1. Epigenetics Autophagy
  2. Histone Methyltransferase Autophagy
  3. BIX-01294

BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.

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CAS 番号 : 935693-62-2

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カスタマーレビュー

Based on 27 publication(s) in Google Scholar

Other Forms of BIX-01294:

Top Publications Citing Use of Products
Bio/Physico-chemical Assay
ELISA
Cell Proliferation/Viability Assay
WB
RT-PCR

    BIX-01294 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2025 Oct 10.  [Abstract]

    Both KL1 (40, 100 µM) and BIX-01294 (1, 4 µM) reduced ROS levels at 4 hpi. Chemiluminescent L-012 probes were used to quantify reactive species.

    BIX-01294 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2025 Oct 10.  [Abstract]

    Inhibition of EHMT2/G9a phenocopied KL1-mediated sensitization in intracellular S. aureus. A selective EHMT2/G9a inhibitor, BIX-01294 (BIX; 1–10 µM), increased the bioluminescence signal (grey bars) of strain JE2-lux compared to the vehicle control (Veh; 0.1% DMSO). Cytotoxicity of BIX was also assessed (red circles). Representative data of 3 experiments (n = 6, two-sided unpaired t-test) were obtained.

    BIX-01294 purchased from MedChemExpress. Usage Cited in: NPJ Regen Med. 2024 Apr 29;9(1):17.  [Abstract]

    CCL3 was found to be the most altered cytokine by inhibiting G9a using BIX-01294 (1 μM). Inhibition of G9a using BIX-01294 (1 μM) largely altered the secretion in the F-EPC and OVX-EPC. ELISA showed secretory upregulation of CCL3 and VEGF-A in M-EPC, F-EPC, and OVX-EPC with the inhibition of G9a using BIX-01294.

    BIX-01294 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 17;37(1):196.  [Abstract]

    The relative mRNA levels of Ki67 and PCNA in primary CRC cells responding to rhIL-33 (100 ng/mL) incubation and/ or indicated inhibitors (SB203580, 10 μg/mL; PD98059, 20 μg/mL; SP600125, 10 μg/mL; BIX01294, 2 μM; 5Aza, 10 μM; SC560, 0.1 μg/mL; celecoxib, 20 μg/mL) for 24 h.

    BIX-01294 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Apr 6;8(4):e2726.  [Abstract]

    Upper and middle panels: WB detection of H3K9me2 and G9A in PC9 and A549 cells treated with 0, 1, 2.5, 5 or 10 μM BIX-01294. The total level of histone H3 and actin serve as loading controls. Lower panel: WB detection of the total (T-) level of and phosphorylated (P-) ERK kinase in PC9 and A549 cells treated with 0, 1, 5 or 10 μM BIX-01294. GAPDH serves as the loading control
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    製品説明

    BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells[1][2][3][4][5].

    IC50 & Target[2]

    EHMT2/G9a/KMT1C

     

    EHMT1/GLP/KMT1D

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    2.8 3
    Compound: BIX01294
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    A549 IC50
    2.8 3
    Compound: BIX01294
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    HEK293 IC50
    2.05 3
    Compound: 38; BIX01294
    Cytotoxicity against HEK293 cells
    Cytotoxicity against HEK293 cells
    [PMID: 34107385]
    HeLa IC50
    0.966 3
    Compound: BIX-01294
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    [PMID: 29624387]
    HeLa IC50
    0.966 3
    Compound: BIX-01294
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    [PMID: 29624387]
    HepG2 IC50
    3.7 3
    Compound: BIX01294
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    A549 IC50
    2.8 3
    Compound: BIX01294
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    HepG2 IC50
    4800 1
    Compound: BIX01294; 1
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    [PMID: 29308121]
    HepG2 IC50
    3.7 3
    Compound: BIX01294
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    HL-60 IC50
    2.2 3
    Compound: BIX01294
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    HL-60 IC50
    2.2 3
    Compound: BIX01294
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    K562 IC50
    3.9 3
    Compound: BIX01294
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    K562 IC50
    3.9 3
    Compound: BIX01294
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    HEK293 IC50
    2.05 3
    Compound: 38; BIX01294
    Cytotoxicity against HEK293 cells
    Cytotoxicity against HEK293 cells
    [PMID: 34107385]
    MCF7 EC50
    3.3 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    HEK293 IC50
    2.05 3
    Compound: BIXO1294
    Cytotoxicity HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs
    Cytotoxicity HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs
    [PMID: 38056296]
    MCF7 EC50
    3.3 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    HFF IC50
    4997 1
    Compound: 18; BIX01294
    Cytotoxicity against HFF
    Cytotoxicity against HFF
    [PMID: 30366254]
    MDA-MB-231 EC50
    2.9 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    MDA-MB-231 EC50
    2.9 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    HL-60 IC50
    2.2 3
    Compound: BIX01294
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    MDA-MB-231 IC50
    9.6 3
    Compound: 133; BIX-01294
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 35531606]
    MDA-MB-231 IC50
    9.6 3
    Compound: 133; BIX-01294
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 35531606]
    MDA-MB-231 IC50
    500 1
    Compound: 37; BIX01294
    Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay
    Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay
    [PMID: 36528996]
    HepG2 IC50
    4800 1
    Compound: BIX01294; 1
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    [PMID: 29308121]
    HeLa IC50
    0.966 3
    Compound: BIX-01294
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    [PMID: 29624387]
    HFF IC50
    4997 1
    Compound: 18; BIX01294
    Cytotoxicity against HFF
    Cytotoxicity against HFF
    [PMID: 30366254]
    HepG2 IC50
    3.7 3
    Compound: BIX01294
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    Vero C1008 IC50
    1 3
    Compound: BIX-01294
    Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay
    Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay
    [PMID: 29624387]
    HepG2 IC50
    4800 1
    Compound: BIX01294; 1
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay
    [PMID: 29308121]
    K562 IC50
    3.9 3
    Compound: BIX01294
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
    [PMID: 27393948]
    L02 IC50
    4.28 3
    Compound: BIX-01294
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
    [PMID: 37788550]
    MCF7 EC50
    3.3 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    MDA-MB-231 EC50
    2.9 3
    Compound: 1; BIX01294
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    [PMID: 31627059]
    MDA-MB-231 EC50
    2700 1
    Compound: 2
    Antiproliferative activity against human MDA-MB-231 cells by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells by MTT assay
    [PMID: 38799223]
    MDA-MB-231 IC50
    500 1
    Compound: 2
    Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis
    Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis
    [PMID: 38799223]
    MDA-MB-231 IC50
    500 1
    Compound: 37; BIX01294
    Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay
    Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay
    [PMID: 36528996]
    MDA-MB-231 IC50
    9.6 3
    Compound: 133; BIX-01294
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
    [PMID: 35531606]
    Vero C1008 IC50
    1 3
    Compound: BIX-01294
    Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay
    Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay
    [PMID: 29624387]
    体外実験

    BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth[1].
    BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL[1].
    BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1].
    BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1].
    BIX-01294 leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h)[1].
    BIX-01294 (4.1 μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2].
    BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2].
    BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)[2].
    BIX-01294 (1 μg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF[3].

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

    Cell Viability Assay[1]

    Cell Line: Primary or recurrent tumor cells
    Concentration: 2 μM
    Incubation Time: 48 hours
    Result: Selectively inhibited recurrent tumor cell growth.
    体内実験

    BIX-01294 (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited[1].

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

    Animal Model: Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells[1]
    Dosage: 10 mg/kg
    Administration: IP; three times a week for 2 weeks
    Result: Significantly reduced tumor growth and tumor burden in recurrent tumor cells.
    Primary tumor growth was not inhibited.
    Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.
    分子量

    490.64

    分子式

    C28H38N6O2

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=C(OC)C=C(C(NC2CCN(CC3=CC=CC=C3)CC2)=NC(N4CCN(C)CCC4)=N5)C5=C1

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 110 mg/mL (224.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0382 mL 10.1908 mL 20.3815 mL
    5 mM 0.4076 mL 2.0382 mL 4.0763 mL
    10 mM 0.2038 mL 1.0191 mL 2.0382 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
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    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
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    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0382 mL 10.1908 mL 20.3815 mL 50.9539 mL
    5 mM 0.4076 mL 2.0382 mL 4.0763 mL 10.1908 mL
    10 mM 0.2038 mL 1.0191 mL 2.0382 mL 5.0954 mL
    15 mM 0.1359 mL 0.6794 mL 1.3588 mL 3.3969 mL
    20 mM 0.1019 mL 0.5095 mL 1.0191 mL 2.5477 mL
    25 mM 0.0815 mL 0.4076 mL 0.8153 mL 2.0382 mL
    30 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6985 mL
    40 mM 0.0510 mL 0.2548 mL 0.5095 mL 1.2738 mL
    50 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0191 mL
    60 mM 0.0340 mL 0.1698 mL 0.3397 mL 0.8492 mL
    80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6369 mL
    100 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5095 mL
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    製品名:
    BIX-01294
    製品番号:
    HY-10587
    数量:
    MCE 日本正規代理店: