fkbp12

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

FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader.

FKBP12 PROTAC RC32 contains conjugation of Rapamycin and a ligand for an E3 ubiquitin ligase.FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology.

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].

SLF-amido-C2-COOH is a synthetic ligand for FKBP (SLF), and can be used in the synthesis of PROTACs.

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

AUTAC2, an autophagy-mediated degrader (AUTAC) targeting FKBP12, comprises an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. The SLF component binds non-covalently to FKBP12 [1].

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, known as a molecular glue. It facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. Moreover, KB02-SLF enhances the longevity of protein degradation in biological systems. The compound SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, resulting in the formation of KB02-SLF[1].

dTAGV-1 TFA is a highly effective and specific compound that targets mutant FKBP12 F36V fusion proteins for degradation. It possesses potent activity in inducing the degradation of the FKBP12 F36V -Nluc protein in living organisms.

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].

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].

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.

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

AUTAC1 is a MetAP2-targeted autophagy-mediated degrader (AUTAC) with potential anticancer activity that degrades MetAP2 and FKBP12 proteins and can be used to synthesize PROTAC.

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].

SLF is a synthetic ligand for FK506-binding protein (FKBP)( with an affinity of 3.1 μM for FKBP51 and an IC50 of 0.22 μM for FKBP12). SLF can be used in the synthesis of PROTAC.

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].