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NHI-2 | LDHA inhibitor

NHI-2 (1269802-97-2) is a selective inhibitor of Lactate Dehydrogenase A (LDHA) - IC50 in vitro = 14.7 μM (NADH), 10.5 μM (Pyruvate).1 NHI-2 has also shown cellular growth inhibitory effects against pancreatic cancer cells (PANC-1 cells IC50 = 22.2 μM normoxic and 4.0 μM hypoxic; LPC006 cells IC50 = 17.8 μM normoxic and 1.1 μM hypoxic) with increased efficacy in a cancer cells hypoxic environment.2 LDHA is a key enzyme involved in the Warburg effect and a cancer cells ability to survive in a hypoxic environment.

References/Citations
1) Granchi et al., (2013), Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (MaI) scaffolds; Org. Biomol. Chem., 11 6588
2) Maftouh et al. (2014), Synergistic interaction of novel lactate dehydrogenase inhibitors with gemcitabine against pancreatic cancer cells in hypoxia; Br. J. Cancer, 110 172
3) Granchi et al. (2011), Discovery of N-Hydroxyindole-based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents against Cancer Cells; J. Med. Chem., 54 1599
4) Allison et al. (2014), Identification of LDH-A as a therapeutic target for cancer cell killing via (i) p53/NAD(H)-dependent and (ii) p-53-independent pathways; Oncogenesis, 3 e102
5) Lea et al. (2016) Inhibition of growth by combined treatment with inhibitors of Lactate Dehydrogenase and either Phenformin of Inhibitors of 6-Phosphofructo-2-kinase / Fructose-2,6-bisphosphatase 3; Anticancer Research, 36 1479 [Focus Biomolecules Citation]

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Catalog#  10-4555

$95.00
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CAS:
1269802-97-2
Catalog Number:
10-4555
Activity:
LDHA inhibitor
Chemical Name:
Methyl 1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylate
Molecular Weight:
335.28
Molecular Formula:
C17H12F3NO3
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Confirms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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