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FKBP(FK506结合蛋白)

FKBP (FK506-binding protein) is one of two major immunophilins and most of FKBP family members bind FK506 and show peptidylprolyl cis/trans isomerase (PPIase) activity. Small size FKBP family members contain only FK506-binding domain, while FKBPs with large molecular weights possess extra domains such as tetratricopeptide repeat domains, calmodulin binding and transmembrane motifs. FKBPs are involved in several biochemical processes including protein folding, receptor signaling, protein trafficking and transcription. FKBP family proteins play important functional roles in the T-cell activation, when complexed with their ligands.

FK506-binding proteins 1a and 1b (FKBP1a/1b) are immunophilin proteins that bind the immunosuppressant agent FK506 and AY 22989. FKBP12 is a ubiquitous abundant protein that acts as a receptor for FK506, binds tightly to intracellular calcium release channels and to the transforming growth factor β (TGF-β) type I receptor.

Products for  FKBP

  1. Cat.No. 产品名称 Information
  2. GC66370 Zapalog Zapalog 是一种光可裂解的小分子异二聚体,可用于重复启动和瞬间终止两种靶蛋白之间的物理相互作用。 Zapalog 对用 FKBP 和 DHFR 结构域标记的任何两种蛋白质进行二聚化,直到暴露于光下导致其光解。
  3. GC62186 KB02-SLF KB02-SLF 是一种基于 PROTAC 的核 FKBP12 降解剂 (molecular glue)。KB02-SLF 通过共价修饰 DCAF16 (E3 ligase) 促进 FKBP12 降解,并可以提高生物系统中蛋白质降解的持久性。KB02-SLF 由 SLF 与泛素 E3 连接酶配体 (KB02) 通过 linker 连接而成。
  4. GC61745 AP1867-2-(carboxymethoxy) AP1867-2-(carboxymethoxy)是一种基于AP1867(一种合成的FKBP12F36V配体)的配体,可通过linker与CRBN配体结合从而形成dTAG分子。
  5. GC61461 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。
  6. GC48027 Rapamycin-d3 An internal standard for the quantification of rapamycin
  7. GC39503 PROTAC FKBP Degrader-3 PROTAC FKBP Degrader-3 是一种包含 FKBP 配体结合基团,linker 和 VHL 结合基团的 PROTAC。PROTAC FKBP Degrader-3 是一种有效的 FKBP 降解剂。
  8. GC38060 Shield-1 Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP). Shield-1 reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 stabilizes the entire fusion protein.
  9. GC44899 SLF A synthetic FK-506 Binding Protein (FKBP) ligand
  10. GC34172 AP1867 AP1867是合成的FKBP12F36V的配体。
  11. GC34093 SAFit2 An FKBP51 inhibitor
  12. GC33699 SAFit1 SAFit1是一种特异性的FK506结合蛋白51(FKBP51)抑制剂,Ki为4±0.3nM。
  13. GC33200 Target Protein-binding moiety 13 Target Protein-binding moiety 13 (PROTAC FKBP12-binding moiety 1) 是 FKBP (SLF) 的合成配体。目标蛋白结合部分 13(PROTAC FKBP12 结合部分 1)可用于 PROTAC 的合成。
  14. GC15586 AP1903 A CID for FKBPF36V fusion proteins
  15. GC17995 Tacrolimus monohydrate 他克莫司一水合物 (FK506 monohydrate) 是一种大环内酯,与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶,从而抑制 T 淋巴细胞信号转导和 IL-2 转录。
  16. GC14498 AP20187 A CID for FKBP fusion proteins
  17. GC16233 Tacrolimus (FK506) A potent immunosuppressant/inhibitor of T cell activation
  18. GC13215 Ascomycin(FK 520) A potent macrolide immunosuppressant
  19. GC13601 Everolimus (RAD001) A rapamycin derivative
  20. GC15031 Rapamycin (Sirolimus)

    An allosteric inhibitor of mTORC1

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