2. Metabolic Enzyme/Protease Anti-infection
  3. Farnesyl Transferase HCV
  4. YM-53601

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

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YM-53601 Chemical Structure

YM-53601 Chemical Structure

CAS No. : 182959-33-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1107 In-stock
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Solid
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5 mg USD 1350 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].

In Vitro

YM-53601 inhibits squalene synthase activities in hepatic microsomes from several species of rat, hamster, guinea-pig, rhesus monkey, and human-derived HepG2 cell with IC50s of 90, 170, 46, 45, and 79 nM, respectively[1].
YM-53601 inhibits conversion of [3H]farnesyl diphosphate to [3H]squalene by hamster liver squalene synthase with the IC50 of 170 nM[2].
YM-53601 (1 μM) potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells[4].

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

YM-53601 Related Antibodies

Cell Viability Assay[4]

Cell Line: H35 and HepG2 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Reduced the mitochondrial cholesterol levels in both H35 and HepG2 cells.
In Vivo

YM-53601 suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg)[1].
YM-53601 also reduces plasma non-HDL cholesterol levels in hamsters by approximately 70% at an oral dose of 50 mg/kg/day for 5 days[2].
YM-53601 potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo[4].

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

Animal Model: Sprague-Dawley (SD) rats weighing 150-170 g[1]
Dosage: 6.25, 12.5, 25 or 50 mg/kg
Administration: Given a single p.o.
Result: Inhibited cholesterol biosynthesis from acetate in a dose-dependent manner in rats. The ED50 value for YM-53601 cholesterol biosynthesis inhibition is 32  mg/kg.
Animal Model: Five- to six-week-old male BALB/c athymic (nu/nu) nude mice[4]
Dosage: 15 mg/kg
Administration: 2 wk of daily treatment by p.o. gavage
Result: Significantly decreased the intratumor cholesterol levels.
Molecular Weight

372.86

Formula

C21H22ClFN2O
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

F/C(COC1=CC(NC2=C3C=CC=C2)=C3C=C1)=C4CN5CCC/4CC5.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (268.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6820 mL 13.4099 mL 26.8197 mL
5 mM 0.5364 mL 2.6820 mL 5.3639 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6820 mL 13.4099 mL 26.8197 mL 67.0493 mL
5 mM 0.5364 mL 2.6820 mL 5.3639 mL 13.4099 mL
10 mM 0.2682 mL 1.3410 mL 2.6820 mL 6.7049 mL
15 mM 0.1788 mL 0.8940 mL 1.7880 mL 4.4700 mL
20 mM 0.1341 mL 0.6705 mL 1.3410 mL 3.3525 mL
25 mM 0.1073 mL 0.5364 mL 1.0728 mL 2.6820 mL
30 mM 0.0894 mL 0.4470 mL 0.8940 mL 2.2350 mL
40 mM 0.0670 mL 0.3352 mL 0.6705 mL 1.6762 mL
50 mM 0.0536 mL 0.2682 mL 0.5364 mL 1.3410 mL
60 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1175 mL
80 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8381 mL
100 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6705 mL
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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:

YM-53601182959-33-7YM53601YM 53601Farnesyl TransferaseHCVFtaseHepatitis C virusSqualenesynthaseplasmacholesteroltriglyceridehepatomafarnesyl-diphosphatefarnesyltransferaseFDFT1hypocholesterolemicHMG-CoAreductasehypercholesterolemiaInhibitorinhibitorinhibit

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