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PGMI-004A

Name: PGMI-004A
Brand: TargetMol
SKU: T16517
Rating: 4.5 (1 reviews)

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Catalog No. T16517Cas No. 1313738-90-7

PGMI-004A is an effective inhibitor of phosphoglycerate mutase 1 (IC50: 13.1 μM).

PGMI-004A

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Catalog No. T16517Cas No. 1313738-90-7

PGMI-004A is an effective inhibitor of phosphoglycerate mutase 1 (IC50: 13.1 μM).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$347	6-8 weeks	6-8 weeks
25 mg	$987	6-8 weeks	6-8 weeks
50 mg	$1,360	6-8 weeks	6-8 weeks
100 mg	$2,190	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	PGMI-004A is an effective inhibitor of phosphoglycerate mutase 1 (IC50: 13.1 μM).
Targets&IC50	PGAM1:13.1 μM
In vitro	PGMI-004A inhibits PGAM1 with an IC50 of approximately 13.1 μM and the Kd value of the PGMI-004A-PGAM1 interaction is determined to be 7.2±0.7 μM from the fluorescence-based binding assay. PGMI-004A treatment induces decreased cell proliferation of diverse human cancer and leukemia cells, but not control human dermal fibroblasts (HDF), human foreskin fibroblasts (HFF), human HaCaT keratinocyte cells and human melanocyte PIG1 cells, suggesting minimal non-specific toxicity of PGMI-004A in normal, proliferating human cells. PGMI-004A may allosterically modulate the enzyme activity of PGAM1. The Ki value is determined to be 3.91±2.50 μM using a Dixon plot analysis. The Kd value for protein-ligand interaction is calculated to be 9.4±2.0 μM. PGMI-004A (20 μM) treatment, causes significantly reduced lactate production that is rescued by methyl-2-PG treatment but has no significant effect on intracellular ATP levels. Inhibition of PGAM1 activity by PGMI-004A (20 μM) treatment results in decreased 2-PG and increased 3-PG levels in H1299 cells, which could be rescued by treatment with methyl-2-PG. PGMI-004A (20 μM) treatment results in decreased oxidative PPP flux and NADPH/NADP+ratio, as well as reduced biosynthesis of lipids and RNA, and cell proliferation in H1299 cells [1].
In vivo	Treatment with PGMI-004A significantly reduces tumor growth and size in mice when compared to those treated with a vehicle control. It effectively inhibits PGAM1 enzyme activity within tumors of nude mice bearing xenografts. The xenograft model is established by injecting H1299 cells into nude mice, and after six days, the mice are segregated into two groups (n=8/group). They are subsequently treated with either PGMI-004A (100mg/kg/day) or a vehicle for 21 days [1].

Chemical Properties

Molecular Weight	463.38
Formula	C₂₁H₁₂F₃NO₆S
Cas No.	1313738-90-7
Smiles	Oc1c(O)c(cc2C(=O)c3ccccc3C(=O)c12)S(=O)(=O)Nc1ccc(cc1)C(F)(F)F
Relative Density.	1.663 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (269.76 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.12 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1581 mL	10.7903 mL	21.5806 mL	107.9028 mL
5 mM	0.4316 mL	2.1581 mL	4.3161 mL	21.5806 mL
10 mM	0.2158 mL	1.0790 mL	2.1581 mL	10.7903 mL
20 mM	0.1079 mL	0.5395 mL	1.0790 mL	5.3951 mL
50 mM	0.0432 mL	0.2158 mL	0.4316 mL	2.1581 mL
100 mM	0.0216 mL	0.1079 mL	0.2158 mL	1.0790 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc