cyclo(RLsKDK)
Based on 2 publication(s) in Google Scholar
cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer.
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- 純度: 98.85%
- CAS 番号: 1975145-82-4
- 分子式: C31H57N11O9
- 分子量:727.85
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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)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 cyclo(RLsKDK)
More
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
182 nM
Compound: 1
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Inhibition of recombinant ADAM8 (unknown origin) expressed in African green monkey COS7 cells co-expressing CD23 assessed as inhibition of CD23 shedding after 24 hrs by ELISA
Inhibition of recombinant ADAM8 (unknown origin) expressed in African green monkey COS7 cells co-expressing CD23 assessed as inhibition of CD23 shedding after 24 hrs by ELISA
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[PMID: 27407033] |
cyclo(RLsKDK) promotes ADAM8 activation and CD23 shedding with IC50 values of 120 nM and 182 nM, respectively[2].
cyclo(RLsKDK) (200 nM; 0-120 h) increases activity of pro-ADAM8[2].
cyclo(RLsKDK) (200 nM and 500 nM; 12 h) promotes the growth of Panc1_ctrl and Panc1_A8 cells[2].
cyclo(RLsKDK) (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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CAS 番号 1975145-82-4
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性状 Solid
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分子量 727.85
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分子式 C31H57N11O9
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Color White to off-white
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別名
BK-1361
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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
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
DMSO : 3.33 mg/mL (4.58 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: ≥ 100 mg/mL (137.39 mM); Clear solution
純度とドキュメンテーション
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データシート (277 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). 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 | 1.3739 mL | 6.8695 mL | 13.7391 mL | 34.3477 mL |
cyclo(RLsKDK) 関連分類
HY-P1676 関連分類
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