PKM2-IN-1

目录号: HY-103617 纯度: 99.79%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

PKM2-IN-1 (compound 3k) 是一种丙酮酸激酶 M2 (PKM2) 抑制剂，其 IC₅₀ 值为 2.95 μM。

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PKM2-IN-1 Chemical Structure

CAS No. : 94164-88-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
1 mg	￥320	In-stock
5 mg	￥800	In-stock
10 mg	￥1200	In-stock
25 mg	￥2640	In-stock
50 mg	￥4200	In-stock
100 mg	现货	询价
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 16 篇科研文献

PKM2-IN-1 相关产品

•相关化合物库:

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95 μM^[1].

IC₅₀ & Target

IC50: 2.95 μM (PKM2)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BEAS-2B	IC₅₀	18.46 μM Compound: 3k	Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 48 hrs by MTS assay Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 48 hrs by MTS assay	[PMID: 28688274]
HCT-116	IC₅₀	0.18 μM Compound: 3k	Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay	[PMID: 28688274]
HeLa	IC₅₀	0.29 μM Compound: 3k	Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay	[PMID: 28688274]
NCI-H1299	IC₅₀	1.56 μM Compound: 3k	Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay	[PMID: 28688274]
NCI-H1299	IC₅₀	2.01 μM Compound: 3k	Antiproliferative activity against human NCI-H1299 cells after 48 hrs in presence of PKM2 activator FBP by MTS assay Antiproliferative activity against human NCI-H1299 cells after 48 hrs in presence of PKM2 activator FBP by MTS assay	[PMID: 28688274]

体外研究
(In Vitro)

PKM2-IN-1（Compound 3k）是一种丙酮酸激酶 M2 (PKM2) 抑制剂，IC₅₀ 为 2.95 μM。结果表明，大多数测试化合物表现出一定程度的 PKM2 抑制作用，并且某些化合物（例如 PKM2-IN-1（Compound 3k）和 6d）比阳性对照紫草素表现出更强的活性。PKM2-IN-1 对 PKM2 表现出剂量依赖性抑制作用，对 PKM1 和 PKL 的抑制作用与紫草素类似。PKM2-IN-1 对 HCT116 和 Hela 细胞的 IC₅₀ 值分别范围为 0.18 μM 和 0.29 μM。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

345.48

Formula

C₁₈H₁₉NO₂S₂

CAS 号

94164-88-2

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 4 mg/mL (11.58 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8945 mL	14.4726 mL	28.9452 mL
5 mM	0.5789 mL	2.8945 mL	5.7890 mL
10 mM	0.2895 mL	1.4473 mL	2.8945 mL

查看完整储备液配制表

* 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (72.36 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.79%

选择批次：

Data Sheet (626 KB) SDS (393 KB)

COA (285 KB) HNMR (251 KB) RP-HPLC (251 KB) LCMS (100 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ning X, et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. Eur J Med Chem. 2017 Sep 29;138:343-352. [Content Brief]

Cell Assay ^[1]	Cell lines (HCT116, Hela, H1299, BEAS-2B) are cultured in RPMI 1640 containing 9% fetal bovine serum (FBS) at 37°C in 5% CO₂. Cell viability is detected with the MTS assay according to the manufacturer's instructions. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h, the cells are treated with different concentration of tested compound (including PKM2-IN-1) or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3 h. Absorbance of each well is determined by a microplate reader at a 490 nm wavelength. The IC₅₀ values are calculated using Prism Graphpad software of the triplicate experiment^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Ning X, et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. Eur J Med Chem. 2017 Sep 29;138:343-352. [Content Brief]

Cell Assay
^[1]

Cell lines (HCT116, Hela, H1299, BEAS-2B) are cultured in RPMI 1640 containing 9% fetal bovine serum (FBS) at 37°C in 5% CO₂. Cell viability is detected with the MTS assay according to the manufacturer's instructions. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h, the cells are treated with different concentration of tested compound (including PKM2-IN-1) or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3 h. Absorbance of each well is determined by a microplate reader at a 490 nm wavelength. The IC₅₀ values are calculated using Prism Graphpad software of the triplicate experiment^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Ning X, et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. Eur J Med Chem. 2017 Sep 29;138:343-352. [Content Brief]

PKM2-IN-1 相关分类

Cancer

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8945 mL	14.4726 mL	28.9452 mL	72.3631 mL
	5 mM	0.5789 mL	2.8945 mL	5.7890 mL	14.4726 mL
	10 mM	0.2895 mL	1.4473 mL	2.8945 mL	7.2363 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKM2-IN-194164-88-2Pyruvate KinaseInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

PKM2-IN-1

Customer Review

MCE 顾客使用本产品发表的 16 篇科研文献