TEPP-46
Based on 56 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.93%
- CAS No.: 1221186-53-3
- Formule: C17H16N4O2S2
- Masse moléculaire:372.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
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- Références
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Glycolysis Compound Library
HY-L058
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Pyroptosis Compound Library
HY-L059
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Anti-Cancer Metabolism Compound Library
HY-L083
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Glucose Metabolism Compound Library
HY-L092
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Activators Library
HY-L159
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Lactic Acid Metabolic Compound Library
HY-L204
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) TEPP-46
More- Nat Nanotechnol. 2024 Sep;19(9):1399-1408. [Abstract]
- Kidney Int. 2023 Apr;103(4):735-748. [Abstract]
- Nat Commun. 2022 May 16;13(1):2698. [Abstract]
- Exp Hematol Oncol. 2022 Nov 8;11(1):88. [Abstract]
- Sci Transl Med. 2019 Feb 6;11(478):eaau8866. [Abstract]
- Adv Sci (Weinh). 2025 Jun 5:e10386. [Abstract]
- Adv Sci (Weinh). 2025 Jan 21:e2408753. [Abstract]
- Sci Adv. 2022 Sep 23;8(38):eabo0987. [Abstract]
- Neuro Oncol. 2023 Nov 2;25(11):1989-2000. [Abstract]
- Cardiovasc Res. 2024 Aug 27:cvae187. [Abstract]
- Engineering. 2024 May 22.
- Cell Death Dis. 2023 Oct 10;14(10):663. [Abstract]
- Phytomedicine. 2025 Jul 25:143:156886. [Abstract]
- Phytomedicine. 2024 May 28:131:155775. [Abstract]
- J Pharm Anal. 2026 Mar 11.
- Food Chem. 2026 May 30:512:148928. [Abstract]
- Acta Pharmacol Sin. 2025 Jun 11. [Abstract]
- Diabetes. 2026 Jul 1;75(7):1243-1255. [Abstract]
- Food Chem X. 2024 Jan 9:21:101125. [Abstract]
- Int J Nanomedicine. 2022 Apr 13;17:1711-1724. [Abstract]
- EMBO J. 2024 May 15. [Abstract]
- Am J Chin Med. 2026;54(2):661-683. [Abstract]
- Cell Rep. 2025 Jun 13;44(6):115851. [Abstract]
- Cell Rep. 2022 Nov 29;41(9):111741. [Abstract]
- Cell Rep. 2020 May 26;31(8):107690. [Abstract]
- Int J Oncol. 2022 Dec;61(6):144. [Abstract]
- Anal Chem. 2021 Sep 21;93(37):12682-12689. [Abstract]
- Sci Signal. 2020 Oct 27;13(655):eaay9217. [Abstract]
- JCI Insight. 2022 May 23;7(10):e154198. [Abstract]
- J Agric Food Chem. 2025 Aug 13;73(32):20385-20395. [Abstract]
- Oncogenesis. 2025 Aug 24;14(1):32. [Abstract]
- Colloids Surf B Biointerfaces. 2024 May 26:241:113992. [Abstract]
- Int Immunopharmacol. 2026 Jun 15:179:116640. [Abstract]
- Int Immunopharmacol. 2025 Jun 20:162:115110. [Abstract]
- Int Immunopharmacol. 2025 Feb 3:149:114148. [Abstract]
- Mucosal Immunol. 2019 Nov;12(6):1280-1290. [Abstract]
- Molecules. 2026 Jan 16;31(2):319. [Abstract]
- Am J Pathol. 2020 Nov;190(11):2267-2281. [Abstract]
- Cell Signal. 2025 Aug 21:112066. [Abstract]
- ASN Neuro. 2023 Jan-Dec:15:17590914231151534. [Abstract]
- FASEB J. 2025 Jun 30;39(12):e70696. [Abstract]
- J Neurosci. 2024 May 15;44(20):e1563232024. [Abstract]
- FASEB J. 2020 Dec;34(12):16645-16661. [Abstract]
- J Biol Chem. 2022 Sep;298(9):102340. [Abstract]
- Mol Immunol. 2021 Dec:140:250-266. [Abstract]
- J Integr Neurosci. 2023 Nov 23;22(6):168. [Abstract]
- Cell Tissue Res. 2020 Dec;382(3):585-598. [Abstract]
- Onco Targets Ther. 2018 Dec 11:11:8995-9006. [Abstract]
- bioRxiv. 2025 July 15.
- bioRxiv. 2024 June 05.
- Heliyon. 2024 Apr 10;10(8):e29515. [Abstract]
- Research Square Preprint. 2023 Sep 6.
- Research Square Preprint. 2023 Sep 11.
- bioRxiv. 2023 Sep 17:2023.09.15.557984. [Abstract]
- bioRxiv. 2023 Sep 8.
- bioRxiv. 2023 Jan 23.
Customer Validation & Images
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WB
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Histological Imaging/Staining
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Cell Migration/Invasion Assay
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Cell Imaging/Staining
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Histological Imaging/Staining
Activité biologique
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Cell Line
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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
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[PMID: 34847663] |
| C6 | IC50 |
81.8 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
| HCT-116 | IC50 |
89.91 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| HepG2 | IC50 |
>100 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| HT-29 | IC50 |
>100 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| NIH3T3 | IC50 |
56.58 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
| SF-126 | IC50 |
88.98 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
| SW480 | IC50 |
92.95 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| U-118-MG | IC50 |
85 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
| U-251 | IC50 |
65.43 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
| U2OS | IC50 |
>100 μM
Compound: TEPP-46
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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
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[PMID: 34847663] |
| U-87MG ATCC | IC50 |
86.3 μM
Compound: TEPP-46
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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
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[PMID: 31977207] |
TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine[1]. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1221186-53-3
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Appearance Solid
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Masse moléculaire 372.46
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Formule C17H16N4O2S2
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Color White to light yellow
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SMILES
O=C1C(N(C)C2=C3SC(S(C)=O)=C2)=C3C=NN1CC4=CC=CC(N)=C4
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Synonyms
ML-265
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (56)
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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 -
Kidney Int
Reduction of anaerobic glycolysis contributes to angiotensin II-induced podocyte injury with foot process effacement. [Abstract]2023 Apr;103(4):735-748. PMID: 36731609 -
Nat Commun
Purine nucleotide depletion prompts cell migration by stimulating the serine synthesis pathway. [Abstract]2022 May 16;13(1):2698. PMID: 35577785
TEPP-46 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 May 16;13(1):2698. [Abstract]
Quantification of A375 cell migration in the wound-healing assay after MTX treatment in the presence or absence of TEPP-46 (100 µM, 24 h).
TEPP-46 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 May 16;13(1):2698. [Abstract]
Representative images of actin cytoskeleton in A375 cells treated with MTX in the presence or absence of TEPP-46 (100 µM, 24 h). Cell length was quantified relative to vehicle control.
TEPP-46 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 May 16;13(1):2698. [Abstract]
Representative images of lung sections from metastasis-bearing mice treated with MTX in the presence or absence of TEPP-46 (50 mg/kg, oral gavage, ten weeks), immunostained with S100 (green) or subjected to H&E staining.
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Exp Hematol Oncol
Gut fungi enhances immunosuppressive function of myeloid-derived suppressor cells by activating PKM2-dependent glycolysis to promote colorectal tumorigenesis. [Abstract]2022 Nov 8;11(1):88. PMID: 36348389 -
Sci Transl Med
Tissue-specific regulation of p53 by PKM2 is redox dependent and provides a therapeutic target for anthracycline-induced cardiotoxicity. [Abstract]2019 Feb 6;11(478):eaau8866. PMID: 30728290 -
Adv Sci (Weinh)
METTL14-Mediated M6A Modification of LINC01094 Induces Glucose Metabolic Reprogramming in Breast Cancer by Recruiting the PKM2/JMJD5 Complex. [Abstract]2025 Jun 5:e10386. PMID: 40470773
TEPP-46 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 5:e10386. [Abstract]
Western blot assays following DSS crosslinking demonstrated that TEPP‐46 (40 mg/kg, administered daily by intraperitoneal injection for three weeks)effectively nullified the enhancement of PKM2 dimerization induced by LINC01094.
TEPP-46 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 5:e10386. [Abstract]
The mice were administered daily by intraperitoneal injection 40 mg/kg TEPP‐46 for three weeks.The xenograft tumors were visually represented through H&E staining.
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Adv Sci (Weinh)
Deletion of Pyruvate Carboxylase in Tubular Epithelial Cell Promotes Renal Fibrosis by Regulating SQOR/cGAS/STING-Mediated Glycolysis. [Abstract]2025 Jan 21:e2408753. PMID: 39836535 -
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 -
Neuro Oncol
PKM2 rewires glucose metabolism during radiation therapy to promote an antioxidant response and glioblastoma radioresistance. [Abstract]2023 Nov 2;25(11):1989-2000. PMID: 37279645 -
Cardiovasc Res
Regulation of Ptbp1-controlled alternative splicing of pyruvate kinase muscle by Liver kinase b1 governs vascular smooth muscle cell plasticity in vivo. [Abstract]2024 Aug 27:cvae187. PMID: 39189621 -
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Cell Death Dis
Pyruvate kinase M2 regulates mitochondrial homeostasis in cisplatin-induced acute kidney injury. [Abstract]2023 Oct 10;14(10):663. PMID: 37816709 -
Phytomedicine
Chemoproteomics reveals Ailanthone directly binds to PKM2 to inhibit the progression of Hepatocellular carcinoma. [Abstract]2025 Jul 25:143:156886. PMID: 40466508 -
Phytomedicine
Hernandezine acts as a CDK4 suppressor inhibiting tumor growth by the CDK4/PKM2/NRF2 axis in colon cancer. [Abstract]2024 May 28:131:155775. PMID: 38838401 -
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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 -
Acta Pharmacol Sin
YOD1 mediates isoproterenol-induced cardiac remodeling by deubiquitinating PKM2 and reducing PKM2 tetramerization in cardiomyocytes. [Abstract]2025 Jun 11. PMID: 40500343 -
Diabetes
2026 Jul 1;75(7):1243-1255. PMID: 42138738 -
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 -
Int J Nanomedicine
PD-1 Targeted Nanoparticles Inhibit Activated T Cells and Alleviate Autoimmunity via Suppression of Cellular Energy Metabolism Mediated by PKM2. [Abstract]2022 Apr 13;17:1711-1724. PMID: 35444416 -
EMBO J
PKM2 functions as a histidine kinase to phosphorylate PGAM1 and increase glycolysis shunts in cancer. [Abstract]2024 May 15. PMID: 38750259 -
Am J Chin Med
Triptolide from Tripterygium wilfordii Suppresses Glycolysis and Induces Cuproptosis via the HK2/DLAT Signaling Pathway in Colorectal Cancer. [Abstract]2026;54(2):661-683. PMID: 41709570 -
Cell Rep
ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. [Abstract]2025 Jun 13;44(6):115851. PMID: 40516055 -
Cell Rep
2022 Nov 29;41(9):111741. PMID: 36450257 -
Cell Rep
Pyruvate Kinase M2 Promotes the Activation of Dendritic Cells by Enhancing IL-12p35 Expression. [Abstract]2020 May 26;31(8):107690. PMID: 32460017
TEPP-46 purchased from MedChemExpress. 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 MedChemExpress. 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.
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Int J Oncol
TRIM35 ubiquitination regulates the expression of PKM2 tetramer and dimer and affects the malignant behaviour of breast cancer by regulating the Warburg effect. [Abstract]2022 Dec;61(6):144. PMID: 36196894 -
Anal Chem
TEPP-46-Based AIE Fluorescent Probe for Detection and Bioimaging of PKM2 in Living Cells. [Abstract]2021 Sep 21;93(37):12682-12689. PMID: 34505513 -
Sci Signal
2020 Oct 27;13(655):eaay9217. PMID: 33109748 -
JCI Insight
2022 May 23;7(10):e154198. PMID: 35603790 -
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 -
Oncogenesis
BRG1 inhibits glycolysis by promoting SHP1-mediated dephosphorylation of PKM2 in non-small cell lung cancer. [Abstract]2025 Aug 24;14(1):32. PMID: 40849293 -
Colloids Surf B Biointerfaces
Co-delivery of doxorubicin-dihydroartemisinin prodrug/TEPP-46 nano-liposomes for improving antitumor and decreasing cardiotoxicity in B16-F10 tumor-bearing mice. [Abstract]2024 May 26:241:113992. PMID: 38833960 -
Int Immunopharmacol
Ailanthone ameliorates CCl4-induced liver fibrosis by targeting PKM2-mediated macrophage M1 polarization and glycolytic reprogramming. [Abstract]2026 Jun 15:179:116640. PMID: 41980396 -
Int Immunopharmacol
Palmatine ameliorates intestinal epithelial barrier injury in ulcerative colitis via targeting enolase 3. [Abstract]2025 Jun 20:162:115110. PMID: 40543101 -
Int Immunopharmacol
TEPP-46 inhibits glycolysis to promote M2 polarization of microglia after ischemic stroke. [Abstract]2025 Feb 3:149:114148. PMID: 39904037 -
Mucosal Immunol
Intestinal epithelial PKM2 serves as a safeguard against experimental colitis via activating β-catenin signaling. [Abstract]2019 Nov;12(6):1280-1290. PMID: 31462699 -
Molecules
Trichostatin A Influences Dendritic Cells' Functions by Regulating Glucose and Lipid Metabolism via PKM2. [Abstract]2026 Jan 16;31(2):319. PMID: 41599367 -
Am J Pathol
Pyruvate Kinase M2 Tetramerization Protects against Hepatic Stellate Cell Activation and Liver Fibrosis. [Abstract]2020 Nov;190(11):2267-2281. PMID: 32805235 -
Cell Signal
Poly-L-arginine induces asthma pyroptosis in lung epithelial cells by promoting nuclear translocation of the PKM2 dimer. [Abstract]2025 Aug 21:112066. PMID: 40848938 -
ASN Neuro
Pyruvate Kinase 2, an Energy Metabolism Related Enzyme, May Have a Neuroprotective Function in Retinal Degeneration. [Abstract]2023 Jan-Dec:15:17590914231151534. PMID: 36799552 -
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 -
J Neurosci
Imbalance in glucose metabolism regulates the transition of microglia from homeostasis to Disease Associated Microglia stage 1. [Abstract]2024 May 15;44(20):e1563232024. PMID: 38565291 -
FASEB J
Sirtuin 3 governs autophagy-dependent glycolysis during Angiotensin II-induced endothelial-to-mesenchymal transition. [Abstract]2020 Dec;34(12):16645-16661. PMID: 33131100 -
J Biol Chem
EGF promotes PKM2 O-GlcNAcylation by stimulating O-GlcNAc transferase phosphorylation at Y976 and their subsequent association. [Abstract]2022 Sep;298(9):102340. PMID: 35931120 -
Mol Immunol
Pyruvate kinase M2 (PKM2) interacts with activating transcription factor 2 (ATF2) to bridge glycolysis and pyroptosis in microglia. [Abstract]2021 Dec:140:250-266. PMID: 34798593 -
J Integr Neurosci
PKM2 Nuclear Translocation Promotes Glial Cell Activation and Aggravates the Brain Injury of Intracerebral Hemorrhage. [Abstract]2023 Nov 23;22(6):168. PMID: 38176945 -
Cell Tissue Res
Pyruvate kinase M2 activation protects against the proliferation and migration of pulmonary artery smooth muscle cells. [Abstract]2020 Dec;382(3):585-598. PMID: 32719938 -
Onco Targets Ther
Resveratrol induces apoptosis in human melanoma cell through negatively regulating Erk/PKM2/Bcl-2 axis. [Abstract]2018 Dec 11:11:8995-9006. PMID: 30588012 -
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Heliyon
FV-429 induces apoptosis by regulating nuclear translocation of PKM2 in pancreatic cancer cells. [Abstract]2024 Apr 10;10(8):e29515. PMID: 38638982 -
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bioRxiv
Pyruvate Kinase Activity Regulates Cystine Starvation Induced Ferroptosis through Malic Enzyme 1 in Pancreatic Cancer Cells. [Abstract]2023 Sep 17:2023.09.15.557984. PMID: 37745559 -
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Solvant et solubilité
DMSO : 50 mg/mL (134.24 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.71 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (26.85 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 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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Instruction de manipulation (2659 KB)
Références
[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]
[3]. Goran Hamid Mohammad, et al. Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an Effective Combination Strategy for the Treatment of Pancreatic Cancer. Cancers (Basel). 2019 Sep 16;11(9):1372. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 |
TEPP-46 Related Classifications
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