计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
FX-11 是一种有效的、选择性的、可逆的和竞争性的乳酸脱氢酶 A (LDHA) 抑制剂，Ki 为 8 μM。FX-11 可降低 ATP 水平，诱导氧化应激、ROS 生成和细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植中显示出抗肿瘤 (antitumor) 活性。
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A ( LDHA ) specific inhibitor, with a K i of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts
In Vitro
FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase. ?\nFX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells. ?\nFX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: P493 cells Concentration: 9 μM Incubation Time: 24 h, 48 h Result: Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase. Cell Proliferation AssayCell Line: BxPc-3 and MIA PaCa-2 cells Concentration: 0-100 µM Incubation Time: 72 h Result: Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC 50 values of 49.27 µM and 60.54 µM for BxPc-3 and MIA PaCa-2 cells, respectively.
In Vivo
FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth. ?\nFX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)Dosage: 42 µg/mouse (2.1 mg/kg) Administration: IP; daily for 10-14 days Result: Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression. Animal Model: Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)Dosage: 2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46 Administration: IP (100 µL), daily, for 3 weeks Result: Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth.
IC50& Target:IC50: 23.3 μM (LDHA in HeLa cell)
规格
规格或纯度
10mM in DMSO
英文名称
FX-11
生化机理
FX-11 是一种强效、选择性、可逆和竞争性的乳酸脱氢酶 A（LDHA）特异性抑制剂，其 K i 为 8 μM。FX-11 能有效激活 PKM2（丙酮酸激酶 M2）。FX-11 可降低 ATP 水平，诱导氧化应激和 ROS 生成。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CCCC1=C(C(=C(C2=C1C=C(C(=C2)CC3=CC=CC=C3)C)C(=O)O)O)O
PubChem CID
分子量
350.41
技术文档
高级数据
关联靶点（人）
LDHB
Tchem
L-乳酸脱氢酶B链(L-lactate dehydrogenase B chain)
(3 活性数据)
LDHA
Tchem
L-乳酸脱氢酶A链(L-lactate dehydrogenase A chain)
(2 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
溶液计算器
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