IMT1 - 10mM in DMSO , CAS No.2304621-31-4

CAS: 2304621-31-4 Cat. No.: I655153 Formula: C₂₁H₂₁NO₄ Peso molecolare: 351.40 PubChem CID: 138490559

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases.

In Vitro

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. 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 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 severely impairs mtDNA gene expression in A2780 cells that express wild-type POLRMT, whereas cells that express mutant POLRMT (L796Q or L816Q) are resistant. POLRMT is essential for mtDNA transcription and biogenesis of the oxidative phosphorylation (OXPHOS) system. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A2780, A549 and HeLa cells Concentration: 0.00001-10 μM Incubation Time: 0-168 hours Result: Had a dose-dependent decrease in cell viability in A2780, A549 and HeLa cells, but had not cytotoxic to human PBMCs or pooled primary human hepatocytes.

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deox

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

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Tipo di azione

INHIBITOR

Nomi e identificatori

• PubChem CID: 138490559
• Peso molecolare: 351.40

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2304621-31-4, the molecular formula is C21H21NO4, and the molecular weight is 351.40 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.