fkbp

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.

PROTAC FKBP Degrader-3 is a bifunctional PROTAC molecule composed of an FKBP ligand-binding group, a rationally designed linker, and a VHL E3 ligase-binding moiety, and functions as a potent FKBP degrader, enabling selective protein degradation studies and validation of FKBP as a therapeutic target.

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].

SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.

SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.

FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.

FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

SLF TFA, a synthetic ligand for FK506-binding protein (FKBP), exhibits affinity toward FKBP51 with a value of 3.1 μM and demonstrates an IC50 of 2.6 μM for FKBP12. This compound is utilized in the synthesis of PROTAC [1] [2] [3].

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, also known as a molecular glue, that facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, thus forming KB02-SLF[1] and enhancing the longevity of protein degradation in biological systems.

AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].

10-SLF is a PROTAC FKBP12 degrader. It facilitates the formation of a ternary complex between FKBP12 and FBXW7-R465C, leading to the proteasomal degradation of FKBP12 in a FBXW7-R465C-dependent manner. 10-SLF selectively reduces FKBP12 levels in cells that express FBXW7-R465C.

Negative control for dTAGV-1.

dTAGV-1-NEG TFA, a diastereomer, serves as the heterobifunctional negative control for dTAGV-1. It acts specifically as an FKBP12 F36V-selective degrader [1].

dTAG-47, a heterobifunctional molecule, specifically targets the mutant FKBP12 (FKBP12 F36V), which functions as a degradation tag (dTAG) when fused to a protein of interest. This compound is utilized in the study of basal-like breast cancers (BBC) [1].

FKBP12 Ligand-Linker Conjugate 2 is a conjugate composed of an FKBP12 target protein ligand and a linker. It is utilized in the synthesis of FKBP12PROTACFM4.

FKBP12PROTACFM4 is a PROTAC degrader targeting MTH1, with a degradation efficiency (Dmax) greater than 90%.

YT117R is a PROTAC that targets degradation of FKBP12 and BRD4.

22-SLF is a PROTAC degrader that operates by FBXO22-dependent degradation of FK506 Binding Protein 12 (FKBP12) with a DC50 of 0.5 µM. Additionally, 22-SLF can degrade other endogenous proteins, such as BRD4 and the EML4-ALK fusion protein (EML4-ALK fusion protein).

Thalidomide-O-C6-NH2 hydrochloride (4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride) is a synthesized E3 ligase ligand-linker conjugate.

AUTAC2 is an FKBP12-targeting autophagy-mediated degrader that incorporates both an FBnG (p-fluorobenzyl guanine) moiety and an SLF moiety, with SLF binding noncovalently to FKBP12, AUTAC2 is utilized in targeted protein degradation research to explore selective autophagic clearance, intracellular quality control mechanisms, and novel degrader design strategies.

TSPO ligand-3, functioning as an AUTAC2 ligand, incorporates both a p-fluorobenzylguanine (FBnG) and a synthetic ligand of FKBP (SLF) moiety, leading to the substantial inhibition of FKBP12 in HeLa cells [1].