| Identification | Back Directory | [Name]
NHI 2 | [CAS]
1269802-97-2 | [Synonyms]
NHI 2
NHI-2 >=98% (HPLC)
Methyl 1-hydroxy-6-phenyl-4-(trifluoromethyl)-1H-indole-2-carboxylate
1H-Indole-2-carboxylic acid, 1-hydroxy-6-phenyl-4-(trifluoromethyl)-, methyl ester | [Molecular Formula]
C17H12F3NO3 | [MDL Number]
MFCD20264847 | [MOL File]
1269802-97-2.mol | [Molecular Weight]
335.28 |
| Chemical Properties | Back Directory | [Boiling point ]
495.7±55.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 25 mg/ml). | [form ]
solid | [pka]
10?+-.0.58(Predicted) | [color ]
Off-white | [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. | [InChI]
1S/C17H12F3NO3/c1-24-16(22)15-9-12-13(17(18,19)20)7-11(8-14(12)21(15)23)10-5-3-2-4-6-10/h2-9,23H,1H3 | [InChIKey]
YPPFWRWCZNXINO-UHFFFAOYSA-N | [SMILES]
ON(C(C(OC)=O)=C1)C2=C1C(C(F)(F)F)=CC(C3=CC=CC=C3)=C2 |
| Hazard Information | Back Directory | [Description]
NHI 2 is an inhibitor of lactate dehydrogenase A (LDHA; IC50 = 14.7 μM). It is selective for LDHA over LDHB (IC50 = 55.8 μM). It inhibits lactate production in HeLa cells when used at concentrations of 100 and 200 μM. NHI 2 is cytotoxic to HeLa cells (IC50 = 33.4 μM). | [Uses]
NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 μM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 μM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S/G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppress tumor growth in mice[1][2]. | [in vivo]
NHI-2 (0.9 mg/kg; Intra-tumoral; once daily for 15 days) can suppress tumor volume when combined with immune checkpoint inhibitors (ICIs) in murine B78 melanoma tumor model[2].
| Animal Model: | C57BL/6 female mice (6-8 weeks) were intradermally implanted with B78 syngeneic melanoma cells[2] | | Dosage: | 0.9 mg/kg | | Administration: | Intra-tumoral (IT) via percutaneous needle puncture; once daily for 15 days | | Result: | Suppressed tumor volume when combined with checkpoint inhibitors (ICIs). |
| [storage]
Store at +4°C | [References]
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] |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|