(R)-GNE-140

Name: (R)-GNE-140
Brand: MedChemExpress
SKU: HY-100742A
Rating: 5.0 (19 reviews)

Art. -Nr.: HY-100742A Reinheit: 99.73%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

(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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CAS. Nr. : 2003234-63-5

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Kostenlose Probe (0.1 - 0.2 mg)	Jetzt bewerben
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 19 publication(s) in Google Scholar

Other Forms of (R)-GNE-140:

GNE-140 racemate In-stock
(S)-GNE-140 In-stock
(R)-GNE-140 (Standard) Angebot einholen

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

Cell Proliferation/Viability Assay

Histological Imaging/Staining

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: (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.

: (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.

: (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.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biologische Aktivität
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Beschreibung

IC₅₀ & Target

LDHA

3 nM (IC₅₀)

LDHB

5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.36 3 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]
A549	IC₅₀	0.36 3 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 3 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]
A673	IC₅₀	2.63 3 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]
A549	IC₅₀	0.36 3 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 3 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 3 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]
MG-63	IC₅₀	0.66 3 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 3 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	0.48 3 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 3 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]
MIA PaCa-2	IC₅₀	1.24 3 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]
MG-63	IC₅₀	0.66 3 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 3 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 3 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.

Molekulargewicht

499.04

Formel

C₂₅H₂₃ClN₂O₃S₂

CAS. Nr.

2003234-63-5

Appearance

Solid

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

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Verdünnungsrechner

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.73%

Select Batch:

Data Sheet (287 KB) SDS (396 KB)

COA (260 KB) HNMR (274 KB) LCMS (94 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]

Complete Stock Solution Preparation Table

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

(R)-GNE-140 Related Classifications

Help & FAQs

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:

(R)-GNE-1402003234-63-5Lactate DehydrogenaseBacterialLDHInhibitorinhibitorinhibit

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(R)-GNE-140

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Other Forms of (R)-GNE-140:

(R)-GNE-140 Related Antibodies

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

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

(R)-GNE-140 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

(R)-GNE-140 Related Classifications

Keywords:

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