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  4. Recombinant Human Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1)

Recombinant Human Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1)

  • 貨號：
    CSB-YP013409HU
  • 規格：
  • 來源：
    Yeast
  • 其他：
  • 貨號：
    CSB-EP013409HU
  • 規格：
  • 來源：
    E.coli
  • 其他：
  • 貨號：
    CSB-EP013409HU-B
  • 規格：
  • 來源：
    E.coli
  • 共軛：
    Avi-tag Biotinylated

    E. coli biotin ligase (BirA) is highly specific in covalently attaching biotin to the 15 amino acid AviTag peptide. This recombinant protein was biotinylated in vivo by AviTag-BirA technology, which method is BriA catalyzes amide linkage between the biotin and the specific lysine of the AviTag.

  • 其他：
  • 貨號：
    CSB-BP013409HU
  • 規格：
  • 來源：
    Baculovirus
  • 其他：
  • 貨號：
    CSB-MP013409HU
  • 規格：
  • 來源：
    Mammalian cell
  • 其他：

產品詳情

  • 純度：
    >85% (SDS-PAGE)
  • 基因名：
  • Uniprot No.：
  • 別名：
    Dual specificity mitogen-activated protein kinase kinase 1; MAP kinase kinase 1; MAPKK 1; MKK1; EC 2.7.12.2; ERK activator kinase 1; MAPK/ERK kinase 1; MEK 1; MAP2K1 MEK1 PRKMK1
  • 種屬：
    Homo sapiens (Human)
  • 蛋白長度：
    Full Length
  • 表達區域：
    1-393
  • 氨基酸序列
    MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
  • 蛋白標簽：
    Tag?type?will?be?determined?during?the?manufacturing?process.
    The tag type will be determined during production process. If you have specified tag type, please tell us and we will develop the specified tag preferentially.
  • 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.
  • 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：
    Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
    Note: All of our proteins are default shipped with normal blue ice packs, if you request to ship with dry ice, please communicate with us in advance and extra fees will be charged.
  • 注意事項：
    Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
  • Datasheet ：
    Please contact us to get it.

產品評價

靶點詳情

  • 功能：
    Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2K2/MEK2 function specifically in the MAPK/ERK cascade, and catalyze the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2, leading to their activation and further transduction of the signal within the MAPK/ERK cascade. Activates BRAF in a KSR1 or KSR2-dependent manner; by binding to KSR1 or KSR2 releases the inhibitory intramolecular interaction between KSR1 or KSR2 protein kinase and N-terminal domains which promotes KSR1 or KSR2-BRAF dimerization and BRAF activation. Depending on the cellular context, this pathway mediates diverse biological functions such as cell growth, adhesion, survival and differentiation, predominantly through the regulation of transcription, metabolism and cytoskeletal rearrangements. One target of the MAPK/ERK cascade is peroxisome proliferator-activated receptor gamma (PPARG), a nuclear receptor that promotes differentiation and apoptosis. MAP2K1/MEK1 has been shown to export PPARG from the nucleus. The MAPK/ERK cascade is also involved in the regulation of endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC), as well as in the fragmentation of the Golgi apparatus during mitosis.
  • 基因功能參考文獻：
    1. Upregulation of miR101 inhibited DLBCL cell proliferation and facilitated apoptosis by inhibiting the expression of MEK1. PMID: 30365139
    2. Somatic activating mutations in MAP2K1 cause melorheostosis. PMID: 29643386
    3. Here the authors identified a direct interaction of both MEK1 and MEK2 with AKT. The interaction between MEK and AKT affects cell migration and adhesion, but not proliferation. The specific mechanism of action of the MEK-AKT complex involves phosphorylation of the migration-related transcription factor FoxO1. PMID: 28225038
    4. Activating mutations enhance the rate of MEK1 phosphorylation by Raf. Activating mutations affect thermal stability of MEK1 and its activity toward ERK2. PMID: 29018093
    5. Data indicate two atypical hairy cell leukemia (HCLc)- and hairy cell leukemia variant (HCLv)-like cases with clinically detected mitogen-activated protein kinase kinase 1 (MAP2K1) mutations. PMID: 27241017
    6. Reactive oxygen species-mediated EGFR/MEK/ERK/HIF-1A loop regulates glucose metabolism in pancreatic cancer. PMID: 29702094
    7. High MEK1 expression is associated with urinary bladder cancer metastasis. PMID: 28534984
    8. we detected mutually exclusive KRAS and MAP2K1 mutations in one-third of cases of Rosai-Dorfman disease PMID: 28664935
    9. The rs1549854 and rs1432441 polymorphisms of the MAP2K1 gene may be associated with major depressive disorder, especially in females. PMID: 28688265
    10. MEK1 does not act as a general tumor suppressor in leukemogenesis. Rather, its effects strongly depend on the genetic context (RAS versus MYC-driven leukemia) and on the cell type involved. PMID: 27741509
    11. Report a synthetic lethal interaction of cetuximab in combination with MEK1/2 inhibition for the NRAS mutant subgroup of metastatic colorectal cancer. PMID: 27636997
    12. High MEK1 expression is associated with liver cancer. PMID: 26967560
    13. The BRAF/MAP2K1-mut LCH cells had a more immature state than BRAF/MAP2K1-wt LCH cells. Authors also found the BRAFV600E and MAP2K1 mutations were significantly associated with pERK expression. PMID: 27597420
    14. There are no other biomarkers correlated with treatment responses following MEK1/2 inhibition. PMID: 27956260
    15. High MEK1 expression is associated with neuroblastoma. PMID: 28687621
    16. mutations in MAP2K1, which are frequently associated with neurological complications and intellectual disability, can be associated with a milder clinical and neurocognitive profile more typical of individuals with Noonan syndrome. Variability of expression may arise from a complex interplay between RAS/MAPK pathway genotype, epigenetics, medical and obstetric factors, and environmental influences. PMID: 27862862
    17. High MEK1 expression is associated with infant acute lymphoblastic leukemia. PMID: 27588400
    18. Data show that combined therapy using HER2 inhibitor and BRAF/MEK inhibitor presented more significant redifferentiation effect on papillary thyroid cancer cells harboring BRAFV600E than BRAF/MEK inhibitor alone. PMID: 28423638
    19. MEK1 is constitutively and mainly phosphorylated at the Thr-292, Ser-298, Thr-386, and Thr-388 residues in vivo, and combinations of phosphorylations at these four residues produce at least six phosphorylated variants of MEK1. The phosphorylation statuses of Thr-292, Ser-298, Thr-386, and Thr-388 residues vary widely during activation and deactivation of the MAPK pathway. PMID: 27169363
    20. TNFRSF14 and MAP2K1 mutations are the most frequent genetic alterations found in pediatric-type follicular lymphoma (PTFL) and occur independently in most cases, suggesting that both mutations might play an important role in PTFL lymphomagenesis. PMID: 28533310
    21. There was no statistically significant association between BRAF or MAP2K1 mutation and anatomic site, unifocal versus multifocal presentation, or clinical outcome in Langerhans cell histiocytosis. PMID: 26980021
    22. High MEK1 expression is associated with inflammation. PMID: 28178421
    23. Lgr4 is a critical positive factor for skin tumorigenesis by mediating the activation of MEK1/ERK1/2 and Wnt/beta-catenin pathways. PMID: 27693558
    24. somatic mutations in MAP2K1 are a common cause of extracranial arteriovenous malformation PMID: 28190454
    25. MEK1 mutation is associated with central nervous system metastases of non-small cell lung cancer. PMID: 26860843
    26. The MAP2K1 mutation analysis of three hairy cell leukemia cases, one hairy cell leukemia-variant case, and three splenic marginal zone lymphoma cases revealed negative results. PMID: 25729732
    27. Data show that mitogen-activated protein kinase kinases MEK1/2 inhibitor pimasertib (MEKI) sensitized the cells to apoptosis through its ability to promote a G1 cell cycle arrest. PMID: 26625317
    28. Specific inhibition of BRAF oncogene, MEK or p38 signaling was associated with decreases in DIO3 expression in papillary thyroid cancer cells PMID: 26825960
    29. Data show that Ba/F3 cells transformed with mutant HRAS protien indicated equal sensitivity towards Map kinase kinase (MEK) and mTOR serine-threonine kinase (mTOR) inhibition. PMID: 26544513
    30. Our data demonstrate that MEK inhibitors can inhibit breast cancer stem cells and may have clinical potential for the prevention of metastasis in certain cases in which tumors are MAPK dependent. PMID: 26384399
    31. Data show that src kinases (SRC) and mitogen-activated protein kinase kinase 1 (MEK) co-inhibition by saracatinib and PD0325901 respectively can be broadly effective in tumor growth control of a wide panel of non-small cell lung cancer (NSCLC) cell lines. PMID: 26358373
    32. at clinically relevant concentrations, cDDP binds to and inhibits MEK1/2 and both the binding and inhibitory activity are related to its interaction with Cu bound to MEK1/2 PMID: 26155939
    33. Studies indicate that concurrent inhibition of proto-oncogene protein B-raf (BRAF) and Map kinase kinase (MEK) improved the most effective therapeutic modality as compared as single BRAF or MEK inhibition for patients with metastatic melanoma (MM). PMID: 26143635
    34. Findings suggest that triple therapy directed against BRAF/MEK/ErbB3 may be able to provide durable control of BRAF mutated metastatic melanoma. PMID: 26208478
    35. MEK1 levels are upregulated at transcriptional level whereas MEK2 levels are downregulated at posttranslational level. PMID: 26163823
    36. NOTCH1, TP53, and MAP2K1 mutations in splenic diffuse red pulp small B-cell lymphoma are associated with progressive disease. PMID: 26426381
    37. MEK1/2 inhibitor trametinib showed similar PFS and a response rate as docetaxel in patients with previously treated KRAS-mutant-positive non-small cell lung carcinoma. PMID: 25722381
    38. Findings establish that the convergence of 2 distinct Ras effector pathways on mammalian target of rapamycin signaling maintains neurofibromatosis type 1 mouse optic glioma growth. PMID: 25534823
    39. MEK1 Mutations are associated with Low-grade Serous Ovarian Cancer. PMID: 26324360
    40. SGK1 inhibits intestinal epithelial cell apoptosis and promotes proliferation via the MEK/ERK/p53 pathway in colitis. PMID: 26034353
    41. MEK1 mutations define a distinct subset of lung cancers ( approximately 1%) with potential sensitivity to MEK inhibitors. Mutations are predominantly transversions, in keeping with a strong association with smoking. PMID: 25351745
    42. Data show that licochalcone A (LicoA) suppresses solar UV-induced cyclooxygenase (COX-2) expression by acting as a potent inhibitor of enzymes PI3K, MEK1, and B-Raf. PMID: 25710724
    43. Langerhans cell histiocytosis cells can harbor additional genetic alterations in the RAS-RAF-MEK pathway which, in the case of MAP2K1, may be responsible for ERK activation in a wild type BRAF setting. PMID: 25899310
    44. our data indicate that preexisting MEK1(P124) mutations are associated with a reduced response to BRAF inhibitor therapy and identify a subset of patients with BRAF-mutant melanoma likely to benefit from combination therapies PMID: 25370473
    45. MAP2K1 missense mutations were found in 2 of 11 patients with cadiofaciocutaneous syndrome: Pro124Gln and Asp67Asn. PMID: 25194980
    46. We documented three novel mutations in the BRAF gene in cardio-facio-cutaneous syndrome patients and correlated clinical findings with causative mutations in the BRAF or MEK1/MEK2 genes PMID: 25463315
    47. MEK1 is associated with carboplatin resistance and is a prognostic biomarker in epithelial ovarian cancer. PMID: 25408231
    48. Treatment of cells with sirtuin inhibitors, or siRNA knockdown of SIRT1 or SIRT2 proteins, increases MEK1 acetylation and subsequent phosphorylation of the extracellular signal-regulated kinase. PMID: 24681949
    49. MEK1/2 inhibitor potentiated the anti-tumor effects of cisplatin in KRAS-dependent lung cancer cells and an animal model through inhibition of BIM degradation PMID: 25541062
    50. Findings support the hypothesis that BDNF and MEK1 mRNA expression levels are more obviously decreased in patients with treatment-resistant depression. PMID: 24709918

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  • 相關疾病：
    Cardiofaciocutaneous syndrome 3 (CFC3)
  • 亞細胞定位：
    Cytoplasm, cytoskeleton, microtubule organizing center, centrosome. Cytoplasm, cytoskeleton, microtubule organizing center, spindle pole body. Cytoplasm. Nucleus. Membrane; Peripheral membrane protein.
  • 蛋白家族：
    Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase subfamily
  • 組織特異性：
    Widely expressed, with extremely low levels in brain.
  • 數據庫鏈接：

    HGNC: 6840

    OMIM: 176872

    KEGG: hsa:5604

    STRING: 9606.ENSP00000302486

    UniGene: Hs.145442



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