2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. 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.

For research use only. We do not sell to patients.

IMT1B Chemical Structure

IMT1B Chemical Structure

CAS No. : 2304621-06-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 417 In-stock
Solution
10 mM * 1 mL in DMSO USD 417 In-stock
Solid
1 mg USD 190 In-stock
5 mg USD 400 In-stock
10 mg USD 680 In-stock
50 mg USD 1250 In-stock
100 mg USD 1680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

IMT1B Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

POLRMT[1]
In Vitro

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.

IMT1B Related Antibodies

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.
In Vivo

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).
Molecular Weight

473.88

Formula

C24H21ClFNO6
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (527.56 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
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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.08 mg/mL (4.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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.
Purity & Documentation
References

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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IMT1B Related Classifications

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.

Keywords:

IMT1B2304621-06-3LDC203974LDC 203974LDC-203974DNA/RNA SynthesismitochondrialDNAmtDNAhumanRNApolymerasePOLRMToxidativephosphorylationOXPHOSanti-tumourInhibitorinhibitorinhibit

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