GlpBio

PGMI-004A

目录号: GC33387纯度: >99.00%
PGMI-004A是一种有效的磷酸甘油酸变位酶1(PGAM1)抑制剂，IC50为13.1μM。
PGMI-004A
Cas No.: 1313738-90-7
规格价格库存数量操作
1mg¥864.00现货
1
5mg¥2,160.00现货
1
10mg¥3,510.00现货
1
10mM (in 1mL DMSO)¥2,376.00现货
1
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文献被引

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    641, 529–536 (2025)
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

产品描述 Description

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

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].

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].

[1]. Hitosugi T, et al. Phosphoglycerate mutase 1 coordinates glycolysis and biosynthesis to promote tumor growth. Cancer Cell. 2012 Nov 13;22(5):585-600.

实验参考方法 Experimental Reference Method

Cell experiment:

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].

Animal experiment:

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].

References:

[1]. Hitosugi T, et al. Phosphoglycerate mutase 1 coordinates glycolysis and biosynthesis to promote tumor growth. Cancer Cell. 2012 Nov 13;22(5):585-600.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
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
分子式
C21H12F3NO6S
分子量
463.38 g/mol
溶解性
DMSO : ≥ 125 mg/mL (269.76 mM);Water : < 0.1 mg/mL (insoluble)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol