2. Metabolic Enzyme/Protease Anti-infection Apoptosis NF-κB Immunology/Inflammation
  3. Lactate Dehydrogenase Bacterial Apoptosis Reactive Oxygen Species (ROS)
  4. GNE-140

GNE-140 是一种具有口服活性和选择性的乳酸脱氢酶 (LDH) A、B 和 C 抑制剂，对 LDHA、LDHB、LDHC 的 IC50 分别为 3、5、5 nM。GNE-140 可阻断丙酮酸向乳酸的转化，减少乳酸生成与组蛋白赖氨酸乳酸化，并抑制糖酵解。GNE-140 可减轻心肌肥厚，缓解 PM2.5 诱导的肺部炎症与纤维化，阻断 MRSA 诱导的 Arg1 表达，调控糖酵解及磷酸戊糖通路的代谢物，减少葡萄糖摄取，增加 ROS，诱导癌细胞凋亡 (apoptosis)。GNE-140 可用于病理性心肌肥厚、肺纤维化、MRSA 感染及胰腺癌的相关研究。

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GNE-140

GNE-140 Chemical Structure

CAS No. : 1809794-70-4

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GNE-140 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-140 is an orally active and selective inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC50 values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. GNE-140 attenuates cardiac hypertrophy, alleviates PM2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression, regulates metabolites of glycolysis and the pentose phosphate pathway, reduces glucose uptake, increases ROS, and induces cancer cell apoptosis. GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer[1][2][3][4].

IC50 & Target[4]

LDHA

3 nM (IC50)

LDHB

5 nM (IC50)

体外研究
(In Vitro)

GNE-140 (10 μM; 48 h) 可降低细胞内乳酸水平，减小新生小鼠心肌细胞的表面积，下调心肌肥大标志物的表达，并抑制多种组蛋白赖氨酸乳酸化修饰，从而缓解血管紧张素 II (Ang II) 诱导的新生小鼠心肌细胞 (NMCM) 肥大[1]。
GNE-140 (10 μM; 4 h) 预处理小鼠 RAW264.7 巨噬细胞可抑制 PM2.5 诱导的糖酵解、组蛋白乳酸化、促纤维化基因表达及细胞因子分泌，并可部分逆转巨噬细胞介导的 MLE-12 细胞上皮间质转化 (EMT)[2]。
GNE-140 (6-12 h) 在感染后 6 h 和 12 h 时抑制 MSM 诱导的 MRSA 感染 THP1 细胞中 Arg1 mRNA 的表达[3]。
GNE-140 (6-12 h) 在感染后 6 h 和 12 h 时阻断 MRSA 感染的 THP1 细胞中 MSM 诱导的 Arg1 蛋白表达[3]。
GNE-140 (6-72 h) 会干扰糖酵解过程并抑制人胰腺癌细胞 MIA PaCa-2 的增殖，其乳酸生成抑制作用 (6 h) 的 EC50 为 0.67 μM，增殖抑制作用 (72 h) 的 IC50 为 0.43 μM[4]。
GNE-140 (2 μM; 1-5 d) 可在 MIA PaCa-2 细胞中于 1-2 d 时诱导 Caspase-3 活化，并在 3 d 后诱导细胞死亡；其中不可逆细胞死亡的发生需要持续暴露[4]。
GNE-140 (0-10 μM; 0-48 h) 可调控 MIA PaCa-2 细胞的整体代谢，降低葡萄糖摄取能力 (IC50 = 0.47 μM, 6 h)，提升 ROS 水平 ，并将糖酵解碳流从乳酸转向丙酮酸、丙氨酸及磷酸戊糖途径[4]。
GNE-140 (6-72 h) 可抑制 13% 受试胰腺细胞系 (依赖糖酵解的细胞系) 的增殖，其 IC50 < 5 μM，并且会干扰敏感细胞系和耐药细胞系的糖酵解过程[4]。
GNE-140 (8-10 d) 可从 MIA PaCa-2 细胞中产生稳定的、耐药性超过 100 倍的克隆，这些克隆的代谢方式从糖酵解转变为依赖 OXPHOS 的代谢[4]。
GNE-140 (16-72 h) 可与 AMPK、S6K 或 OXPHOS 抑制剂协同作用以降低 MIA PaCa-2 细胞活力，其中 S6K 抑制作用可阻止与获得性耐药相关的代谢转变[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GNE-140 相关抗体:
体内研究
(In Vivo)

GNE-140 (5 mg/kg；经气管给药；每 2 天 1 次；持续 4 周) 可通过抑制糖酵解及后续的组蛋白乳酸化，减轻 PM2.5 诱导的雄性 C57BL/6 J 小鼠肺部炎症与纤维化[2]。
GNE-140 (100-400 mg/kg；口服；每日 2 次；7-21 天) 可在给药后 1 小时内以剂量依赖的方式短暂调控 MIA PaCa-2 异种移植物中的糖酵解代谢物，但由于清除速度快，在 21 天的体内实验中未表现出肿瘤生长抑制作用[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 J (male, intratracheal instillation of PM2.5 once every other day for 4 weeks)[2]
Dosage: 5 mg/kg
Administration: i.t.; once every other day; 4 weeks (administered 4 h prior to each PM2.5 dose)
Result: Significantly reduced PM2.5-induced peribronchial inflammation scores by 41%.
Reduced collagenous fiber area by 31%.
Reduced macrophage infiltration by 39%.
Decreased lung collagen content by 28%.
Decreased LDH activity by 31%.
Decreased lactate content by 55%.
Attenuated PM2.5-induced up-regulation of histone lactylation.
Restored the expression of epithelial (ZO-1, E-cadherin) and mesenchymal (N-cadherin, vimentin) markers to near control levels.
Animal Model: NCR nu/nu (female, immunocompromised, subcutaneous xenograft model)[4]
Dosage: 100 mg/kg; 200 mg/kg; 400 mg/kg
Administration: p.o.; BID; 7 days; 21 days
Result: Caused dose-dependent reduction in tumor lactate levels relative to vehicle: ~85% (100 mg/kg), ~88% (200 mg/kg), ~90% (400 mg/kg) at 1 hour post-final dose.
Increased tumor pyruvate levels relative to vehicle: ~100% (100 mg/kg), ~200% (200 mg/kg), ~250% (400 mg/kg) at 1 hour post-final dose.
Increased tumor glycerol-3-phosphate levels relative to vehicle: ~200% (100 mg/kg), ~300% (200 mg/kg), ~400% (400 mg/kg) at 1 hour post-final dose.
Eliminated significant metabolite changes across all doses by 6 hours post-final dose.
Showed no tumor growth inhibition relative to vehicle control after 21 days of treatment.
Exhibited no significant body weight loss after 21 days of treatment.
分子量

499.04

Formula

C25H23ClN2O3S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GNE-140 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-1401809794-70-4GNE140GNE 140Lactate DehydrogenaseBacterialApoptosisReactive Oxygen Species (ROS)LDHxenograft tumorslactate dehydrogenase Cpancreatic cellsMRSAcardiac hypertrophymalate dehydrogenases-1lactate dehydrogenase Blactate dehydrogenase Apulmonary fibrosismalate dehydrogenases-2Inhibitorinhibitorinhibit

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