22-SLF
Based on 1 Customer Validation
22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway.
(Pink: FKBP12 ligand (HY-114872); Blue: VHL ligand (HY-163826); Black: linker (HY-163821)).
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 : 95.72%
- CAS 番号: 3079209-82-5
- 分子式: C60H76ClN5O13S
- 分子量:1142.79
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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FKBP12 |
体外実験
22-SLF (2-5 μM, 24 h) has no effect on FKBP12-EGFP levels in the SFFV promoter system but induces a mild yet significant reduction of FKBP12 (~30 %) in the hPGK promoter system[1].
22-SLF (0.025-15 μM, 2-24 h) recruits FBXO22 to FKBP12, resulting in the proteasomal degradation of FKBP12 in an FBXO22-dependent manner, with a Dmax of ~ 89%[1].
22-SLF (2 μM, 2 h) effectively drives the formation of a ternary complex involving 22-SLF, FBXO22 and FKBP12 by engaging C227/228 in FBXO22, with approximately 20% engagement of FBXO22 C228 at 2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HEK293T and A549 cells
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Concentration:0.025, 0.1, 0.25, 0.5, 0.75, 1, 2, 5, 7.5, 10 and 15 μM for HEK293T cells, 2, 10, and 50 μM for A549 cells
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Incubation Time:2, 4, and 8 h for HEK293T cells, 2, and 24 h for A549 cells
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Result:Induced FKBP12 degradation in a FBXO22-dependent manner.
Its FKBP12 degradation was blocked by the proteasome inhibitor MG132 (HY-13259), the neddylation inhibitor MLN4924 (HY-70062) and the FKBP12 ligand SLF (HY-114872).
Induced rapid and nearly complete degradation of FKBP12 within 2 hours.
Degraded FKBP12 in a dose- and time-dependent manner.
Induced FKBP12 degradation in A549 wildtype, but not FBXO22 knockout cells at 2 μM. Competed with 22-biotin-enriched FBXO22 in a dose-dependent manner, thereby further confirming its direct binding to FBXO22.
Its FKBP12 degradation was partially blocked by single mutation of C227 or C228, and completely abolished by the double mutant C227A/C228A.
Its FKBP12 degradation was supported by mouse FBXO22.
Its FKBP12 degradation was abolished by mutation of both C226 and C227 in mouse FBXO22.
The formation of the 22-SLF/FKBP12/FBXO22 ternary complex was confirmed by co-immunoprecipitation.
化学情報
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CAS 番号 3079209-82-5
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性状 Solid
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分子量 1142.79
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分子式 C60H76ClN5O13S
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Color Light yellow to brown
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SMILES
CCC(C)(C(C(N1CCCC[C@H]1C(O[C@@H](C2=CC(OCC(NCCCOCCOCCOCCCN(C(C3=NC4=C(S3)C=CC=C4)C(NCC5=CC=CC=C5)=O)C(CCl)=O)=O)=CC=C2)CCC6=CC=C(C(OC)=C6)OC)=O)=O)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (43.75 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. 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. 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 (272 KB)
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SDS (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. 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 | 0.8751 mL | 4.3753 mL | 8.7505 mL | 21.8763 mL |
| 5 mM | 0.1750 mL | 0.8751 mL | 1.7501 mL | 4.3753 mL | |
| 10 mM | 0.0875 mL | 0.4375 mL | 0.8751 mL | 2.1876 mL | |
| 15 mM | 0.0583 mL | 0.2917 mL | 0.5834 mL | 1.4584 mL | |
| 20 mM | 0.0438 mL | 0.2188 mL | 0.4375 mL | 1.0938 mL | |
| 25 mM | 0.0350 mL | 0.1750 mL | 0.3500 mL | 0.8751 mL | |
| 30 mM | 0.0292 mL | 0.1458 mL | 0.2917 mL | 0.7292 mL | |
| 40 mM | 0.0219 mL | 0.1094 mL | 0.2188 mL | 0.5469 mL |
22-SLF 関連分類
HY-163807 関連分類
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