IMT1B

IMT1B : Allosteric inhibitor of POLRMT

Structure

SERP Rating

Probe IMT1B is in the process of SERP review.

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Information

POLRMT

Allosteric

up to 10 uM

In Vitro Validations

Uniprot ID: O00411

Target Class: Enzyme

Target SubClass: RNA Polymerase

Potency: ΔTm

Potency Value: 5 K

Potency Assay: Differential scanning fluorimetry performed in the absence or presence of 10 μM IMT1B

PDB ID for probe-target interaction (3D structure): 7A8P

Target aliases:

DNA-directed RNA polymerase, mitochondrial, POLRMT ...

DOI Reference: 10.1038/s41586-020-03048-z

Uniprot ID: O00411

Target Class: Enzyme

Target SubClass: RNA Polymerase

Potency Value: Km 14.2 ± 6.4 nM

Potency Assay: Single nucleotide incorporation assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

DNA-directed RNA polymerase, mitochondrial, POLRMT ...

DOI Reference: 10.1038/s41586-020-03048-z

Uniprot ID: O00411

Target Class: Enzyme

Target SubClass: RNA Polymerase

Potency: IC50

Potency Value: about 50 nM

Potency Assay: in vitro promoter-dependent transcription on linear LSP and supercoiled circular LSP templates

PDB ID for probe-target interaction (3D structure): --

Target aliases:

DNA-directed RNA polymerase, mitochondrial, POLRMT ...

DOI Reference: 10.1038/s41586-020-03048-z

Uniprot ID: O00411

Target Class: Enzyme

Target SubClass: RNA Polymerase

Potency: IC50

Potency Value: 748 nM

Potency Assay: Microscale thermophoresis binding curves in the absence or presence of 10 μM IMT1B, causing a dose-dependent decrease in the levels of mitochondrial transcripts.

PDB ID for probe-target interaction (3D structure): --

Target aliases:

DNA-directed RNA polymerase, mitochondrial, POLRMT ...

DOI Reference: 10.1038/s41586-020-03048-z

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): IMT1B did not inhibit budding yeast mitochondrial RNA polymerase (RPO41), bacteriophage T7 RNA polymerase, Escherichia coli RNA polymerase or a reverse transcriptase. In addition, IMT1B did not inhibit the human multi-subunit RNA polymerase II (RNA Pol II) in vitro and had no effect on RNA Pol I-, II- and III-dependent transcript levels in cell lines. Furthermore, IMT1B did not inhibit human mitochondrial DNA polymerase γ in vitro or mitochondrial protein synthesis in organello

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