PKM2-IN-1

Name: PKM2-IN-1
Brand: MedChemExpress
SKU: HY-103617
Rating: 5.0 (26 reviews)

製品番号: HY-103617 純度: 99.79%: Data Sheet SDS COA 取扱説明書
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PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95 μM.

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CAS 番号 : 94164-88-2

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 105	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 105	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$96	在庫あり	Estimated Time of Arrival: December 31
10 mg	$120	在庫あり	Estimated Time of Arrival: December 31
25 mg	$190	在庫あり	Estimated Time of Arrival: December 31
50 mg	$245	在庫あり	Estimated Time of Arrival: December 31
100 mg	$320	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 26 publication(s) in Google Scholar

Other Forms of PKM2-IN-1:

PKM2-IN-1 (Standard) お問い合わせ

顧客検証

Bio/Physico-chemical Assay

Cell Imaging/Staining

Cell Proliferation/Viability Assay

: PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: Metabolism. 2025 Nov 6:175:156429. [Abstract]; Pyruvate kinase activities of B16F10 cells after incubation with MTyr–OANPs, MTyr–OANPs + PKM inhibitor PKM2-IN-1 and MTyr–OANPs + PKM activator TEPP-46.

: PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: Metabolism. 2025 Nov 6:175:156429. [Abstract]; Cell viabilities of indole-5,6-quinone, indole-5,6-quinone + PKM inhibitor PKM2-IN-1 and indole 5,6-quinone + PKM activator TEPP-46-treated, co-treated cells after 72 h.

: PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: Metabolism. 2025 Nov 6:175:156429. [Abstract]; Immunofluorescence images showing SPP1 expression in control and Slc2a5− /− BV2 cells treated with C3k, with OGD at various time points.

: PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2020 Apr;54:102722. [Abstract]; ORO staining and quantification demonstrated that 10 μM PKM2-IN (a kinase inhibitor) could rescue the impaired adipogenic differentiation in the TRAF4-overexpressing group.

: PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2020 Apr;54:102722. [Abstract]; PKM2-IN (10 μM) decreased the active β-catenin expression in the TRAF4-overexpressing group to a level near that in the NC1 group.

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

Cellular Effect

Cell Line	Type	Value	Description	References
BEAS-2B	IC₅₀	18.46 3 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]
BEAS-2B	IC₅₀	18.46 3 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]
BEAS-2B	IC₅₀	18.46 3 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 3 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]
HCT-116	IC₅₀	0.18 3 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]
HCT-116	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition	[PMID: 34355179]
HeLa	IC₅₀	0.29 3 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]
HeLa	IC₅₀	0.29 3 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 3 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]
HeLa	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition Antiproliferative activity against human HeLa cells assessed as cell growth inhibition	[PMID: 34355179]
NCI-H1299	IC₅₀	2.01 3 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]
HCT-116	IC₅₀	0.18 3 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]
NCI-H1299	IC₅₀	1.56 3 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 3 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]
HCT-116	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition	[PMID: 34355179]
NCI-H1299	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition	[PMID: 34355179]
HeLa	IC₅₀	0.29 3 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]
HeLa	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition Antiproliferative activity against human HeLa cells assessed as cell growth inhibition	[PMID: 34355179]
NCI-H1299	IC₅₀	1.56 3 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 3 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]
NCI-H1299	IC₅₀	2.95 3 Compound: 26	Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition	[PMID: 34355179]

体外実験

PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95±0.53 μM. Results show that most of the tested compounds exhibit some degree of PKM2 inhibition and some compounds, such as PKM2-IN-1 (compound 3k) and 6d, display more potent activity than the positive control shikonin. The representative compounds PKM2-IN-1, 6d display dose-dependent inhibition of PKM2 with less inhibition of PKM1 and PKL like shikonin. Among all tested compounds, the most potent compounds are 3a, PKM2-IN-1 and 3r, which exhibit IC₅₀ values against HCT116 and Hela cells ranging from 0.39 to 0.41 μM, 0.18 to 0.29 μM and 0.18 to 0.38 μM, respectively^[1].

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

分子量

345.48

分子式

C₁₈H₁₉NO₂S₂

CAS 番号

94164-88-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

S=C(N1CCCCC1)SCC(C2=O)=C(C)C(C3=C2C=CC=C3)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 4 mg/mL (11.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (72.36 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 99.79%

Select Batch:

データシート (274 KB) SDS (396 KB)

COA (248 KB) HNMR (251 KB) RP-HPLC (251 KB) LCMS (100 KB)

取扱説明書 (2659 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]

細胞実験
^[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

PKM2-IN-1 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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PKM2-IN-1

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Other Forms of PKM2-IN-1:

PKM2-IN-1 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

PKM2-IN-1 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PKM2-IN-1 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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