polrmt

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

POLRMT-IN-2 is a potent inhibitor of POLRMT, exhibiting significant antiproliferative activity in MOLM-13 cells with an IC50 of 1.01 μM. It disrupts mitochondrial function and induces apoptosis, making it a valuable candidate for research in acute myeloid leukemia (AML).

POLRMT-IN-4 is a photoactivatable mitochondrial RNA polymerase (POLRMT) inhibitor. Upon exposure to light, POLRMT-IN-4 is released from its photoactivatable prodrug, enabling precise spatiotemporal inhibition and targeted tissue selectivity. It disrupts mitochondrial transcription, impairs oxidative phosphorylation, and inhibits the proliferation of cancer cells. POLRMT-IN-4 is useful in researching various cancers, such as pancreatic cancer.

POLRMT-IN-3 is a photoactivatable inhibitor of mitochondrial RNA polymerase (POLRMT). In its inactive form in darkness, POLRMT-IN-3 rapidly releases the active parent compound LJ03 when exposed to 405 nm light, enabling precise spatial and temporal inhibition of POLRMT. It exhibits anti-tumor activity and is useful for research in cancers like pancreatic and ovarian tumors.

POLRMT-IN-1 (compound S7) is an inhibitor of POLRMT, specifically utilized in cancer-related research.

YH-0623 is an orally active inhibitor of mitochondrial RNA polymerase (POLRMT) with an IC50 of 50.48 nM as determined by NanoBRET assay. It exhibits antiproliferative effects on 22Rv1 cells by downregulating mitochondrial gene expression. YH-0623 suppresses 22Rv1 cell growth, colony formation, and expression of proteins related to OXPHOS. Significant tumor growth inhibition was observed in a prostate cancer xenograft mouse model. YH-0623 is applicable for prostate cancer research.