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methylations

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10586
    5-Azacytidine
    Maximum Cited Publications
    128 Publications Verification

    Azacitidine; 5-AzaC; Ladakamycin

    Organoid Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Infection Cancer
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes . 5-Azacytidine induces cell autophagy .
    5-Azacytidine
  • HY-139664
    GSK-3685032
    10+ Cited Publications

    DNA Methyltransferase Cancer
    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    GSK-3685032
  • HY-101938
    Sinefungin
    4 Publications Verification

    Adenosyl-Ornithine; A-9145; Antibiotic 32232RP

    Histone Methyltransferase Fungal Antibiotic Parasite Infection Inflammation/Immunology
    Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication . Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation .
    Sinefungin
  • HY-134124

    Reactive Oxygen Species (ROS) Metabolic Disease
    Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .
    Glutathione ethyl ester
  • HY-W012078
    5-Methyl-2'-deoxycytidine
    3 Publications Verification

    5-Methyldeoxycytidine

    DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells .
    5-Methyl-2'-deoxycytidine
  • HY-111558
    Bobcat339
    20+ Cited Publications

    DNA Methyltransferase TET Protein Cancer
    Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
    Bobcat339
  • HY-30008
    Cycloleucine
    5+ Cited Publications

    iGluR Infection Neurological Disease Metabolic Disease Cancer
    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects .
    Cycloleucine
  • HY-103236
    NSC232003
    5 Publications Verification

    E1/E2/E3 Enzyme Cancer
    NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
    NSC232003
  • HY-111558A
    Bobcat339 hydrochloride
    20+ Cited Publications

    DNA Methyltransferase TET Protein Cancer
    Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
    Bobcat339 hydrochloride
  • HY-113081
    1-Methyladenosine
    4 Publications Verification

    Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis .
    1-Methyladenosine
  • HY-W015114

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid disodium
  • HY-124124
    N-Methylnicotinamide
    1 Publications Verification

    Endogenous Metabolite Drug Metabolite Cardiovascular Disease Metabolic Disease Cancer
    N-Methylnicotinamide is an endogenous metabolite with antithrombotic effect. N-Methylnicotinamide via production/release of prostacyclin inhibits arterial thrombosis development. N-Methylnicotinamide is also the N-methylation product from nicotinamide catalyzed by N-methyltransferase within nicotinate and nicotinamide metabolism pathway .
    N-Methylnicotinamide
  • HY-102047B
    KDOAM-25 citrate
    5+ Cited Publications

    Histone Demethylase Cancer
    KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25 citrate
  • HY-16513
    VAL-083
    2 Publications Verification

    Dianhydrodulcitol; Dianhydrogalactitol

    DNA Alkylator/Crosslinker Cancer
    VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
    VAL-083
  • HY-19980A
    PRIMA-1
    2 Publications Verification

    NSC-281668

    Autophagy MDM-2/p53 Ferroptosis Apoptosis Cancer
    PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
    PRIMA-1
  • HY-113039

    (S)-2-Hydroxyglutaric acid

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid
  • HY-P1108A
    Astressin 2B TFA
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B TFA
  • HY-P1108
    Astressin 2B
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B
  • HY-113138
    3-Methyluridine
    1 Publications Verification

    N3-Methyluridine

    Endogenous Metabolite Metabolic Disease
    3-Methyluridine (m 3U; N3-Methyluridine) is a methylated nucleotide present in ribosomal RNA (rRNA), mainly targeting specific base sites of RNA molecules such as 23S rRNA. 3-Methyluridine can introduce a methyl group at the N3 position of uracil, affecting the secondary structure stability and base pairing ability of RNA, and regulating ribosome function. For example, it affects ribosomal subunit binding and tRNA interaction. 3-Methyluridine is often used as a key raw material for the synthesis of modified nucleotides, and is used to construct RNA oligonucleotides containing methylation modifications to study the effects of RNA methylation on gene expression and drug resistance .
    3-Methyluridine
  • HY-30170

    Endogenous Metabolite Adrenergic Receptor Neurological Disease
    N-Methylphenethylamine is an indirectly acting sympathomimetic amine that is formed via PNMT-catalyzed N-methylation of phenethylamine (PEA) in the human body. N-Methylphenethylamine exhibits affinity for β-adrenergic receptors on the surface of cancer cells or bacterial cells. N-Methylphenethylamine can be used for neurotransmitter research or as a pharmaceutical intermediate .
    N-Methylphenethylamine
  • HY-157719

    COMT Others
    S-Adenosylhomocysteine sulfoxide is an inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. S-Adenosylhomocysteine sulfoxide can be used in the research of methylation reaction modulators .
    S-Adenosylhomocysteine sulfoxide
  • HY-112080

    Histone Methyltransferase Cancer
    BAY-6035, a chemical probe, is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM .
    BAY-6035
  • HY-111130

    Histamine Receptor mAChR Neurological Disease Cancer
    Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats .
    Methapyrilene
  • HY-N0739
    Betaine chloride
    5 Publications Verification

    Endogenous Metabolite Others
    Betaine chloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
    Betaine chloride
  • HY-122635A

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .
    T-448
  • HY-D1603

    Fluorescent Dye Others
    BODIPY FL-EDA is a widely used fluorescent dye for quantitative analysis of nucleotides. BODIPY FL-EDA is an aliphatic amine analog that can react with aldehydes and ketones. BODIPY FL-EDA can be used to detect both modified and unmodified deoxynucleotides and to determine DNA damage and genomic DNA methylation through capillary electrophoresis with laser-induced fluorescence (CE-LIF). Additionally, it can be used for quantifying intracellular ATP levels. The excitation wavelength is 500 nm, and the emission wavelength is 510 nm .
    BODIPY FL-EDA
  • HY-W740027

    5-Methyldeoxycytidine-d3

    Isotope-Labeled Compounds DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine-d3 (5-Methyldeoxycytidine-d3) is the deuterium labeled Methyl-2'-deoxycytidine (HY-W012078). 5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells .
    5-Methyl-2'-deoxycytidine-d3
  • HY-134828
    AZ506
    2 Publications Verification

    Histone Methyltransferase Cancer
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal .
    AZ506
  • HY-12759
    CARM1-IN-1
    4 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1
  • HY-12759A
    CARM1-IN-1 hydrochloride
    4 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1 hydrochloride
  • HY-152296

    Nucleoside Antimetabolite/Analog Bacterial Infection
    8-Methyladenosine is a modified adenosine nucleoside. Through methylation at the 8-position, 8-Methyladenosine confers bacterial resistance to five classes of antibiotics that bind to the ribosomal peptidyl transferase center. 8-Methyladenosine can be used in studies of antibiotic-resistant bacterial infections .
    8-Methyladenosine
  • HY-Q36691

    Histone Methyltransferase Cancer
    PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation .
    PRMT5-IN-30
  • HY-102047

    Histone Demethylase Cancer
    KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25
  • HY-P2258

    Histone Methyltransferase Others
    Histone H3 (1-34) is a peptide derived from human histone isotype 3.1. Histones are the main protein components of eukaryotic chromatin. Histone variants and histone modifications modulate chromatin structure, ensuring the precise operation of cellular processes associated with genomic DNA .
    Histone H3 (1-34)
  • HY-121095

    Histone Demethylase Neurological Disease Cancer
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects .
    Bizine
  • HY-106689

    DHAC; NSC 264880

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Cancer
    Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity .
    Dihydro-5-azacytidine
  • HY-P10387A
    RSM3 TFA
    1 Publications Verification

    METTL3 Apoptosis Cancer
    RSM3 TFA is a METTL3-METTL14 complex inhibitor with a Kd of 3.10 μM for the METTL3-METTL14 complex. RSM3 TFA reduces the m 6A modification level of SLC31A1 and the global RNA methylation level. RSM3 TFA upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 TFA is applicable to the research of preeclampsia and cancer .
    RSM3 TFA
  • HY-125980
    LX-3
    1 Publications Verification

    p38 MAPK Cancer
    LX-3 is a selective activator of the p38 MAPK signaling pathway and activates EGFP reporter genes that are silenced by DNA methylation, such as TNF, EGR1, LY6K, and ISG20 .
    LX-3
  • HY-W017077

    4-Phenyltoluene

    Drug Intermediate Inflammation/Immunology
    4-Methylbiphenyl (4-Phenyltoluene) is an organic compound. 4-Methylbiphenyl has excellent chemical stability and antioxidant properties, and is widely used in industry. 4-Methylbiphenyl can serve as a solvent, coating additive, plastic additive and dye intermediate .
    4-Methylbiphenyl
  • HY-P10463

    Histone Methyltransferase Cancer
    ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36
  • HY-145654

    Adenosine Kinase Cancer
    MRS-4203 is an ADK (IC50 = 88 nM) inhibitor. MRS-4203 can reduce DNA methylation. MRS-4203 is commonly used in cancer research .
    MRS-4203
  • HY-W014004

    CBHA

    HDAC Apoptosis Others Cancer
    m-Carboxycinnamic acid bishydroxamide (CBHA) is a histone deacetylase inhibitor. m-Carboxycinnamic acid bishydroxamide modulates histone acetylation sites, alters DNA methylation and epigenetic status, increases global histone acetylation, alleviates transcription repression, and facilitates chromatin remodelling. m-Carboxycinnamic acid bishydroxamide can be used for the research of cloned embryo development and epigenetic regulation .
    m-Carboxycinnamic acid bishydroxamide
  • HY-W850994

    Tridecyl beta-D-maltopyranoside

    Biochemical Assay Reagents Others
    Tridecyl β-D-maltopyranoside is a synthetic sugar, modified by fluorination and methylation. Carbohydrates can be used for the synthesis of glycosylated proteins (biosynth: W-204093).
    Tridecyl β-D-maltopyranoside
  • HY-P2255

    Histone Demethylase Others
    H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
    H3K4(Me) (1-20)
  • HY-103641C

    Octyl-2-HG

    Histone Methyltransferase Cancer
    Octyl-α-hydroxyglutarate (octyl-2-HG) increases histone methylation and enhances viability of LMP1-negative NPC cells .
    Octyl-α-hydroxyglutarate
  • HY-N0739R

    Reference Standards Endogenous Metabolite Others
    Betaine (chloride) (Standard) is the analytical standard of Betaine (chloride). This product is intended for research and analytical applications. Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
    Betaine chloride (Standard)
  • HY-P10463A

    Histone Methyltransferase Cancer
    ssK36 TFA is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2) , and ssK36 TFA is designed for the SETD2 protein, a specific PKMT. ssK36 TFA is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 TFA can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 TFA can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36 TFA
  • HY-B1481A

    Isoetarine

    Adrenergic Receptor Cardiovascular Disease Inflammation/Immunology
    Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
    Isoetharine
  • HY-111589

    Histone Methyltransferase Cancer
    EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research .
    EPZ-4777
  • HY-161334

    Histone Methyltransferase Apoptosis Cancer
    CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
    CARM1-IN-4

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