Art. -Nr.: HY-111108

LDH-IN-1

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC₅₀s of 32 and 27 nM for LDHA and LDHB, respectively.

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Reinheit: 99.84%
CAS. Nr.: 1964515-43-2
Formel: C₃₀H₂₆N₄O₄S₂
Molecular Weight:570.68

Speicherung:

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

LDH-IN-1 Chemical Structure

CAS. Nr.: 1964515-43-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC₅₀s of 32 and 27 nM for LDHA and LDHB, respectively.

IC₅₀ & Target

IC50: 32 nM (LDHA), 27 nM (LDHB)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A673	IC₅₀	2.23 μM Compound: 63	Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
A673	IC₅₀	2.9 μM Compound: 63	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	2454 nM Compound: 1	Cytotoxicity against human A673 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay	[PMID: 32902275]
MIA PaCa-2	GI₅₀	>30 μM Compound: 5	Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by WST-8 assay Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by WST-8 assay	[PMID: 36538511]
MIA PaCa-2	IC₅₀	1.21 μM Compound: 63	Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	3.96 μM Compound: 63	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	8448 nM Compound: 1	Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay	[PMID: 32902275]
PANC-1	GI₅₀	>30 μM Compound: 5	Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 72 hrs by WST-8 assay Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 72 hrs by WST-8 assay	[PMID: 36538511]

In Vitro

LDH-IN-1 exhibits low nM inhibition of both LDHA and LDHB (IC₅₀=32, 27 nM, respectively), submicromolar inhibition of lactate production, and inhibition of lactate in MiaPaCa2 pancreatic cancer and A673 sarcoma cells (IC₅₀=0.517, 0.854μM, respectively). LDH-IN-1 inhibits the growth of MiaPaCa2 pancreatic cancer and A673 sarcoma cells with IC₅₀s of 2.23 and 1.21 μM). Dose?response treatment of MiaPaCa-2 cells with LDH-IN-1 shows effects on cellular proliferation at concentrations as low as 250 nM and with nearly complete arrest of cell growth at 20 μM^[1].

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

In Vivo

LDH-IN-1 shows clearance values that far exceed hepatic blood flow (HBF) in mouse species (90 mL/min/kg), with in vivo clearances of 227 mL/min/kg^[1].

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

Chemical Information

CAS. Nr. 1964515-43-2
Appearance Solid
Molecular Weight 570.68
Formel C₃₀H₂₆N₄O₄S₂
Color White to off-white
SMILES

O=S(C1=CC=C(CC2=C(N(C3=NC(C(O)=O)=CS3)N=C2C4=CC=CC(C5=CC=CC=C5)=C4)CC6CC6)C=C1)(N)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (2)

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Cell Rep

Tumor metabolite lactate promotes tumorigenesis by modulating MOESIN lactylation and enhancing TGF-β signaling in regulatory T cells. [Abstract]

2022 Jun 21;39(12):110986. PMID: 35732125
bioRxiv

2024 November 05.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 52 mg/mL (91.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.7523 mL

8.7615 mL

17.5230 mL

5 mM

0.3505 mL

1.7523 mL

3.5046 mL

10 mM

0.1752 mL

0.8761 mL

1.7523 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.17 mg/mL (3.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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% Corn Oil

Solubility: ≥ 2.17 mg/mL (3.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 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 (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Protokoll

Cell Assay^[1]

A673 and MiaPaCa-2 cellsA673 and MiaPaCa-2 cells are cultured and plated in 1536-well white solid tissue culture plates. A 1536-well pintool dispenser outfitted with 20 nL pins is used to transfer 23 nL of LDH-IN-1 in DMSO to the 1536-well assay plates. After a 48 h incubation at 37°C, 2.5 μL of CellTiter-Glo is dispensed into each well using a BioRAPTR FRD dispenser. Plates are incubated at room temperature for 10 min, transferred to a ViewLux microplate imager, and the ATP-coupled luminescence is measured using a 1 s exposure^[1].

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

Animal Administration^[1]

Mice^[1]

Male CD1 mice approximately 6−8 weeks of age and a weight of approximately 20−30 g, are dosed with LDH-IN-1 at 2 mg/ kg (iv) and 50 mg/kg (po). Each cohort had three mice, and plasma is collected at 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24h postdose for iv and 15 min 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h for po. Approximately 0.025 mL of blood is collected via the dorsal metatarsal vein at each time point. Blood samples are then transferred into plastic microcentrifuge tubes containing heparin−Na as anticoagulant. Samples are then centrifuged at 4000g for 5 min at 4 °C to obtain plasma. Plasma samples are then stored in polypropylene tubes, quickly frozen, and kept at −75 °C until analyzed by LC/MS/MS^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Rai G, et al. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem. 2017 Nov 22;60(22):9184-9204. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7523 mL	8.7615 mL	17.5230 mL	43.8074 mL
	5 mM	0.3505 mL	1.7523 mL	3.5046 mL	8.7615 mL
	10 mM	0.1752 mL	0.8761 mL	1.7523 mL	4.3807 mL
	15 mM	0.1168 mL	0.5841 mL	1.1682 mL	2.9205 mL
	20 mM	0.0876 mL	0.4381 mL	0.8761 mL	2.1904 mL
	25 mM	0.0701 mL	0.3505 mL	0.7009 mL	1.7523 mL
	30 mM	0.0584 mL	0.2920 mL	0.5841 mL	1.4602 mL
	40 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	50 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8761 mL
	60 mM	0.0292 mL	0.1460 mL	0.2920 mL	0.7301 mL
	80 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5476 mL

Keywords

LDH-IN-1

2 Cited Publications

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LDH-IN-1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LDH-IN-1

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDH-IN-1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LDH-IN-1

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDH-IN-1 Related Classifications

HY-111108 Related Classifications