NHI 2 - CAS:1269802-97-2

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NHI 2 (Synonyms:NHI 2)

目录号 : KCM10892 CAS No. : 1269802-97-2 纯度 : ≥98%

Data Sheet 产品使用指南

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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1mg		In-stock
5mg		In-stock
10mg		In-stock

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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.

IC₅₀&Target

LDHB LDHA

55.8 μM (IC50) 14.7 μM (IC50)

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。

纯度： ≥98%

Data Sheet

产品使用指南

[1]. Granchi C, et al. Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds. Org Biomol Chem. 2013;11(38):6588-6596.

[2]. Gurel Z, et al. Metabolic modulation of melanoma enhances the therapeutic potential of immune checkpoint inhibitors. Front Oncol. 2024 Oct 1;14:1428802.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器