1. Metabolic Enzyme/Protease
  2. Lactate Dehydrogenase
  3. LDH-IN-1

LDH-IN-1 

Cat. No.: HY-111108 Purity: 99.84%
Handling Instructions

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.

For research use only. We do not sell to patients.

LDH-IN-1 Chemical Structure

LDH-IN-1 Chemical Structure

CAS No. : 1964515-43-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 691 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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]

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].

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 52 mg/mL (91.12 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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].

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].

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

References
Molecular Weight

570.68

Formula

C₃₀H₂₆N₄O₄S₂

CAS No.

1964515-43-2

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.84%

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LDH-IN-1
Cat. No.:
HY-111108
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LDH-IN-1

Cat. No.: HY-111108