dtagv 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.

dTAGV-1 hydrochloride is a PROTAC-based bifunctional degrader that utilizes the VHL E3 ligase recruitment mechanism to efficiently and selectively induce the in vivo and in vitro degradation of FKBP12F36V-tagged proteins, while having no effect on wild-type FKBP12 protein.

dTAGV-1 TFA is a highly efficient, highly selective VHL-dependent PROTAC-mediated protein degrader that specifically targets and degrades mutant FKBP12 fusion proteins. dTAGV-1 TFA efficiently induces the degradation of FKBP12 fusion proteins at both the cellular and in vivo levels.

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].

(R,S,S)-VH032-Me-N-Boc-7-aminoheptanoic acid is a conjugate of an E3 ligase ligand and a linker (E3LigaseLigand-Linker Conjugates), composed of N-Boc-7-aminoheptanoic acid and the corresponding linker. It is utilized in the synthesis of dTAGV-1-NEG.

(R,S,S)-VH032-Me is a ligand for the E3 ubiquitin ligase. It can connect with a target protein ligand via a linker to form dTAGV-1-NEG. This PROTAC can induce the ubiquitination and subsequent degradation of oncogenic proteins.

(R,S,S)-VH032-Me TFA is an E3 ligase ligand utilized in the synthesis of [dTAGV-1 hydrochloride].

(R,S,S)-VH032-Me-N-Boc-7-aminoheptanoic acid TFA is a conjugate that consists of an E3 ubiquitin ligase ligand and a linker. This compound is useful for synthesizing dTAGV-1 hydrochloride.