cyclo(RLsKDK) TFA
Based on 2 publication(s) in Google Scholar
cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) (TFA) has potential applications in inflammatory diseases and cancer.
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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: 99.76%
- 分子式: C33H58F3N11O11
- 分子量:841.88
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保管条件:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 cyclo(RLsKDK) TFA
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生物活性
cyclo(RLsKDK) (TFA) promotes ADAM8 activation and CD23 shedding with IC50 values of 120 nM and 182 nM, respectively[2].
cyclo(RLsKDK) (TFA) (200 nM; 0-120 h) increases activity of pro-ADAM8[2].
cyclo(RLsKDK) (TFA) (200 nM and 500 nM; 12 h) promotes the growth of Panc1_ctrl and Panc1_A8 cells[2].
cyclo(RLsKDK) (TFA) (500 nM) causes ERK1/2 phosphorylation in Panc1_ctrl and Panc1_A8 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc1_A8 cells.
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Concentration:10, 100 and 1,000 nM.
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Incubation Time:6 h.
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Result:Reduced cell invasion with dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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性状 Solid
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分子量 841.88
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分子式 C33H58F3N11O11
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Color White to off-white
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別名
BK-1361 TFA
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配列
Cyclo(Arg-Leu-{d-Ser}-Lys-Asp-Lys)
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シーケンスの短縮
Cyclo(RL-{d-Ser}-KDK)
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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 and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Exp Neurol
Roles of Adam8 in Neuroinflammation in experimental ischemic Stroke: Insights from single-cell and ribosome-bound mRNA sequencing. [Abstract]2025 Jun:388:115207. PMID: 40064361 -
FASEB J
ADAM8 Destroys the Endothelial Barrier and Promotes Leukocyte Extravasation to Aggravate Hepatic Ischemia-Reperfusion Injury. [Abstract]2025 Nov 30;39(22):e71217. PMID: 41222986
溶剤 & 溶解度
H2O : 100 mg/mL (118.78 mM; Need ultrasonic)
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 and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yim V, et al. Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037. [Content Brief]
[2]. Schlomann U, et al. ADAM8 as a drug target in pancreatic cancer. Nat Commun. 2015 Jan 28;6:6175. [Content Brief]
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 and light, under nitrogen). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.1878 mL | 5.9391 mL | 11.8782 mL | 29.6954 mL |
| 5 mM | 0.2376 mL | 1.1878 mL | 2.3756 mL | 5.9391 mL | |
| 10 mM | 0.1188 mL | 0.5939 mL | 1.1878 mL | 2.9695 mL | |
| 15 mM | 0.0792 mL | 0.3959 mL | 0.7919 mL | 1.9797 mL | |
| 20 mM | 0.0594 mL | 0.2970 mL | 0.5939 mL | 1.4848 mL | |
| 25 mM | 0.0475 mL | 0.2376 mL | 0.4751 mL | 1.1878 mL | |
| 30 mM | 0.0396 mL | 0.1980 mL | 0.3959 mL | 0.9898 mL | |
| 40 mM | 0.0297 mL | 0.1485 mL | 0.2970 mL | 0.7424 mL | |
| 50 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5939 mL | |
| 60 mM | 0.0198 mL | 0.0990 mL | 0.1980 mL | 0.4949 mL | |
| 80 mM | 0.0148 mL | 0.0742 mL | 0.1485 mL | 0.3712 mL | |
| 100 mM | 0.0119 mL | 0.0594 mL | 0.1188 mL | 0.2970 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.