YM-53601

SKU: orb1701462

Description

YM-53601 is a potent inhibitor of squalene synthase (FDFT1), functioning as a cholesterol-lowering agent in rodent models. It demonstrates research utility in studies of lipid metabolism, adipogenesis, and has shown potential antiviral and chemosensitizing effects in hepatocellular carcinoma research in vivo.

Research Area

Epigenetics & Chromatin, Infectious Disease & Virology, Metabolism Research, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 182959-33-7
• MW: 372.86
• Purity: 99.65% (May vary between batches)
• Formula: C₂₁H₂₂ClFN₂O
• SMILES: O(C/C(/F)=C\1/C2CCN(C1)CC2)C=3C=C4C(C=5C(N4)=CC=CC5)=CC3.Cl
• Target: PKC,HCV Protease,Transferase
• Solubility: DMSO:80 mg/mL (214.56 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (8.85 mM)

Bioactivity

• Target IC50:
  HepG2 cells (rat liver microsomes):90 nM|HepG2 cells (human liver microsomes):79 nM|HepG2 cells (hamster liver microsomes):170 nM|Squalene synthase (hamster liver):170 nM|HepG2 cells (rhesus monkey liver microsomes):45 nM|HepG2 cells (guinea pig liver microsomes):46 nM
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• In Vivo:
  YM-53601 inhibited cholesterol biosynthesis in rats at an ED50 of 32 mg/kg . In addition, in a hamster model, YM-53601 reduced plasma non-HDL cholesterol levels by approximately 70% when administered orally at 50 mg/kg/day for 5 days. YM-53601 also enhanced doxorubicin-mediated inhibition of hepatocellular carcinoma (HCC) cell proliferation and cell death in vivo.
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• In Vitro:
  YM-53601 inhibited squalene synthase activity in a variety of animal and human cell lines, with IC50s of 90, 170, 46, 45, and 79 nM in liver microsomes of rat, hamster, guinea pig, rhesus monkey, and human HepG2 cells, respectively. YM-53601 inhibited the conversion of [3H] farnesyl diphosphate to [3H] squalene by squalene synthase in hamster liver with an IC50 of 170 nM. In H35 cells, 1 μM M-53601 enhanced sensitivity to toxic carotenoids, lonidamine and adriamycin, and reduced mitochondrial cholesterol levels in H35 and HepG2 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YM 53601, YM53601, YM-53601

Compound Identifiers

PubChem CID

60196293