PIISVYWK
PIISVYWK is an orally active PPARγ Inhibitor, heme oxygenase-1 Activator, and Nrf2 Activator. PIISVYWK mediates activity via the HO-1/Nrf2 pathway, ameliorates oxidative stress, reduces inflammation, and mediates anti-obesity activity. PIISVYWK can be used for the research of obesity.
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- CAS No.: 2016043-80-2
- 화학식: C51H76N10O11
- 분자량:1005.21
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
PIISVYWK (10-100 μM; 48 h) is non-cytotoxic to BMMSCs[1].
PIISVYWK (10-100 μM; 7 days) inhibits adipocyte differentiation in BMMSCs by suppressing adipogenic transcription factors and lipogenic enzymes, and enhancing lipolysis, with up to 40.97% inhibition of lipid accumulation at 100 μM[1].
PIISVYWK (10-100 μM; 2 days for Nrf2, 3 days for HO-1) activates the HO-1/Nrf2 signaling pathway in BMMSCs, increasing HO-1 cytoplasmic expression and Nrf2 nuclear expression at 100 μM[1].
PIISVYWK (10-100 μM; 7 days) reduces oxidative stress in BMMSCs during adipogenesis by decreasing ROS generation and increasing antioxidant enzyme activities, with significant effects at 100 μM[1].
PIISVYWK (10-100 μM; 7 days) reduces inflammation in BMMSCs by suppressing pro-inflammatory cytokine production and modulating the MAPK pathway, with significant effects at 100 μM[1].
PIISVYWK (100 μM; 7 days, pre-treated with 5 μM ZnPP for 1 h) exerts anti-adipogenic effects in BMMSCs that are mediated by HO-1, as pre-treatment with ZnPP reverses its inhibitory effects on adipocyte differentiation, transcription factor expression, and lipolysis[1].
PIISVYWK (100 μM; 7 days, pre-treated with 5 μM ZnPP for 1 h) exerts oxidative stress-reducing and anti-inflammatory effects in BMMSCs that are mediated by HO-1, as pre-treatment with ZnPP reverses these effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:bone marrow-derived mesenchymal stem cells (BMMSCs)
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Concentration:10-100 μM
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Incubation Time:7 days
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Result:Inhibited lipid accumulation in BMMSCs in a dose-dependent manner, with up to 40.97% inhibition at 100 μM; suppressed the expression of adipogenic transcription factors PPARγ, SREBP-1, and C/EBPα, alongside adipocyte protein 2 (aP2); increased free glycerol levels in the culture medium; inhibited lipogenic enzymes FAS and LPL; upregulated lipolysis-related p-HSL.
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Cell Line:bone marrow-derived mesenchymal stem cells (BMMSCs)
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Concentration:10-100 μM
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Incubation Time:2 days (Nrf2); 3 days (HO-1)
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Result:Elevated HO-1 expression in the cytoplasm of BMMSCs, with significance at 100 μM (P < 0.05); increased Nrf2 expression in the cell nucleus at high concentrations (P < 0.05); induced Nrf2 nuclear translocation as observed via immunostaining.
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Cell Line:bone marrow-derived mesenchymal stem cells (BMMSCs)
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Concentration:10-100 μM
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Incubation Time:7 days
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Result:Significantly reduced the production of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) in BMMSCs compared to the control group, with significant effects at higher concentrations (P < 0.01 for 100 μM; P < 0.05 for lower concentrations); modulated the MAPK pathway, with changes in p-ERK, p-P38, and p-JNK expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 3 weeks old at acclimation start, 6 weeks old at study initiation, HFD-induced obesity model)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 15 weeks
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Result:Reduced weight gain to 17.29 g, decreased fat percentage to 45.26%, reduced adipose tissue weight, suppressed adipogenic transcription factors (PPARγ, SREBP-1, C/EBPα) and lipogenic enzymes (LPL, FAS, aP2) in subcutaneous adipose tissue, increased p-HSL and p-AMPK expression in subcutaneous adipose tissue, reduced fasting blood glucose to 146.00 mg/dL, reduced total cholesterol (4.98 mmol/L), LDL (1.00 mmol/L), and triglycerides (1.43 mmol/L), increased HDL (1.49 mmol/L) and free glycerol levels, reduced serum pro-inflammatory cytokines (IL-6: 34.33 pg/mL, IL-1β: 17.00 pg/mL, TNFα: 22.67 pg/mL), increased antioxidant enzyme activities (CAT: 35.4 U/mL, SOD: 165.2 U/mL, GPx: 82.7 U/mL), and activated HO-1 and Nrf2 in subcutaneous adipose tissue at 10 mg/kg; moderately reduced weight gain, fasting blood glucose, LDL, pro-inflammatory cytokines, and increased antioxidant enzyme activities at 1 mg/kg.
Chemical Information
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CAS No. 2016043-80-2
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분자량 1005.21
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화학식 C51H76N10O11
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Sequence
Pro-Ile-Ile-Ser-Val-Tyr-Trp-Lys
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Sequence Shortening
PIISVYWK
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PIISVYWK Related Classifications
Cat. No.: HY-P11589
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- PIISVYWK
- 2016043-80-2
- PPAR
- Reactive Oxygen Species (ROS)
- Keap1-Nrf2
- nuclear factor erythroid 2-related factor 2
- CCAAT/enhancer-binding protein alpha
- heme oxygenase-1
- bone marrow-derived mesenchymal stem cell
- AMP-activated protein kinase
- peroxisome proliferator-activated receptor gamma
- mitogen-activated protein kinase pathway
- hormone-sensitive lipase
- sterol regulatory element-binding protein 1
- high-fat diet-induced obese mice
- Inhibitor
- inhibitor
- inhibit