，6-二磷酸酶3(PFKFB3)抑制剂，用于研究其对结直肠癌细胞中细胞活力丧失、凋亡和坏死性凋亡的影响。它还用作 PFKFB3 抑制剂来抑制糖酵解，并研究其对曲贝替定（TRB）和鲁比卡丁（LUR）处理的人巨噬细胞（hMF）中细胞活力和产生活性氧（ROS）的影响。
生化/生理作用
3PO 是一种有效的选择性 PFKFB3 抑制剂（6-磷酸果糖-2-激酶/果糖-2,6-双磷酸酶），PFKFB3 可降低糖酵解流量并抑制葡萄糖摄取。3PO 对转化细胞具有选择性抑制细胞生长的作用，并抑制荷瘤小鼠肿瘤的生长。
通过3PO介导的PFKFB3阻断对糖酵解的抑制减少了癌症和炎症的病理性血管生成。3PO有助于调节内皮细胞的增殖和迁移。它还减少了内皮细胞的促炎激活和 体内实验性炎症。因此，它可能是一种治疗慢性炎症的潜在疗法。其在人内皮细胞中的抗炎活性与其靶PFKFB3无关。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Siyuan Yan et al.
American journal of cancer research, 11(5), 2062-2080 (2021-06-08)
Cancer cells prone to utilize aerobic glycolysis other than oxidative phosphorylation to sustain its continuous cell activity in the stress microenvironment. Meanwhile, cancer cells generally suffer from genome instability, and both radiotherapy and chemotherapy may arouse DNA strand break, a
Yi-Jia Li et al.
Cell reports, 39(9), 110870-110870 (2022-06-02)
Overcoming resistance to chemotherapies remains a major unmet need for cancers, such as triple-negative breast cancer (TNBC). Therefore, mechanistic studies to provide insight for drug development are urgently needed to overcome TNBC therapy resistance. Recently, an important role of fatty
Krzysztof Kotowski et al.
Anticancer research, 40(5), 2613-2625 (2020-05-06)
The occurrence of BRAFV600E mutation causes an up-regulation of the B-raf kinase activity leading to the stabilization of hypoxia-inducible factor 1-alpha (HIF-1α) - the promoter of the 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) enzyme. The aim of the study was to examine the
Husniye Kantarci et al.
eLife, 9 (2020-04-28)
Recent studies indicate that many developing tissues modify glycolysis to favor lactate synthesis (Agathocleous et al., 2012; Bulusu et al., 2017; Gu et al., 2016; Oginuma et al., 2017; Sá et al., 2017; Wang et al., 2014; Zheng et al.
Adrián Povo-Retana et al.
Cancers, 12(10) (2020-10-24)
Tumor-associated macrophages (TAMs) play a crucial role in suppressing the immunosurveillance function of the immune system that prevents tumor growth. Indeed, macrophages can also be targeted by different chemotherapeutic agents improving the action over immune checkpoints to fight cancer. Here
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