LDH-IN-1
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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- Pureté: 99.84%
- CAS No.: 1964515-43-2
- Formule: C30H26N4O4S2
- Masse moléculaire:570.68
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LDH-IN-1
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Activité biologique
IC50: 32 nM (LDHA), 27 nM (LDHB)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A673 | IC50 |
2.23 μM
Compound: 63
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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
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[PMID: 29120638] |
| A673 | IC50 |
2.9 μM
Compound: 63
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Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay
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[PMID: 29120638] |
| A673 | IC50 |
2454 nM
Compound: 1
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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
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[PMID: 32902275] |
| MIA PaCa-2 | GI50 |
>30 μM
Compound: 5
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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
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[PMID: 36538511] |
| MIA PaCa-2 | IC50 |
1.21 μM
Compound: 63
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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
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[PMID: 29120638] |
| MIA PaCa-2 | IC50 |
3.96 μM
Compound: 63
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Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay
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[PMID: 29120638] |
| MIA PaCa-2 | IC50 |
8448 nM
Compound: 1
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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
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[PMID: 32902275] |
| PANC-1 | GI50 |
>30 μM
Compound: 5
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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
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[PMID: 36538511] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1964515-43-2
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Appearance Solid
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Masse moléculaire 570.68
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Formule C30H26N4O4S2
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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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Journal Impact Factor
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Most Recent
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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 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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.
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.
Pureté et documentation
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Fiche technique (281 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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, 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 |
LDH-IN-1 Related Classifications
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