PKM2-IN-1

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

Cat. No.: HY-103617 Purity: 99.79%: Data Sheet
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SDS
Handling Instructions
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PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95 μM.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 94164-88-2

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 26 publication(s) in Google Scholar

Other Forms of PKM2-IN-1:

PKM2-IN-1 (Standard) 견적 받기

26 Publications Citing Use of MCE PKM2-IN-1

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.

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

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 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]
HCT-116	IC₅₀	2.95 μM 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 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]
HeLa	IC₅₀	2.95 μM 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 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]
NCI-H1299	IC₅₀	2.95 μM 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]

In Vitro

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.

분자량

345.48

화학식

C₁₈H₁₉NO₂S₂

CAS No.

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

순도&문서

Purity: 99.79%

Select Batch:

Data Sheet (274 KB) SDS (396 KB)

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

Handling Instructions (2659 KB)

References

[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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

[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

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

고객리뷰

Other Forms of PKM2-IN-1:

PKM2-IN-1 Related Antibodies

26 Publications Citing Use of MCE PKM2-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

순도&문서

References

고객리뷰

PKM2-IN-1 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

PKM2-IN-1 Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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