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- FKBP (FK506-binding protein)
- SLF TFA
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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包装价格促销价数量
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5mg￥812.00650.00- +
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10mg￥1525.001220.00- +
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50mg￥6037.004830.00- +
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100mg￥10037.008030.00- +
- 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.
