NHI-2 | LDHA inhibitor

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 from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT

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10 mg$95.00
50 mg$395.00
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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]

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 from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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