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  • SLF TFA
SLF TFA的可视化放大

SLF TFA

SLFTFA是FK506结合蛋白(FKBP)的合成配体,对FKBP51的亲和力为3.1μM,对FKBP12的IC50为2.6μM,可用于合成PROTAC分子。

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¥812-10037
价格
650-8030
SLF TFA的二维码

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  • 库存: 现货
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  • 货号: ajcx31820
  • CAS: 2378802-47-0
  • 别名:
  • 分子式: C32H41F3N2O8
  • 分子量: 638.67
  • 纯度: >98%
  • 溶解度: DMSO: 200 mg/mL (313.15 mM)
  • 储存: 4°C, away from moisture and light
  • 库存: 现货

Background

SLF TFA is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. SLF TFA can be used in the synthesis of PROTAC[1][2][3].


Three scout fragments-KB02, KB03, and KB05 are fused, which cover two different electrophile groups (chloroacetamide and acrylamide) and display broad cysteine reactivity in the human proteome-to the SLF ligand that binds tightly and selectively to FKBP12, a cytosolic prolyl isomerase that has been frequently used to study ligand-induced protein degradation[3].


[1]. Kolos JM, et al. FKBP Ligands-Where We Are and Where to Go? Front Pharmacol. 2018 Dec 5;9:1425. [2]. Wu X, et al. Creating diverse target-binding surfaces on FKBP12: synthesis and evaluation of a rapamycin analogue library. ACS Comb Sci. 2011 Sep 12;13(5):486-95. [3]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.

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