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PGMI-004A 

Cat. No.: HY-101143
Handling Instructions

PGMI-004A is a potent phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 13.1 μM.

For research use only. We do not sell to patients.

PGMI-004A Chemical Structure

PGMI-004A Chemical Structure

CAS No. : 1313738-90-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PGMI-004A is a potent phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 13.1 μM.

IC50 & Target

IC50: 13.1 μM (PGAM1)[1]

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 fluorescence-based binding assay. PGMI-004A may allosterically modulate the enzyme activity of PGAM1. The Ki value is determined to be 3.91±2.50 μM using Dixon plot analysis. The Kd value for protein-ligand interaction is calculated to be 9.4±2.0 μM. 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. Treatment with PGMI-004A (20 μM) results in significantly reduced lactate production that is rescued by methyl-2-PG treatment, but has no significant effect on intracellular ATP levels. 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. PGMI-004A treatment results in 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[1].

In Vivo

The xenograft experiment is performed by injecting H1299 cells to nude mice. Six days post-injection, mice are divided into two groups (n=8/group) and treated with either PGMI-004A (100mg/kg/day) or vehicle for 21 days. PGMI-004A treatment results in significantly decreased tumor growth and tumor size in treated mice compared with mice receiving vehicle control. Moreover, treatment with PGMI-004A effectively inhibits PGAM1 enzyme activity in tumors in vivo in resected tumors from xenograft nude mice[1].

References
Cell Assay
[1]

For adherent cell viability assay such as H1299 cells with trypan blue exclusion, 5×104 cells are seeded in 6-well plate 24 h before the assay starts and are cultured at 37°C. 24 h after seeding, cells are treated with PGMI-004A (5, 10, 20, and 40 μM) and incubated at 37°C for indicated times. Cell viability is determined by counting drug-treated cells compared to DMSO-treated control cells with trypan blue exclusion under a microscope (×40). For MTT cell viability assay of adherent cells, 5×103 cells are seeded in 96-well plate 24 h before the assay starts and are cultured at 37°C. 24 h after seeding, cells are treated with PGMI-004A and incubated at 37°C for 3 days. Cell viability is determined by using CellTiter96Aqueous One solution proliferation kit[1].

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

Animal Administration
[1]

Mice[1]
Nude mice (female 6-8-week-old) are subcutaneously injected with 10×106 H1299 cells harboring empty vector on the left flank, and cells with stable knockdown of endogenous hPGAM1 on the right flank, respectively. The tumors are harvested and weighed at the experimental endpoint, and the masses of tumors (g) derived from cells with and without stable knockdown of endogenous hPGAM1 in both flanks of each mouse are compared. Statistical analyses are performed by comparison in relation to the control group with a two-tailed paired Student’s ttest. For drug evaluation of PGMI-004A using xenograft mice, PGMI-004A is administered by daily i.p. injection at a dose of 100 mg/kg from 6 days after subcutaneous injection of H1299 cells on right flank of each mouse. Tumor growth is recorded by measurement of two perpendicular diameters of the tumors over a 3-week course[1].

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

References
Molecular Weight

463.38

Formula

C₂₁H₁₂F₃NO₆S

CAS No.

1313738-90-7

SMILES

O=S(C(C=C1C2=O)=C(O)C(O)=C1C(C3=C2C=CC=C3)=O)(NC4=CC=C(C(F)(F)F)C=C4)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PGMI-004A
Cat. No.:
HY-101143
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PGMI-004A

Cat. No.: HY-101143