1. Metabolic Enzyme/Protease
  2. Lactate Dehydrogenase
  3. (R)-GNE-140

(R)-GNE-140 

Cat. No.: HY-100742A Purity: 98.50% ee.: 99.43%
Handling Instructions

(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

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

(R)-GNE-140 Chemical Structure

(R)-GNE-140 Chemical Structure

CAS No. : 2003234-63-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 242 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 370 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

IC50 & Target

IC50: 3 nM (LDHA), 5 nM (LDHB)[1]

In Vitro

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 shows inhibitory effect on two chondrosarcoma (bone) cancer cell lines that harbor IDH1 mutations, with IC50 of 0.8 μM[1].

In Vivo

(R)-GNE-140 (5 mg/kg) has high bioavailability in mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater exposure.

Molecular Weight

499.04

Formula

C₂₅H₂₃ClN₂O₃S₂

CAS No.

2003234-63-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

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 : ≥ 14.43 mg/mL (28.92 mM)

H2O : < 0.1 mg/mL (insoluble)

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

  • 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

  • 3.

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

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

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

(R)-GNE-140Lactate DehydrogenaseLDHInhibitorinhibitorinhibit

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Product name:
(R)-GNE-140
Cat. No.:
HY-100742A
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