TEPP-46 (Synonyms: ML-265)

目录号: HY-18657 纯度: 99.93%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

TEPP-46 (ML-265) 是一种有效，选择性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活剂，AC₅₀ 值为 92 nM，对 PKM1，PKL 和 PKR 作用较小或没有作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

TEPP-46 Chemical Structure

CAS No. : 1221186-53-3

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥963	In-stock
5 mg	￥875	In-stock
10 mg	￥1320	In-stock
50 mg	￥2700	In-stock
100 mg	￥4250	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 38 篇科研文献

: TEPP-46 purchased from MCE. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690. [Abstract]; Analysis of enzymatic activity of PKM2. Protein level of PKM2 is analyzed using Western Blotting.

: TEPP-46 purchased from MCE. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690. [Abstract]; Immunofluorescence of PKM2 in DCs. When added TEPP-46 to prevent the dissociation of PKM2 tetramers, LPS-induced accumulation of nuclear PKM2 as well as IL-12 expression is diminished.

TEPP-46 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC₅₀ of 92 nM, showing little or no effect on PKM1, PKL and PKR^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 100 μM Compound: TEPP-46	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
C6	IC₅₀	81.8 μM Compound: TEPP-46	Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]
HCT-116	IC₅₀	89.91 μM Compound: TEPP-46	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
HepG2	IC₅₀	> 100 μM Compound: TEPP-46	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
HT-29	IC₅₀	> 100 μM Compound: TEPP-46	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
MDA-MB-231	IC₅₀	> 100 μM Compound: TEPP-46	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
NIH3T3	IC₅₀	56.58 μM Compound: TEPP-46	Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]
SF-126	IC₅₀	88.98 μM Compound: TEPP-46	Antiproliferative activity against human SF126 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SF126 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]
SW480	IC₅₀	92.95 μM Compound: TEPP-46	Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
U-118-MG	IC₅₀	85 μM Compound: TEPP-46	Antiproliferative activity against human U118MG cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human U118MG cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]
U-251	IC₅₀	65.43 μM Compound: TEPP-46	Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]
U2OS	IC₅₀	> 100 μM Compound: TEPP-46	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34847663]
U-87MG ATCC	IC₅₀	86.3 μM Compound: TEPP-46	Antiproliferative activity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31977207]

体外研究
(In Vitro)

TEPP-46 和 DASA-58 通过类似于内源性激活剂 FBP 的机制激活 PKM2。用 TEPP-46 或 DASA-58 预处理细胞可防止过钒酸盐诱导的 PKM2 活性抑制。TEPP-46 还会诱导细胞内乙酰辅酶 A、乳酸、核糖磷酸和丝氨酸水平降低^[1]。
TEPP-46 抑制 LPS 诱导的 Hif-1α 和 IL-1β，以及一系列其他 Hif-1α 依赖性基因的表达。TEPP-46 处理显著下调 M1 标志物 Il12p40 和 Cxcl-10 的表达。使用 TEPP-46 激活 PKM2 可显著抑制 FSL-1 和 CpG 诱导的 Il1b mRNA 表达。 TEPP-46 抑制 Mtb 诱导的 Il1b mRNA 水平，提高 Mtb 诱导的 Il10 mRNA 水平，对 Tnf 水平没有影响^[2]。

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

体内研究
(In Vivo)

TEPP-46 具有良好的口服生物利用度，其清除率相对较低，半衰期长，且分布容积参数良好，这些参数预示着 TEPP-46 在肿瘤组织中的药物暴露量较高。在 150 mg/kg 的剂量下，TEPP-46 能够轻易地在 A549 异种移植肿瘤中实现 PKM2 的最大活化^[1]。

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

分子量

372.46

Formula

C₁₇H₁₆N₄O₂S₂

CAS 号

1221186-53-3

性状

固体

颜色

White to light 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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (134.24 mM; 超声助溶; 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	2.6849 mL	13.4243 mL	26.8485 mL
5 mM	0.5370 mL	2.6849 mL	5.3697 mL
10 mM	0.2685 mL	1.3424 mL	2.6849 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.87 mg/mL (7.71 mM); 澄清溶液
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.71 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.71 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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： 50% PEG300 50% Saline
Solubility: 10 mg/mL (26.85 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (13.42 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

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.93%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (288 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Anastasiou D, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol. 2012 Oct;8(10):839-847. [Content Brief]

[2]. Palsson-McDermott EM, et al. Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages. Cell Metab. 2015 Jan 6;21(1):65-80. [Content Brief]

Cell Assay ^[1]	2,000 cells are seeded in 96-well plates 24 h prior to treatment start. CellTiter96^® AQueous is used to assess cell viability following oxidant and PKM2 activator combination treatments. MTS: (3-(4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	H1299 parental and H1299 cells with constitutive expression of a mouse PKM1 cDNA (H1299-PKM1 cells) are propagated in RPMI supplemented with 10% fetal bovine serum, 2 mM glutamine, and hygromycin for transgene selection. Cells are harvested, resuspended in sterile PBS, and 5×10⁵ cells are injected subcutaneously into nu/nu mice. Tumor growth is monitored by caliper measurement, the mice are sacrificed and tumors harvested after the time indicated. Tumors are weighed, divided and either flash-frozen in liquid nitrogen or fixed in formalin for later analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Anastasiou D, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol. 2012 Oct;8(10):839-847. [Content Brief] [2]. Palsson-McDermott EM, et al. Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages. Cell Metab. 2015 Jan 6;21(1):65-80. [Content Brief]

TEPP-46 相关分类

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	2.6849 mL	13.4243 mL	26.8485 mL	67.1213 mL
	5 mM	0.5370 mL	2.6849 mL	5.3697 mL	13.4243 mL
	10 mM	0.2685 mL	1.3424 mL	2.6849 mL	6.7121 mL
	15 mM	0.1790 mL	0.8950 mL	1.7899 mL	4.4748 mL
	20 mM	0.1342 mL	0.6712 mL	1.3424 mL	3.3561 mL
	25 mM	0.1074 mL	0.5370 mL	1.0739 mL	2.6849 mL
	30 mM	0.0895 mL	0.4475 mL	0.8950 mL	2.2374 mL
	40 mM	0.0671 mL	0.3356 mL	0.6712 mL	1.6780 mL
	50 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3424 mL
	60 mM	0.0447 mL	0.2237 mL	0.4475 mL	1.1187 mL
	80 mM	0.0336 mL	0.1678 mL	0.3356 mL	0.8390 mL
	100 mM	0.0268 mL	0.1342 mL	0.2685 mL	0.6712 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:

TEPP-461221186-53-3ML-265TEPP46TEPP 46ML265ML 265Pyruvate KinaseInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

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）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

TEPP-46 (Synonyms: ML-265)

Customer Review

MCE 顾客使用本产品发表的 38 篇科研文献

TEPP-46 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

TEPP-46 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

TEPP-46 (Synonyms: ML-265)

Customer Review

TEPP-46 相关抗体

MCE 顾客使用本产品发表的 38 篇科研文献

TEPP-46 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

TEPP-46 相关抗体:

摩尔计算器

稀释计算器

TEPP-46 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z