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 inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research.
For research use only. We do not sell to patients.
- Formula: C25H25FN2O4
- Molecular Weight:436.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
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Biological Activity
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RNA Polymerase |
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.
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Cell Line:22Rv1 cells
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Concentration:1, 5,,10, 50, 100, 200, 500 nM
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Incubation Time:4 days
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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.
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Cell Line:22Rv1 cells
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Concentration:100 nM
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Incubation Time:30 min
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Result:Stabilized POLRMT.
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Cell Line:22Rv1 cells
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Concentration:0, 0.01, 0.02, 0.04, 0.08, 0.156, 0.312, 0.625, 1.25, 2.5, 5, and 10 μM
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Incubation Time:14 days
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Result:Suppressed proliferation in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:22Rv1 (1 × 106) xenograft mouse (balb/c nude mice, 18-22 g) model[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:p.o., once a day, 18 days
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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.
Chemical Information
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Molecular Weight 436.48
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Formula C25H25FN2O4
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)