FPP29
Based on 1 Customer Validation
FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.20%
- 分子式: C145H228N56O32
- 分子量:3267.72
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
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VHL |
FPP29 (24 h) potently inhibits the viability of HCCLM3 cells, with an IC50 of 3.65 μM after 24 h of incubation[1].
FPP29 (4 μM; 24-48 h) significantly inhibits the migration ability of HCCLM3 cells[1].
FPP29 (2-8 μM; 24 h) induces dose-dependent apoptosis in HCCLM3 cells following 24 h of incubation at concentrations of 2 μM, 4 μM, and 8 μM[1].
FPP29 (2-8 μM; 6-48 h) downregulates the protein expression of FOXM1, cyclin B1 and CDC25B in HCCLM3 cells, and regulates epithelial-mesenchymal transition markers in a dose-dependent and time-dependent manner (upregulating E-cadherin and downregulating N-cadherin)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human hepatocellular carcinoma HCCLM3 cells
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Concentration:4 μM
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Incubation Time:24 h, 48 h
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Result:Significantly inhibited HCCLM3 cell migration at 24 h and 48 h compared to the control, with statistical significance.
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Cell Line:human hepatocellular carcinoma HCCLM3 cells
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Concentration:2-8 μM
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Incubation Time:24 h
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Result:Induced apoptosis in HCCLM3 cells in a dose-dependent manner; the number of yellow-green/orange apoptotic cells increased with increasing FPP29 concentrations.
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Cell Line:human hepatocellular carcinoma HCCLM3 cells
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Concentration:2-8 μM (24 h incubation); 4 μM (6 h, 12 h, 24 h, 48 h incubation)
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Incubation Time:24 h (dose-dependent); 6 h, 12 h, 24 h, 48 h (time-dependent)
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Result:Reduced protein expression of FOXM1, cyclin B1, and CDC25B in both dose-dependent (0-8 μM, 24 h) and time-dependent (4 μM, 0-48 h) manners.
Increased E-cadherin protein expression and decreased N-cadherin protein expression in a dose-dependent manner (0-8 μM, 24 h).
| Species | Dose | Route | Tmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 20 mg/kg | i.v. | 0.25 h | 1.04 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (6-week-old male, subcutaneous xenograft model)[1]
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Dosage:7.5 mg/kg; 15 mg/kg
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Administration:intra-tumoral injection
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Result:Inhibited tumor growth by 55%.
Inhibited tumor growth by 75%.
Reduced tumor weight in a dose-dependent manner.
Downregulated FOXM1 protein levels in tumor tissues in a dose-dependent manner.
Increased tumor necrosis and inflammatory cell infiltration.
Reduced Ki-67-positive proliferating cells.
Significantly increased TUNEL-positive apoptotic cells.
Caused no significant changes in mouse body weight, major organ histopathology, liver function tests, or blood routine indices.
化学情報
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性状 Solid
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分子量 3267.72
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分子式 C145H228N56O32
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Color White to off-white
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配列
Ala-Trp-Trp-Asn-Thr-Glu-Trp-Gly-Ser-Ala-Leu-Ala-Pro-Tyr-Ile-Pro-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg
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シーケンスの短縮
AWWNTEWGSALAPYIPRRRRRRRRR
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 25 mg/mL (7.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 0.3060 mL | 1.5301 mL | 3.0602 mL | 7.6506 mL |
| 5 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5301 mL |