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Reagents and instruments for immunology, cell biology and molecular biology.

TEPP-46 [1221186-53-3]

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Cat# HY-18657-5mg

Size : 5mg

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Phone : +1 850 650 7790

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

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^[1]^[2]^[3].

Cellular Effect

Cell Line	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	[PMID: 34847663]
C6	IC₅₀	81.8 μM Compound: TEPP-46	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	[PMID: 31977207]
HCT-116	IC₅₀	89.91 μM Compound: TEPP-46	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	[PMID: 34847663]
HepG2	IC₅₀	>100 μM Compound: TEPP-46	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	[PMID: 34847663]
HT-29	IC₅₀	>100 μM Compound: TEPP-46	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	[PMID: 34847663]
MDA-MB-231	IC₅₀	>100 μM Compound: TEPP-46	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	[PMID: 34847663]
NIH3T3	IC₅₀	56.58 μM Compound: TEPP-46	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	[PMID: 31977207]
SF-126	IC₅₀	88.98 μM Compound: TEPP-46	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	[PMID: 31977207]
SW480	IC₅₀	92.95 μM Compound: TEPP-46	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	[PMID: 34847663]
U-118-MG	IC₅₀	85 μM Compound: TEPP-46	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	[PMID: 31977207]
U-251	IC₅₀	65.43 μM Compound: TEPP-46	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	[PMID: 31977207]
U2OS	IC₅₀	>100 μM Compound: TEPP-46	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	[PMID: 34847663]
U-87MG ATCC	IC₅₀	86.3 μM Compound: TEPP-46	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	[PMID: 31977207]

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].

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

Solvent & Solubility

In Vitro:

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)

Preparing
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

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, 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.

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.87 mg/mL (7.71 mM); Clear solution
Protocol 2

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.
Protocol 3

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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (26.85 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.93%

Data Sheet (280 KB) SDS (393 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

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. [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]

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TEPP-46 [1221186-53-3]

Cat# HY-18657-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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