MITOTOX

Compound

D1447 | LDC203974

Structure
Description	Small-molecule inhibitors of human mitochondrial DNA transcription

Toxicity	Dose	Time	Model	Method	Action	Positive criterion	Reference
MITOCHONDRIAL TRANSCRIPTION	0–10 μM			Single nucleotide incorporation assays at varying ATP concentrations	inhibit	Vmax app, maximum reaction rate; Km app, substrate affinity	314
MITOCHONDRIAL TRANSCRIPTION	743nM			Microscale thermophoresis binding curves in the absence or presence of 10 μM IMT1B	inhibit	Kd	314
MITOCHONDRIAL TRANSCRIPTION	10 μM	6hr	HeLa cells	Mitochondrial transcript levels of ND1 and CYTB	inhibit		314

Target	Dose	Time	Model	Method	Action	Positive criterion	Reference
DNA-directed RNA polymerase, mitochondrial	0–10 μM			Single nucleotide incorporation assays at varying ATP concentrations	inhibit	Vmax app, maximum reaction rate; Km app, substrate affinity	314
DNA-directed RNA polymerase, mitochondrial	743nM			Microscale thermophoresis binding curves in the absence or presence of 10 μM IMT1B	inhibit	Kd	314
DNA-directed RNA polymerase, mitochondrial	10 μM	6hr	HeLa cells	Mitochondrial transcript levels of ND1 and CYTB	inhibit		314

(S)-1-((R)-2-((4 - (2-chloro - 4 - fluorophenyl) - 2-oxo-2H-chromen-7 - yl)oxy)propanoyl)piperidine - 3 - carboxylic acid

1. https://static-content.springer.com/esm/art%3A10.1038%2Fs41586-020-03048-z/MediaObjects/41586_2020_3048_MOESM1_ESM.pdf