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PGK1 inhibitor

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11

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製品番号 製品名 Target 研究分野 構造式
  • HY-15154
    NG 52
    Maximum Cited Publications
    15 Publications Verification

    Compound 52

    CDK Cancer
    NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p .
    NG 52
  • HY-N0147
    Rutaecarpine
    5+ Cited Publications

    Rutecarpine

    COX Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine
  • HY-W195984
    Z57346765
    1 Publications Verification

    Phosphoglycerate Kinase (PGK) Cancer
    Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer .
    Z57346765
  • HY-178761

    Phosphoglycerate Kinase (PGK) Keap1-Nrf2 Heme Oxygenase (HO) Interleukin Related Inflammation/Immunology
    PGK1-IN-1 (Compound 6e) is a potent and selective PGK1 inhibitor (IC50: 33 nM). PGK1-IN-1 inhibits PGK1-mediated glycolytic metabolism and reduces glucose consumption/lactate production. PGK1-IN-1 enhances Nrf2 accumulation and HO-1 expression, and suppresses the transcription and protein levels of the inflammatory cytokines IL-1β and IL-6. PGK1-IN-1 ameliorates Dextran sulfate sodium (DSS) (HY-116282C)-induced experimental colitis in mice. PGK1-IN-1 can be used for research of inflammatory bowel disease (IBD) .
    PGK1-IN-1
  • HY-134205A
    CBR-470-1
    3 Publications Verification

    Keap1-Nrf2 Neurological Disease Metabolic Disease
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade .
    CBR-470-1
  • HY-N8540

    Phosphoglycerate Kinase (PGK) Fungal Apoptosis Infection Cancer
    Ilicicolin H is a selective and non-ATP-competitive phosphoglycerate kinase 1 (PGK1) (IC50 = 9.02 μM) and mitochondrial cytochrome bc1 reductase (IC50 = 2-3 ng/mL) inhibitor. Ilicicolin H directly binds to PGK1 with KD of 60 μM .Ilicicolin H can inhibit cell proliferation and induce apoptosis. Ilicicolin H can inhibit the lactate production and glucose uptake of hepatocellular carcinoma (HCC) cells. Ilicicolin H has a broad antifungal spectrum including C. albicans, Cryptococcus and A. fumigatus. Ilicicolin H can be used for the researches of cancer and infection, such as hepatocellular carcinoma (HCC) and C. albicans infection .
    Ilicicolin H
  • HY-178989

    Phosphoglycerate Kinase (PGK) Cuproptosis Cancer
    PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma .
    PGK1-IN-2
  • HY-177944

    Phosphoglycerate Kinase (PGK) Keap1-Nrf2 Interleukin Related Inflammation/Immunology
    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 .
    DC-PGKI
  • HY-N0147R

    Rutecarpine (Standard)

    Reference Standards COX Keap1-Nrf2 Inflammation/Immunology Cancer
    Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine (Standard)
  • HY-15154R

    Compound 52 (Standard)

    CDK Reference Standards Cancer
    NG 52 (Standard) is the analytical standard of NG 52. This product is intended for research and analytical applications. NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p .
    NG 52 (Standard)
  • HY-183583

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
    HIF-2α-IN-18

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