2. PROTAC Autophagy Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage
  3. PROTACs FKBP
  4. 22-SLF

22-SLF 是一种 PROTAC 降解剂，可降解 FK506 结合蛋白 12 (FKBP12)，其 DC50 为 0.5 µM。22-SLF 通过与 FBXO22 上的 C227 和 C228 相互作用，以诱导 FKBP12 与 FBXO22 之间形成三元复合物，并以 FBXO22 依赖的方式降解 FKBP12。22-SLF 可作为研究 FBXO22 降解作用机制的工具，用于基础癌症研究。 (粉色: FKBP12 配体 (HY-114872); 黑色: 连接子 (HY-163821); 蓝色: E3 连接酶 FBXO22 配体 (HY-163826))。

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22-SLF

22-SLF Chemical Structure

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1 mg ￥2950
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22-SLF 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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); Black: Linker (HY-163821); Blue: FBXO22 ligand (HY-163826))[1].

体外研究
(In Vitro)

22-SLF (2-5 μM，24 小时) 对 SFFV 启动子系统中的 FKBP12-EGFP 水平无影响，但在 hPGK 启动子系统中可诱导 FKBP12 轻微但显著的降低 (约 30 %)[1]。
22-SLF (0.025-15 μM，2-24 小时) 将 FBXO22 募集至 FKBP12，从而以 FBXO22 依赖的方式导致 FKBP12 的蛋白酶体降解，最大降解率 (Dmax) 约为 89 %[1]。
22-SLF (2 μM，2 小时) 通过结合 FBXO22 上的 C227/228 有效驱动了由 22-SLF、FBXO22 和 FKBP12 形成三元复合物，且在 2 μM 浓度下对 FBXO22 C228 的占据率约为 20 %[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

22-SLF 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293T and A549 cells
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
Incubation Time: 2, 4, and 8 h for HEK293T cells, 2, and 24 h for A549 cells
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.
分子量

1142.79

Formula

C60H76ClN5O13S
性状

固体

颜色

Light yellow to brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

22-SLF 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

22-SLFPROTACsFKBPFK506-binding proteinHEK293TA549MDA-MB-231H2228PC3PROTACFKBP12FBXO22Inhibitorinhibitorinhibit

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