2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. DNA/RNA Synthesis PDGFR Oxidative Phosphorylation Mitochondrial Metabolism
  4. YH-0623

YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibited tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research.

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YH-0623

YH-0623 Chemical Structure

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YH-0623 Related Antibodies

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Description

YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibited tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research[1].

In Vitro

YH-0623 reduces the ND1 mitochondrial factor to 14%, exhibits antiproliferative activity on 22Rv1, C42B, VCap, LNCap, MDA-PCa-2b cells, with IC50s of 0.045, 0.64, 1.988, 1.941 μM, exhibits minimal cytotoxicity to WPMY-1 cells, with an IC50 >100 μM[1].
YH-0623 (1-500 nM) inhibits mitochondrial transcription and mitochondrial-related gene expression in 22Rv1 cells, resulting in reduced expression of mtDNA-encoded OXPHOS proteins while preserving expression of nuclear-encoded proteins[1].
YH-0623 (1 μM, 12 h) accumulates in mitochondria at a concentration of 767.07 ng/mg/protein in 22Rv1 cells[1].
YH-0623 (50-500 nM, 96 h) inhibits mitochondrial function primarily by suppressing OXPHOS without significantly altering MMP, ROS levels, or glycolytic activity in 22Rv1 cells[1].
YH-0623 (10 μM, 96 h) displays inhibitory effect against PDGFRα (IC50 ∼ 10 μM), achieving an inhibition rate of 55.97%[1].
YH-0623 leads to a significant decrease in the levels of several key amino acids, including L-Leucine, L-Valine, L-Alanine, L-Glutamine, L-Isoleucine, L-Aspartic acid, L-Tyrosine, L-Phenylalanine, Phosphorylcholine, L-Lysine, Choline, and L-Threonine, decreases amino acids, causes severe nutrient depletion in 22Rv1 cells[1].
YH-0623 (0.3-30 μM) exhibits minimal hERG channel inhibition (IC50 30 μM), suggesting a low potential for cardiac toxicity[1].

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

YH-0623 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 1, 5,,10, 50, 100, 200, 500 nM
Incubation Time: 4 days
Result: Induced a dose-dependent downregulation of specific subunits of respiratory chain complexes encoded by mtDNA, including NDUFB8 (complex I), UQCRC2 (complex III), and COX1 (complex IV), subunits encoded entirely by nuclear DNA, such as SDHB (complex II) and ATP5A, remained unaffected.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 100 nM
Incubation Time: 30 min
Result: Stabilized POLRMT.

Cell Migration Assay [1]

Cell Line: 22Rv1 cells
Concentration: 0, 0.01, 0.02, 0.04, 0.08, 0.156, 0.312, 0.625, 1.25, 2.5, 5, and 10 μM
Incubation Time: 14 days
Result: Suppressed proliferation in a concentration-dependent manner.
In Vivo

YH-0623 (50-100 mg/kg, p.o., once a day, 18 days) possesses a potent antitumor activity and an excellent safety profile in 22Rv1 xenograft mouse model[1].

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

Animal Model: 22Rv1 (1 × 106) xenograft mouse (balb/c nude mice, 18-22 g) model[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: p.o., once a day, 18 days
Result: Reduced tumor volume in a dose-dependent manner, resulted in a 51.7% and 58.5% reduction in tumor weight at 50 mg/kg and 100 mg/kg after 18 days.
Did not induce significant weight loss and apoptosis.
Molecular Weight

436.48

Formula

C25H25FN2O4
SMILES

O=C([C@H](OC1=CC2=NC=CC(C3=CC=CC=C3C)=C2C=C1F)C)N4CCC[C@@H](C4)C(O)=O
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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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YH-0623 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:

YH-0623YH0623YH 0623DNA/RNA SynthesisPDGFROxidative PhosphorylationMitochondrial MetabolismPlatelet-derived growth factor receptorInhibitor22Rv1 cellsprostate cancerinhibitorinhibit

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