1. Cell Cycle/DNA Damage
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  3. IMT1B

IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.

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CAS 番号 : 2304621-06-3

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 417 在庫あり
Solution
10 mM * 1 mL in DMSO USD 417 在庫あり
Solid
1 mg $190 在庫あり
5 mg $400 在庫あり
10 mg $680 在庫あり
50 mg $1250 在庫あり
100 mg $1680 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    IMT1B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 10;11(1):524.  [Abstract]

    Expression levels of the indicated mitochondrial encoded genes in SK-UT-1 cells treated with10 µM of XMH95, Hoechst 33258 or IMT1B. Incubation time was 18 hours for XMH95 and Hoechst 33258, and 48 hours for IMT1B. RNAs were extracted at the indicated processed for qRT-PCR.

    IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421.  [Abstract]

    Immunofluorescence staining of dsRNA and mitochondria in rNPCs pretreated with TLR4-IN-C34, MitoTempo or IMT1B (200 nM) for 1 h and then treated with LPS for 6 h.

    IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421.  [Abstract]

    cl2 and Ccl7 gene expression in rNPCs with or without IMT1B (200 nM) pretreatment for 1 h and LPS treatment for 6 h.

    IMT1B purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Feb;56(2):408-421.  [Abstract]

    IMT1B (200 nM) pretreatment for 1 h and LPS treatment for 6 h. The expression of PKR-ISR pathway-related proteins in rNPCs.

    IMT1B purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Nov;25(11):1575-1589.  [Abstract]

    qRT-PCR measurements of MT-CO1 mRNA levels after treatment with IMT1B (500nM) for indicated time in NT or NME6 KO K562 cells.

    DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

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    製品説明

    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects[1].

    IC50 & Target

    RNA Polymerase

     

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    0.138 μM
    Compound: IMT1B
    Antiproliferative activity against human A2780 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human A2780 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    A549 IC50
    0.881 μM
    Compound: IMT1B
    Antiproliferative activity against human A549 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human A549 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    CAPAN-1 IC50
    1.352 μM
    Compound: IMT1B
    Antiproliferative activity against human CAPAN-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    Antiproliferative activity against human CAPAN-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    [PMID: 39049433]
    DLD-1 IC50
    0.142 μM
    Compound: IMT1B
    Antiproliferative activity against human DLD-1 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human DLD-1 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    HeLa IC50
    1.052 μM
    Compound: IMT1B
    Antiproliferative activity against human HeLa cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human HeLa cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    HepG2 IC50
    0.168 μM
    Compound: IMT1B
    Antiproliferative activity against human HepG2 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human HepG2 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    HUVEC IC50
    >50 μM
    Compound: IMT1B
    Antiproliferative activity against HUVEC cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    Antiproliferative activity against HUVEC cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    [PMID: 39049433]
    IMR-90 IC50
    >50 μM
    Compound: IMT1B
    Antiproliferative activity against human IMR-90 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human IMR-90 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    MDA-MB-231 IC50
    >10 μM
    Compound: IMT1B
    Antiproliferative activity against human MDA-MB-231 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human MDA-MB-231 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    MDA-MB-468 IC50
    0.189 μM
    Compound: IMT1B
    Antiproliferative activity against human MDA-MB-468 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human MDA-MB-468 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    MIA PaCa-2 IC50
    0.152 μM
    Compound: IMT1B
    Antiproliferative activity against human MIA PaCa-2 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human MIA PaCa-2 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    MIA PaCa-2 IC50
    0.159 μM
    Compound: IMT1B
    Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    Antiproliferative activity against human MIA PaCa-2 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    [PMID: 39049433]
    NCI-H1975 IC50
    0.221 μM
    Compound: IMT1B
    Antiproliferative activity against human NCI-H1975 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human NCI-H1975 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    NCI-H3122 IC50
    >10 μM
    Compound: IMT1B
    Antiproliferative activity against human NCI-H3122 cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human NCI-H3122 cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    PANC-1 IC50
    1.566 μM
    Compound: IMT1B
    Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 168 hrs incubation by SRB assay
    [PMID: 39049433]
    PBMC IC50
    >50 μM
    Compound: IMT1B
    Antiproliferative activity against human PBMC cells incubated for 168 hrs by SRB method
    Antiproliferative activity against human PBMC cells incubated for 168 hrs by SRB method
    [PMID: 36997840]
    体外実験

    IMT1B is a noncompetitive inhibitor that causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro[1].
    IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells[1].
    IMT1B depletes cellular metabolites[1].
    IMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK[1].

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

    Cell Viability Assay[1]

    Cell Line: A2780 cells
    Concentration: 0.01 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
    Incubation Time: 72 hours, 96 hours, 168 hours
    Result: Decreased cell viability in a dose-dependent manner.
    体内実験

    IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts[1].
    IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours[1].
    IMT1B exhibits good oral bioavailability (mice 101 %) and Cmax (mice 5149 ng/mL) following oral administration (mice 10 mg/kg)[1].
    IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (mice 0.44 L/h/kg) following intravenous administration (mice 1 mg/kg)[1].

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

    Animal Model: 7-9 weeks female BALB/c nude mice, with A2780 cells xenograft[1]
    Dosage: 100 mg/kg
    Administration: Oral administration, daily, for four weeks
    Result: Led to a clear reduction of tumour volume.
    Animal Model: Mice[1]
    Dosage: 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous administration and oral administration
    Result: Oral bioavailability (101%), Cmax (5149 ng/mL), T1/2 (1.88 h).
    分子量

    473.88

    分子式

    C24H21ClFNO6

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@H]1CN(C([C@H](OC2=CC=C(C(O3)=C2)C(C4=CC=C(F)C=C4Cl)=CC3=O)C)=O)CCC1)O

    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 : 200 mg/mL (422.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1102 mL 10.5512 mL 21.1024 mL
    5 mM 0.4220 mL 2.1102 mL 4.2205 mL
    10 mM 0.2110 mL 1.0551 mL 2.1102 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.

    • Molarity Calculator

    • Dilution Calculator

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    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

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    体内:

    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:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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: ≥ 5 mg/mL (10.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

      Solubility: ≥ 5 mg/mL (10.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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    (per animal)

    g

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    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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 2.1102 mL 10.5512 mL 21.1024 mL 52.7560 mL
    5 mM 0.4220 mL 2.1102 mL 4.2205 mL 10.5512 mL
    10 mM 0.2110 mL 1.0551 mL 2.1102 mL 5.2756 mL
    15 mM 0.1407 mL 0.7034 mL 1.4068 mL 3.5171 mL
    20 mM 0.1055 mL 0.5276 mL 1.0551 mL 2.6378 mL
    25 mM 0.0844 mL 0.4220 mL 0.8441 mL 2.1102 mL
    30 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7585 mL
    40 mM 0.0528 mL 0.2638 mL 0.5276 mL 1.3189 mL
    50 mM 0.0422 mL 0.2110 mL 0.4220 mL 1.0551 mL
    60 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.8793 mL
    80 mM 0.0264 mL 0.1319 mL 0.2638 mL 0.6594 mL
    100 mM 0.0211 mL 0.1055 mL 0.2110 mL 0.5276 mL
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    • Molarity Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    製品名:
    IMT1B
    製品番号:
    HY-137067
    数量:
    MCE 日本正規代理店: