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Recombinant Human [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (PDK1)

In Stock
  • 中文名稱:
    Recombinant Human [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (PDK1)
  • 貨號:
    CSB-EP613584HU
  • 規格:
    ¥1536
  • 圖片:
    • (Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.
  • 其他:

產品詳情

  • 純度:
    Greater than 85% as determined by SDS-PAGE.
  • 生物活性:
    Not Test
  • 基因名:
  • Uniprot No.:
  • 別名:
    acetyl-transferring;Pyruvate dehydrogenase kinase isoform 1;PDH kinase 1
  • 種屬:
    Homo sapiens (Human)
  • 蛋白長度:
    Full Length of Mature Protein
  • 來源:
    E.coli
  • 分子量:
    53.5 kDa
  • 表達區域:
    29-436aa
  • 氨基酸序列
    SSDSGSSPASERGVPGQVDFYARFSPSPLSMKQFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQELLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYFLDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLCDLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPPIQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLPISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDWCVPSREPKDMTTFRSA
    Note: The complete sequence may include tag sequence, target protein sequence, linker sequence and extra sequence that is translated with the protein sequence for the purpose(s) of secretion, stability, solubility, etc.
    If the exact amino acid sequence of this recombinant protein is critical to your application, please explicitly request the full and complete sequence of this protein before ordering.
  • 蛋白標簽:
    C-terminal Flag-tagged
  • 產品提供形式:
    Liquid or Lyophilized powder
    Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
  • 緩沖液:
    If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
  • 復溶:
    We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20℃/-80℃. Our default final concentration of glycerol is 50%. Customers could use it as reference.
  • 儲存條件:
    Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
  • 保質期:
    The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
    Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
  • 貨期:
    3-7 business days
  • 注意事項:
    Repeated freezing and thawing is not recommended. Store working aliquots at 4℃ for up to one week.
  • Datasheet & COA:
    Please contact us to get it.

產品評價

靶點詳情

  • 功能:
    Kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress.
  • 基因功能參考文獻:
    1. miR-375 and its probable PDK1 target may be utilized for the management of Kidney cancer. PMID: 30098579
    2. The importance of PDK1 in tumor growth and progression.A role of PDK1 in tumor microenvironment.[review] PMID: 28473254
    3. MiR-138 inhibits glycolysis but promotes mitochondrial respiration through directly targetting PDK1, and that contributes to cardiac cells' survival. PMID: 28899927
    4. Study shows higher expression level of PDK1 in non-small cell lung cancer (NSCLC) and its promoter region targeted by miR- 145. PMID: 28661070
    5. These results indicate that the immunohistochemistry analysis of the protein expression of PDK1, PHD3, and HIF-1alpha defines the hypoxic status of Neuroblastoma tumors. PMID: 29117193
    6. The pyruvate dehydrogenase kinases (PDKs) PDK1 and PDK3 are direct targets of KDM4A and E2F1 and modulate the switch between glycolytic metabolism and mitochondrial oxidation. PMID: 27626669
    7. dicumarol potently inhibited the kinase activity of PDK1, shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro. PMID: 28617852
    8. miR-379 could function as a tumour-suppressing miRNA via targeting PDK1 in osteosarcoma. PMID: 27781416
    9. These results also suggest that inhibition of HIF-1a with 2-MeOE2 sensitizes radioresistant melanoma cells 435R to X-ray irradiation through targeting the glycolysis that is regulated by PDK1 PMID: 28339028
    10. PDK1 is frequently upregulated in primary nasopharyngeal carcinoma and may serve as a prognostic marker. PMID: 28029432
    11. A new function for PDK1 in metabolic reprogramming, which could be used to indicate the prognosis of Non small cell lung cancer and provide targeted therapeutic strategy for clinical treatment. PMID: 27878287
    12. Our results demonstrated that down-regulation of SDHB and up-regulation of PDK1 may be novel biomarkers for predicting advanced tumor progression and unfavorable prognosis in recurrent nasopharyngeal carcinoma patients PMID: 26547584
    13. n the conditon of miR- 128b over-expression, we also observed spontaneous inactivation of the Akt/NF-kappaB signalling, implying PDK1 was a potential regulator of this pathway. In conclusion, our study shed some novel light on miR-128b-PDK1/Akt/NF-kappaB axis onGastric cancer (GC) progression PMID: 26949090
    14. Dichloroacetate, an Iihibitor of PDK1, can reverse the mitochondrial suppression of renal cell carcinoma and decrease HIF transcriptional activity, decreasing tumor growth and angiogenesis. PMID: 26433571
    15. Tergeting PDK1 with dichloroacetophenone inhibited acute myeloid leukemia cell growth via multiple signaling pathways. PMID: 26593251
    16. PDK1 was specifically required for metabolic adaptation to nutrient limitation and hypoxia. PMID: 26365179
    17. High expression of PDK1 is associated with Colon Cancer. PMID: 26439504
    18. both PDK 1 and 2 isoforms are overexpressed in cutaneous melanoma compared to nevi, this expression being associated with the expression of the mTOR pathway effectors and independent of the BRAF mutational status PMID: 25976231
    19. Lin28A and Lin28B enhance, whereas let-7 suppresses, aerobic glycolysis via targeting pyruvate dehydrogenase kinase 1, or PDK1. PMID: 25301052
    20. Follow-up replication analyses in up to an additional 21,345 participants identified three new fasting plasma glucose loci reaching genome-wide significance in or near PDK1-RAPGEF4, KANK1, and IGF1R. PMID: 25187374
    21. NOR1 expression causes apoptosis of tumor cells in hypoxia by altering the expression of PDK1 expression and mitochondrial Bax-Bcl2 balance thus suppress tumor cell adaptation to hypoxia PMID: 24788728
    22. Accordingly, elevated levels of PDK1, PDK3, and PKM2 and reduced PK activity could be observed in iPSCs and human embryonic stem cells in the undifferentiated state PMID: 24123565
    23. High expression of pyruvate dehydrogenase kinase-1 is associated with gastric cancer. PMID: 23135628
    24. post-mortem brain extracts from patients with Alzheimer disease exhibited a decrease in PDK1 expression compared with nondemented patients. PMID: 22948140
    25. Pyruvate dehydrogenase kinase 1 is an important regulator of pyruvate dehydrogenase in clonal pancreatic beta-cells. PMID: 20415663
    26. mRNA levels not changed in skeletal muscle during fasting PMID: 14966024
    27. In summary, PDK activity is decreased after a high-fat diet that is rich in n-3 fatty acids, although PDHa activity was unaltered. PMID: 15591305
    28. HIF-1 also actively suppresses metabolism through the tricarboxylic acid cycle (TCA) by directly trans-activating the gene encoding pyruvate dehydrogenase kinase 1 (PDK1). PMID: 16517405
    29. Distinct structural mechanisms for inhibition of PDK1 by AZD7545, dichloroacetate, and radicol. PMID: 17683942
    30. HIF regulation of PDK-1 has a key role in maintaining lactate production in human cancer and that the investigation of PDK-1 inhibitors should be investigated for antitumour effects PMID: 18542064
    31. Data show that PDK1 and HIF prolyl hydroxylase 3 expressions are lowest in children of chronic mountain sickness fathers at altitude. PMID: 18954447

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  • 亞細胞定位:
    Mitochondrion matrix.
  • 蛋白家族:
    PDK/BCKDK protein kinase family
  • 組織特異性:
    Expressed predominantly in the heart. Detected at lower levels in liver, skeletal muscle and pancreas.
  • 數據庫鏈接:

    HGNC: 8809

    OMIM: 602524

    KEGG: hsa:5163

    STRING: 9606.ENSP00000282077

    UniGene: Hs.470633



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