fkbp-12

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

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.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

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.

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.

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.

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

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

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

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].

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.

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%.

FKBP12 ligand-2 (compound d) is a high-affinity ligand that targets FKBP12. This compound is utilized to selectively enhance the binding of heterobifunctional molecules to BRD4, facilitating the intracellular accumulation of drugs through the "CellTrap" effect. It forms a ternary complex of FKBP12-ligand-BRD4, which inhibits BRD4, suppresses the expression of BRD4 target genes such as MYC, and induces tumor cell death. FKBP12 ligand-2 is applicable in selective cancer research based on the differential levels of presenter proteins within cells.

BRD4/FKBP12 degrader-1 (a1d) is an anticancer agent that functions as a BRD4/FKBP12 degrader.

FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. It is utilized to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching drugs intracellularly through the "CellTrap" effect to form an FKBP12-ligand-BRD4 ternary complex. This complex inhibits BRD4, reducing the expression of BRD4 target genes such as MYC, leading to tumor cell death. FKBP12 ligand-3 can be applied in selective cancer research based on differences in intracellular presenter protein levels.

BRD4/FKBP12 degrader-2 (a1d) is a BRD4/FKBP12 degrader with anticancer activity.

EcDHFR/FKBP12 F36V binder-1 (compound 1) is a bifunctional molecule that integrates the domains of Escherichia coli dihydrofolate reductase (EcDHFR) and FKBP12F36V.

FKBP12-IN-Q2 is an inhibitor of FKBP12.

ElteN378 is a highly potent synthetic inhibitor of FKBP12 with Ki of 0.5 nM, a low atomic weight ligand with affinity comparable to that of the macrolide Rapamycin.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.