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[CAS NO. 1221186-53-3] TEPP-46
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18657 |
| Brand: | MCE |
| CAS: | 1221186-53-3 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 372.46 |
| Molecular Formula | C17H16N4O2S2 |
| SMILES | O=C1C(N(C)C2=C3SC(S(C)=O)=C2)=C3C=NN1CC4=CC=CC(N)=C4 |
20 Publications Citing Use of MCE
- [1]Sci Transl Med. 2019 Feb 6;11(478):eaau8866.
- [2]Sci Adv. 2022 Sep 23;8(38):eabo0987.
- [3]Nat Commun. 2022 May 16;13(1):2698.
- [4]Kidney Int. 2023 Jan 30;S0085-2538(23)00052-2.
- [5]Cell Rep. 2022 Nov 29;41(9):111741.
- [6]Cell Rep. 2020 May 26;31(8):107690.
- [7]Anal Chem. 2021 Sep 21;93(37):12682-12689.
- [8]Mucosal Immunol. 2019 Nov;12(6):1280-1290.
- [9]Sci Signal. 2020 Oct 27;13(655):eaay9217.
- [10]JCI Insight. 2022 May 23;7(10):e154198.
- [11]Int J Nanomedicine. 2022 Apr 13;17:1711-1724.
- [12]FASEB J. 2020 Dec;34(12):16645-16661.
- [13]J Biol Chem. 2022 Aug 2;102340.
- [14]Cell Tissue Res. 2020 Dec;382(3):585-598.
- [15]Int J Oncol. 2022 Dec;61(6):144.
- [16]Mol Immunol. 2021 Nov 16;140:250-266.
- [17]Am J Pathol. 2020 Nov;190(11):2267-2281.
- [18]Onco Targets Ther. 2018 Dec 11;11:8995-9006.
- [19]bioRxiv. 2023 Jan 23.
- [20]Exp Hematol Oncol. 2022 Nov 8;11(1):88.
Summary
TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC 50 of 92 nM, showing little or no effect on PKM1, PKL and PKR [1] .
In Vitro
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 134.24 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
Add each solvent one by one: 50% PEG300 >> 50% saline
Solubility: 10 mg/mL (26.85 mM); Suspended solution; Need ultrasonic
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2.
-
3.
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4.
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
-
5.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution
References
- [1] Anastasiou D, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol. 2012 Oct;8(10):839-847.
- [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.
Synonyms
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