PKM2-IN-1
Based on 27 publication(s) in Google Scholar
PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.79%
- CAS 番号: 94164-88-2
- 分子式: C18H19NO2S2
- 分子量:345.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
MedChemExpress(MCE)の使用を引用している文献 PKM2-IN-1
More- Nat Nanotechnol. 2024 Sep;19(9):1399-1408. [Abstract]
- Metabolism. 2026 Feb:175:156429. [Abstract]
- Redox Biol. 2024 May:71:103112. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101966. [Abstract]
- Sci Adv. 2022 Sep 23;8(38):eabo0987. [Abstract]
- Cell Death Dis. 2025 Jun 3;16(1):432. [Abstract]
- Phytomedicine. 2024 Aug:131:155775. [Abstract]
- EBioMedicine. 2020 Apr:54:102722. [Abstract]
- Food Chem. 2026 May 30:512:148928. [Abstract]
- Food Chem X. 2024 Jan 9:21:101125. [Abstract]
- Phytother Res. 2023 May;37(5):1951-1967. [Abstract]
- Free Radic Biol Med. 2025 Jun 15:238:1-16. [Abstract]
- Cell Rep. 2022 Mar 8;38(10):110468. [Abstract]
- J Agric Food Chem. 2025 Aug 13;73(32):20385-20395. [Abstract]
- Eur J Pharmacol. 2019 Jul 5:854:232-239. [Abstract]
- J Pathol. 2022 Apr;256(4):414-426. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Mar;1870(3):167011. [Abstract]
- J Physiol. 2023 Dec;601(24):5655-5667. [Abstract]
- FASEB J. 2025 Jun 30;39(12):e70696. [Abstract]
- Appl Environ Microbiol. 2025 Apr 23;91(4):e0240624. [Abstract]
- FEBS Lett. 2026 Jun 8. [Abstract]
- Biochem Biophys Res Commun. 2023 Feb 12:644:112-121. [Abstract]
- bioRxiv. 2025 Oct 31.
- bioRxiv. 2025 July 15.
- Research Square Preprint. 2022.
- Research Square Print. 2022 May.
- bioRxiv. 2021 Mar 8.
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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IF
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Cell Imaging/Staining
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WB
生物活性
IC50: 2.95 μM (PKM2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | IC50 |
18.46 μM
Compound: 3k
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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
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[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
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[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
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[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
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[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
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[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] |
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.
化学情報
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CAS 番号 94164-88-2
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性状 Solid
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分子量 345.48
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分子式 C18H19NO2S2
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Color Light yellow to yellow
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SMILES
S=C(N1CCCCC1)SCC(C2=O)=C(C)C(C3=C2C=CC=C3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (27)
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Journal Impact Factor
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Most Recent
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Nat Nanotechnol
2024 Sep;19(9):1399-1408. PMID: 38862714 -
Metabolism
2026 Feb:175:156429. PMID: 41205649
PKM2-IN-1 purchased from MedChemExpress. Usage Cited in: Metabolism. 2026 Feb: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. 2026 Feb: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. 2026 Feb:175:156429. [Abstract]
Immunofluorescence images showing SPP1 expression in control and Slc2a5− /− BV2 cells treated with C3k, with OGD at various time points.
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Redox Biol
Enteric coronavirus PDCoV evokes a non-Warburg effect by hijacking pyruvic acid as a metabolic hub. [Abstract]2024 May:71:103112. PMID: 38461791 -
Cell Rep Med
KRASG12D-driven pentose phosphate pathway remodeling imparts a targetable vulnerability synergizing with MRTX1133 for durable remissions in PDAC. [Abstract]2025 Feb 18;6(2):101966. PMID: 39970873 -
Sci Adv
PKM2 promotes pulmonary fibrosis by stabilizing TGF-β1 receptor I and enhancing TGF-β1 signaling. [Abstract]2022 Sep 23;8(38):eabo0987. PMID: 36129984 -
Cell Death Dis
Oncometabolite fumarate facilitates PD-L1 expression and immune evasion in clear cell renal cell carcinoma. [Abstract]2025 Jun 3;16(1):432. PMID: 40461489 -
Phytomedicine
Hernandezine acts as a CDK4 suppressor inhibiting tumor growth by the CDK4/PKM2/NRF2 axis in colon cancer. [Abstract]2024 Aug:131:155775. PMID: 38838401 -
EBioMedicine
TRAF4 acts as a fate checkpoint to regulate the adipogenic differentiation of MSCs by activating PKM2. [Abstract]2020 Apr:54:102722. PMID: 32268273
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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Food Chem
Modulation of postmortem glycolysis in pork by electrostatic field: Roles of pyruvate kinase and myofibrillar protein phosphorylation. [Abstract]2026 May 30:512:148928. PMID: 41865528 -
Food Chem X
Effects of phosphoglycerate kinase 1 and pyruvate kinase M2 on metabolism and physiochemical changes in postmortem muscle. [Abstract]2024 Jan 9:21:101125. PMID: 38292674 -
Phytother Res
Sarsasapogenin, a principal active component absorbed into blood of total saponins of Anemarrhena, attenuates proliferation and invasion in rheumatoid arthritis fibroblast-like synoviocytes through downregulating PKM2 inhibited pathological glycolysis. [Abstract]2023 May;37(5):1951-1967. PMID: 36631974 -
Free Radic Biol Med
PKM2 alleviates mitochondrial oxidative stress and neuronal apoptosis through metabolic and non-metabolic pathways to protect SOD1G93A mice. [Abstract]2025 Jun 15:238:1-16. PMID: 40527446 -
Cell Rep
Moderate heart rate reduction promotes cardiac regeneration through stimulation of the metabolic pattern switch. [Abstract]2022 Mar 8;38(10):110468. PMID: 35263588 -
J Agric Food Chem
Zearalenone Regulates Energy Metabolism and Proliferation of Goat Endometrial Epithelial Cells through Estrogen Receptor 1. [Abstract]2025 Aug 13;73(32):20385-20395. PMID: 40762316 -
Eur J Pharmacol
Dihydroartemisinin represses esophageal cancer glycolysis by down-regulating pyruvate kinase M2. [Abstract]2019 Jul 5:854:232-239. PMID: 31004604 -
J Pathol
MyD88 in myofibroblasts regulates aerobic glycolysis-driven hepatocarcinogenesis via ERK-dependent PKM2 nuclear relocalization and activation. [Abstract]2022 Apr;256(4):414-426. PMID: 34927243 -
Biochim Biophys Acta Mol Basis Dis
USP46 enhances tamoxifen resistance in breast cancer cells by stabilizing PTBP1 to facilitate glycolysis. [Abstract]2024 Mar;1870(3):167011. PMID: 38176460 -
J Physiol
KATP channel activity and slow oscillations in pancreatic beta cells are regulated by mitochondrial ATP production. [Abstract]2023 Dec;601(24):5655-5667. PMID: 37983196 -
FASEB J
Hypoxia Exposure Promotes Th17 Cell Differentiation Through Activin A-PKM2 Axis to Exacerbate Autoimmune and Autoinflammatory Diseases. [Abstract]2025 Jun 30;39(12):e70696. PMID: 40515525 -
Appl Environ Microbiol
Comparative analyses of the biological characteristics, fluconazole resistance, and heat adaptation mechanisms of Candida auris and members of the Candida haemulonii complex. [Abstract]2025 Apr 23;91(4):e0240624. PMID: 40135859 -
FEBS Lett
LncRNA YIYA drives pancreatic cancer proliferation under high-glucose conditions by reinforcing a RAS-PKM2-dependent Warburg phenotype. [Abstract]2026 Jun 8. PMID: 42253181 -
Biochem Biophys Res Commun
Exosomal lncRNA HOTAIR induces PDL1+ B cells to impede anti-tumor immunity in colorectal cancer. [Abstract]2023 Feb 12:644:112-121. PMID: 36640665 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (72.36 mM); Suspended solution; Need ultrasonic
プロトコル
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) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
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.
| 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 |