2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Phosphoglycerate Kinase (PGK) Keap1-Nrf2 Interleukin Related
  4. DC-PGKI

DC-PGKI 是一种口服有效的 ATP 竞争性 PGK1 抑制剂 (IC50 = 0.16 μM，Kd = 99.08 nM) 。DC-PGKI 在体外和体内均能稳定 PGK1，并抑制糖酵解活性和 PGK1 的激酶功能。DC-PGKI 介导的 PGK1 抑制导致 NRF2 (核因子-红细胞因子 2 相关因子 2，NFE2L2) 的积累，NRF2 随后转位至细胞核，与 IL-1β 和 IL-6 基因的近端区域结合，并抑制 LPS 诱导的这些基因的表达。DC-PGKI 可用于结肠炎的研究。

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DC-PGKI

DC-PGKI Chemical Structure

CAS No. : 2829198-49-2

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DC-PGKI 相关抗体

Top Publications Citing Use of Products

查看 Phosphoglycerate Kinase (PGK) 亚型特异性产品:

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PGK1

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis[1].

IC50 & Target[1]

PGK1

0.16 μM (IC50)

PGK1

99.08 nM (Kd)

IL-6

 

IL-1β

 

体外研究
(In Vitro)

DC-PGKI (0.1-30 μM，3 小时) 能以浓度依赖的方式提高 RAW264.7 细胞中 PGK1 的热稳定性[1]。
DC-PGKI (5-10 μM，10 小时) 能抑制静息和激活状态下 RAW264.7 细胞中 PGK1 的糖酵解代谢活性[1]。
DC-PGKI (10-20 μM) 能显著降低 RAW264.7 细胞中 Beclin1 的 Ser30 位点磷酸化水平，表明 DC-PGKI 也能抑制 PGK1 的激酶功能[1]。
DC-PGKI (5-20 μM) 能以浓度依赖的方式抑制 RAW264.7 细胞中 LPS 诱导的 IL-1β 和 IL-6 mRNA 的表达[1]。
DC-PGKI (0-20 μM) 可显著抑制 Lipopolysaccharides (HY-D1056) (LPS) 诱导的 RAW264.7 细胞中 IL-1β 和 IL-6 前体的产生[1]。
DC-PGKI (5-20 μM，7 小时) 可显著降低 LPS 诱导的 RAW264.7 细胞中 KEAP1 蛋白水平，促进 NRF2 的积累，并上调 HMOX1 的 mRNA 和蛋白水平[1]。
DC-PGKI (5-20 μM，7 小时) 可上调 RAW264.7 细胞中 NRF2 的其他下游靶基因，包括 Txnrd1、Prdx1、Gclc、Sod1、Fth1 和 Ephx1，无论是否经 LPS 处理[1]。

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

DC-PGKI 相关抗体:

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM
Incubation Time: 3 h
Result: Increased RAW264.7 cells' PGK1 thermal stability in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: RAW264.7 cells were stimulated with LPS (1 μg/mL) for 4 hours.
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 7 h
Result: Inhibited the mRNA expression of IL-1β and IL-6.
Resulted in a significant reduction in KEAP1 protein level, accumulation of NRF2, as well as upregulation of both the mRNA and protein levels of HMOX1.
Upregulated other downstream target genes of NRF2, including Txnrd1, Prdx1, Gclc, Sod1, Fth1, and Ephx1.
体内研究
(In Vivo)

DC-PGKI (5-10 mg/kg，口服，每日一次，持续 8 天) 通过抑制 PGK1 和激活 NRF2 通路，显著缓解葡聚糖硫酸钠 (DSS) 诱导的小鼠结肠炎症状[1]。

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

Animal Model: 8-week-old C57BL/6 male mice were given 5%(w/v) DSS for 7 days to induce acute colitis, followed by drinking water for one day[1].
Dosage: 5 mg/kg, 10 mg/kg
Administration: P.o., once daily for 8 days
Result: Significantly reduced weight loss induced by DSS.
The disease activity index (DAI) decreased compared to the DSS group.
Reduced colonic tissue damage, lymphocyte infiltration, and crypt destruction.
Lowered serum and tissue protein and mRNA levels of IL-1β and IL-6.
Increased NRF2 protein accumulation in colonic tissue.
分子量

558.46

Formula

C26H29Cl2N7O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DC-PGKI 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DC-PGKI2829198-49-2Phosphoglycerate Kinase (PGK)Keap1-Nrf2Interleukin RelatedPhosphoglycerate KinaseILGlycolysisPhosphoglycerate kinase1MacrophagesNRF2InflammationInhibitorinhibitorinhibit

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