NHI 2 (Synonyms:NHI 2)
目录号 : KCM10892 CAS No. : 1269802-97-2 纯度 : ≥98%
NHI 2 is an inhibitor of lactate dehydrogenase A (LDHA; IC = 14.7 µM). It is selective for LDHA over LDHB (IC = 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 (IC = 33.4 µM).
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生物活性

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 and 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 suppresses tumor growth in murine B78 melanoma tumor model.

体外研究

NHI-2 (50-200 μM, 8 h) inhibits lactate production in HeLa cells [1].
NHI-2 (12-40 μM, 72 h) inhibits the proliferation of B78 cells [2].
The EC50 of NHI-2 (0.1-100 μM, 48 h) on B78 cells was 32 μM [2].
The combination of NHI-2 (40 μM, 24 h) with 30 or 60 mM Oxamate (Oxa) (HY-W013032A) enhances apoptosis [2].
NHI-2 (40 μM, 24 h) induces cell cycle arrest at the S/G2 phase [2].
NHI-2 affects extracellular acidification rate (ECAR) (12-26 μM, 80 min) and ATP (18 μM, 24 h) production, and synergizes with Oxa [2].
As a competitive inhibitor of NADH, NHI-2 not only affects glycolysis but also influences mitochondrial metabolism and the NAD+/NADH balance [2].

 

Cell Viability Assay

Cell Line: B78-D14 melanoma cells
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: The EC50 values of 32 μM.

Cell Proliferation Assay

Cell Line: B78-D14 melanoma cells
Concentration: 12, 18, 26, 40, μM
Incubation Time: 72 hours
Result: Exhibited no effect on B78 cell proliferation at lower concentrations. but decreased cell proliferation at concentrations beginning from 26 μM.

Apoptosis Analysis

Cell Line: B78-D14 melanoma cells
Concentration: 40 μM
Incubation Time: 24 hours
Result: Increased cell apoptosis when combined with either 30 or 60 mM Oxa

Cell Cycle Analysis

Cell Line: B78-D14 melanoma cells
Concentration: 40 μM
Incubation Time: 24 hours
Result: Led to an increased cell population in the S and G2 phases.
体内研究

The combination of NHI-2 (0.9 mg/kg; intratumoral injection; once daily for 15 days) with immune checkpoint inhibitors can inhibit tumor volume in the B78 melanoma tumor model in mice [2].

 

Animal Model: C57BL/6 female mice (6-8 weeks) were intradermally implanted with B78 syngeneic melanoma cells
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).
 
分子式
C17H12F3NO3
分子量
335.2773296
CAS号
1269802-97-2
中文名称
NHI 2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (74.56 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9826 mL 14.9129 mL 29.8258 mL
5 mM 0.5965 mL 2.9826 mL 5.9652 mL
10 mM 0.2983 mL 1.4913 mL 2.9826 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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