2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Mitochondrial Metabolism DNA/RNA Synthesis Oxidative Phosphorylation
  4. POLRMT-IN-4

POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer.

For research use only. We do not sell to patients.

POLRMT-IN-4

POLRMT-IN-4 Chemical Structure

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POLRMT-IN-4 Related Antibodies

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Description

POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer[1].

IC50 & Target

RNA Polymerase

 

In Vitro

POLRMT-IN-4 (LJ03) (168 h) inhibits the proliferation of MIA PaCa-2 pancreatic cancer cells with an IC50 of 0.127 μM and HEK293T normal cells with an IC50 of 0.327 μM[1].
POLRMT-IN-4 (LJ03) (500 nM; 12 h) reduces the mitochondrial ND1 transcript level in MIA PaCa-2 cells to 22.2% of control and in HEK293T cells to 39.9% of control[1].
POLRMT-IN-4 (LJ03) (25-100 nM; 14 days) significantly suppresses colony formation of MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (500 nM; 96 h) does not perturb cell cycle progression in MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (500 nM; 96 h) does not trigger apoptotic pathways in MIA PaCa-2 cells[1].
POLRMT-IN-4 (LJ03) (168 h) exhibits broad-spectrum antiproliferative activity against multiple cancer cell lines (A2780, HeLa, A431, MDA-MB-468, HepG2) with activity unaffected by irradiation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

POLRMT-IN-4 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 500 nM
Incubation Time: 96 h
Result: Did not cause significant changes in the distribution of MIA PaCa-2 cells across G1, S, and G2 phases after 96 h of incubation in the dark or upon light irradiation.

Apoptosis Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 500 nM
Incubation Time: 96 h
Result: Did not induce significant early or late apoptotic markers in MIA PaCa-2 cells after 96 h of incubation in the dark or upon light irradiation.
In Vivo

POLRMT-IN-4 (LJ03) (500 nM; aquatic exposure; 3 days) exhibits significant tumor growth inhibition in a zebrafish pancreatic cancer xenograft model under dark conditions[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zebrafish (Danio rerio, AB strain) bearing MIA PaCa-2 cells.[1]
Dosage: 500 nM
Administration: Aqueous exposure; 3 days
Result: Significantly suppressed tumor-associated fluorescence intensity.
Molecular Weight

410.44

Formula

C23H23FN2O4
SMILES

O=C1C=C(C2=CC=CC=C2C)C3=C(O1)C=C(O[C@H](C)C(N4CCNCC4)=O)C(F)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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POLRMT-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

POLRMT-IN-4Mitochondrial MetabolismDNA/RNA SynthesisOxidative Phosphorylationoxidative phosphorylationlung cancercolorectal cancermitochondrial transcriptionPOLRMTmitochondrial RNA polymeraseosteosarcomaMIA PaCa-2 pancreatic cancer cellspancreatic cancerHEK293T normal cellsInhibitorinhibitorinhibit

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