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GNE-140 racemate {[allProObj[0].p_purity_real_show]}

货号:A649509

GNE-140 racemate is a LDHA inhibitor.

GNE-140 racemate 化学结构 CAS号:1802977-61-2
GNE-140 racemate 化学结构
CAS号:1802977-61-2
GNE-140 racemate 3D分子结构
CAS号:1802977-61-2
GNE-140 racemate 化学结构 CAS号:1802977-61-2
GNE-140 racemate 3D分子结构 CAS号:1802977-61-2
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GNE-140 racemate 纯度/质量文件 产品仅供科研

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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132H-IDH1, IC50: 70 nM

R132C-IDH1, IC50: 0.16 μM

99%+
SW033291 ++++

15-PGDH, Ki: 0.1 nM

15-PGDH, IC50: 1.5 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 98%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (mouse), IC50: 1 nM

SCD1 (rat), IC50: 3 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 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。

GNE-140 racemate 生物活性

描述 GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor. LDHA is a key glycolytic enzyme, a hallmark of aggressive cancers, and believed to be the major enzyme responsible for pyruvate-to-lactate conversion[2]. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance[3].

GNE-140 racemate 参考文献

[1]US2017001990

[2]Ždralević M, Brand A, Di Ianni L, Dettmer K, Reinders J, Singer K, Peter K, Schnell A, Bruss C, Decking SM, Koehl G, Felipe-Abrio B, Durivault J, Bayer P, Evangelista M, O'Brien T, Oefner PJ, Renner K, Pouysségur J, Kreutz M. Double genetic disruption of lactate dehydrogenases A and B is required to ablate the "Warburg effect" restricting tumor growth to oxidative metabolism. J Biol Chem. 2018 Oct 12;293(41):15947-15961

[3]Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y, Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S, Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T. Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition. Nat Chem Biol. 2016 Oct;12(10):779-86

GNE-140 racemate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

10.02mL

2.00mL

1.00mL

20.04mL

4.01mL

2.00mL

GNE-140 racemate 技术信息

CAS号1802977-61-2
分子式C25H23ClN2O3S2
分子量 499.045
别名
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 18 mg/mL(36.07 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
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