Art. -Nr.: HY-100742A

(R)-GNE-140

20 Cited Publications

Kundenbewertung

Based on 20 publication(s) in Google Scholar

(R)-GNE-140 is a potent inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC₅₀ values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. (R)-GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. (R)-GNE-140 attenuates cardiac hypertrophy, alleviates PM_2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression. (R)-GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer.

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Reinheit: 99.73%
CAS. Nr.: 2003234-63-5
Formel: C₂₅H₂₃ClN₂O₃S₂
Molecular Weight:499.04

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

(R)-GNE-140 Chemical Structure

CAS. Nr.: 2003234-63-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

LDHA

3 nM (IC₅₀)

LDHB

5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.36 μM Compound: Gen140	Antiproliferative activity against human A549 cells assessed as reduction in cell viability at incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability at incubated for 72 hrs by MTT assay	[PMID: 31129449]
A673	IC₅₀	2.63 μM Compound: 3	Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
MG-63	IC₅₀	0.66 μM Compound: 1	Antiproliferative activity against human MG63 cells after 72 hrs by MTT assay Antiproliferative activity against human MG63 cells after 72 hrs by MTT assay	[PMID: 29861142]
MIA PaCa-2	IC₅₀	0.48 μM Compound: Gen140	Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31129449]
MIA PaCa-2	IC₅₀	1.24 μM Compound: 3	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]

In Vitro

(R)-GNE-140 (10 μM; 48 h) reduces intracellular lactate levels, decreases the surface area of neonatal mouse cardiomyocytes, downregulates the expression of cardiac hypertrophy markers, and inhibits multiple histone lysine lactylation modifications, thereby alleviating angiotensin II (Ang II)-induced hypertrophy of neonatal mouse cardiomyocytes (NMCM)^[1].
Pretreatment of mouse RAW264.7 macrophages with (R)-GNE-140 (10 μM; 4 h) inhibits PM_2.5-induced glycolysis, histone lactylation, pro-fibrotic gene expression and cytokine secretion, and partially reverses macrophage-mediated epithelial-mesenchymal transition (EMT) in MLE-12 cells^[2].
(R)-GNE-140 (6-12 h) inhibits MSM-induced Arg1 mRNA expression in MRSA-infected THP1 cells at 6 h and 12 h post-infection^[3].
(R)-GNE-140 (6-12 h) blocks MSM-induced Arg1 protein expression in THP1 cells infected with MRSA at 6 h and 12 h post-infection^[3].
(R)-GNE-140 (Compound 29-R) can inhibit lactate production in human pancreatic cancer MiaPaca2 cells, with its IC₅₀ being 0.67 μM^[4].

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

In Vivo

(R)-GNE-140 (5 mg/kg; i.t.; once every other day; 4 weeks) reduces PM_2.5-induced pulmonary inflammation and fibrosis in male C57BL/6 J mice by inhibiting glycolysis and subsequent histone lactylation^[2].

MedChemExpress (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.

Chemical Information

CAS. Nr. 2003234-63-5
Appearance Solid
Molecular Weight 499.04
Formel C₂₅H₂₃ClN₂O₃S₂
Color Off-white to yellow
SMILES

O=C1N[C@@](C2=CSC=C2)(C3=CC=C(N4CCOCC4)C=C3)CC(O)=C1SC5=CC=CC=C5Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (20)

All Cell Proliferation/Viability AssayHistological Imaging/StainingBio/Physico-chemical AssayIn Vivo Efficacy Study

Sort by:

Journal Impact Factor

Cell Metab

Metabolic-Pathway-Based Subtyping of Triple-Negative Breast Cancer Reveals Potential Therapeutic Targets. [Abstract]

2021 Jan 5;33(1):51-64.e9. PMID: 33181091
Cancer Discov

Mitochondrial-Encoded Complex I Impairment Induces a Targetable Dependency on Aerobic Fermentation in Hürthle Cell Carcinoma of the Thyroid. [Abstract]

2023 Aug 4;13(8):1884-1903. PMID: 37262072

(R)-GNE-140 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Aug 4;13(8):1884-1903. [Abstract]

Viability assay for cells treated with (R)-GNE-140 for 3 days was performed.

(R)-GNE-140 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Aug 4;13(8):1884-1903. [Abstract]

ATP levels in cells treated with (R)-GNE-140 for 4 hours were measured. Concentrations were 0.041, 0.37, 3.33, and 30 μM (R)-GNE-140.
Nat Chem Biol

Lysine L-lactylation is the dominant lactylation isomer induced by glycolysis. [Abstract]

2025 Jan;21(1):91-99. PMID: 39030363
J Exp Clin Cancer Res

H4K79 and H4K91 histone lactylation, newly identified lactylation sites enriched in breast cancer. [Abstract]

2025 Aug 23;44(1):252. PMID: 40849487
Adv Sci (Weinh)

NADH-Reductive Stress Induced by Dihydrolipoamide Dehydrogenase Activation Contributes to Cuproptosis. [Abstract]

2025 Dec 5:e20444. PMID: 41346305

(R)-GNE-140 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 5:e20444. [Abstract]

Viability of SH-SY5Y cells after 24 h treatment with 1 mM AKB, 500 μM CuSO4, and (R)-GNE-140 was measured.
Adv Sci (Weinh)

Mesenchymal Stem Cell-Derived Extracellular Vesicles Modulate the Course of Peritoneal Inflammation Through Metabolic and Epigenetic Regulation. [Abstract]

2025 Nov 26:e08645. PMID: 41293953

(R)-GNE-140 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 26:e08645. [Abstract]

Mice received intraperitoneal injections of 0.1% CG or saline, with or without GNE-140 treatment (5 μg/g body weight, three times weekly), starting on day 7. Representative images of H&E, CCL2, and Ly6c immunostaining in peritoneal tissues were shown.

(R)-GNE-140 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 26:e08645. [Abstract]

Mice received intraperitoneal injections of 0.1% CG or saline, with or without GNE-140 treatment (5 μg/g body weight, three times weekly), starting on day 7. The D/D0 glucose ratio was measured.
Sci Adv

Impaired mitochondrial metabolism is a critical cancer vulnerability for MYC inhibitors. [Abstract]

2025 Jul 18;11(29):eadw5228. PMID: 40668928
Cell Death Dis

The mitochondrial NADH shuttle system is a targetable vulnerability for Group 3 medulloblastoma in a hypoxic microenvironment. [Abstract]

2023 Nov 30;14(11):784. PMID: 38036520
Acta Biomater

Enhancing melanoma therapy by modulating the immunosuppressive microenvironment with an MMP-2 sensitive and nHA/GNE co-encapsulated hydrogel. [Abstract]

2024 Oct 15:188:79-92. PMID: 39241819
Fundam Res

2024 Oct 18.
Mol Cancer Ther

Identification and Characterization of IMD-0354 as a Glutamine Carrier Protein Inhibitor in Melanoma. [Abstract]

2021 May;20(5):816-832. PMID: 33632871
Sci Rep

Deploying the high-throughput virtual screening (HTVS) approach for the identification of new lactate dehydrogenase (LDH) inhibitors with anticancer assets. [Abstract]

2026 Jan 21;16(1):5921. PMID: 41565942
Biochim Biophys Acta Mol Cell Res

Cytoskeletal orchestration of glucose uptake in Sertoli cell to support efferocytosis of apoptotic germ cells. [Abstract]

2023 Apr;1870(4):119434. PMID: 36716822
J Biol Chem

Lactate production is a prioritized feature of adipocyte metabolism. [Abstract]

2020 Jan 3;295(1):83-98. PMID: 31690627
Bone

PGC-1α/LDHA signaling facilitates glycolysis initiation to regulate mechanically induced bone remodeling under inflammatory microenvironment. [Abstract]

2024 Aug:185:117132. PMID: 38789096
Mol Immunol

Methylsulfonylmethane protects against lethal dose MRSA-induced sepsis through promoting M2 macrophage polarization. [Abstract]

2022 Jun;146:69-77. PMID: 35461144
Theriogenology

Lactate metabolism inhibition disrupts goat oocyte meiosis via H3K18la-mediated epigenetic dysregulation. [Abstract]

2026 Jan 15:250:117706. PMID: 41086577
SSRN

2026 Apr 14.
bioRxiv

2024 November 05.
bioRxiv

Forward genetic screens identify mechanisms of resistance to small molecule lactate dehydrogenase inhibitors. [Abstract]

2023 Sep 30:2023.09.30.560315. PMID: 37808702

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (100.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0038 mL

10.0192 mL

20.0385 mL

5 mM

0.4008 mL

2.0038 mL

4.0077 mL

10 mM

0.2004 mL

1.0019 mL

2.0038 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.01 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (5.01 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhao SS, et al. Lactate regulates pathological cardiac hypertrophy via histone lactylation modification. J Cell Mol Med. 2024;28(16):e70022. [Content Brief]

[2]. Li J, et al. Urban airborne PM_2.5 induces pulmonary fibrosis through triggering glycolysis and subsequent modification of histone lactylation in macrophages. Ecotoxicol Environ Saf. 2024;273:116162. [Content Brief]

[3]. Ma W, et al. Methylsulfonylmethane protects against lethal dose MRSA-induced sepsis through promoting M2 macrophage polarization. Mol Immunol. 2022;146:69-77. [Content Brief]

[4]. Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0038 mL	10.0192 mL	20.0385 mL	50.0962 mL
	5 mM	0.4008 mL	2.0038 mL	4.0077 mL	10.0192 mL
	10 mM	0.2004 mL	1.0019 mL	2.0038 mL	5.0096 mL
	15 mM	0.1336 mL	0.6679 mL	1.3359 mL	3.3397 mL
	20 mM	0.1002 mL	0.5010 mL	1.0019 mL	2.5048 mL
	25 mM	0.0802 mL	0.4008 mL	0.8015 mL	2.0038 mL
	30 mM	0.0668 mL	0.3340 mL	0.6679 mL	1.6699 mL
	40 mM	0.0501 mL	0.2505 mL	0.5010 mL	1.2524 mL
	50 mM	0.0401 mL	0.2004 mL	0.4008 mL	1.0019 mL
	60 mM	0.0334 mL	0.1670 mL	0.3340 mL	0.8349 mL
	80 mM	0.0250 mL	0.1252 mL	0.2505 mL	0.6262 mL
	100 mM	0.0200 mL	0.1002 mL	0.2004 mL	0.5010 mL

Keywords

(R)-GNE-140

20 Cited Publications

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(R)-GNE-140

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Antibacterial Compound Library

Glycolysis Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) (R)-GNE-140

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(R)-GNE-140

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Antibacterial Compound Library

Glycolysis Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) (R)-GNE-140

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(R)-GNE-140 Related Classifications

HY-100742A Related Classifications