IMT1B - 10mM in DMSO , CAS No.2304621-06-3

CAS: 2304621-06-3 Cat. No.: I656332 Molecular Weight: 473.88 PubChem CID: 138490769

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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

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. ?\nIMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells. ?\nIMT1B depletes cellular metabolites. ?\nIMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 . ?\nIMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours . ?\nIMT1B exhibits good oral bioavailability (mice 101 %) and C max (mice 5149 ng/mL) following oral administration (mice 10 mg/kg) . ?\nIMT1B 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) . 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 Dosage: 100 mg/kg Administration: Oral administration, daily, for four weeks Result: Led to a clear reduction of tumour volume. Animal Model: Mice Dosage: 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) Administration: Intravenous administration and oral administration Result: Oral bioavailability (101%), C max (5149 ng/mL), T 1/2 (1.88 h).

IC50& Target:POLRMT

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• PubChem CID: 138490769
• Molecular Weight: 473.88