LDC195943 (IMT1)

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LDC195943 (IMT1)
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Size Price Stock
100mg$1200In Stock
250mg$1950In Stock
500mg$2925In Stock

Cat #: V2257 CAS #: 2304621-31-4 Purity ≥ 99%

Description: LDC195943 (also known as IMT1) is a novel, potent and highly specific inhibitor of POLRMT (human mitochondrial RNA polymerase) with anticancer activity.

References: Nina A Bonekamp, et al. Small-molecule inhibitors of human mitochondrial DNA transcription. Nature. 2020 Dec;588(7839):712-716.

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Molecular Weight (MW)351.40
Molecular FormulaC21H21NO4
CAS No.2304621-31-4
Synonyms LDC 195943; LDC-195943; LDC195943;  IMT1; IMT 1; IMT-1
ProtocolIn VitroPOLRMT is essential for mtDNA transcription and biogenesis of the oxidative phosphorylation (OXPHOS) system. IMT1 severely impairs mtDNA gene expression in A2780 cells that express wild-type POLRMT, whereas cells that express mutant POLRMT (L796Q or L816Q) are resistant. IMT1 reveals a time-dependent and marked increase in the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK in A2780 cells. IMT1 (0.01-10 μM; for 24-200 h) causes a dose-dependent decrease in the levels of mitochondrial transcripts and gradual depletion of mtDNA in HeLa cells. There is a dose-dependent decrease in the levels of subunits (NDUFB8, UQCRC2 and COXI) of respiratory chain complexes I, III and IV. IMT1 (0.00001-10 μM; 0-168 h) has a dose-dependent decrease in cell viability in A2780, A549 and HeLa cells. IMT1 shows a strong decrease in cell viability in about one third of the cancer cell lines, 89 cancer cell lines and primary cells (IMR90 lung fibroblasts and human peripheral blood mononuclear cells (PBMCs)), whereas primary cells remained unresponsive.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.8458 mL14.2288 mL28.4576 mL56.9152 mL
5mM0.5692 mL2.8458 mL5.6915 mL11.3830 mL
10mM0.2846 mL1.4229 mL2.8458 mL5.6915 mL
20mM0.1423 mL0.7114 mL1.4229 mL2.8458 mL
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.