dTAGV-1，5MG，SML4123-5MG，Sigma

Biochem/physiol Actions

Degradation tag (dTAG) system heterobifunctional degrader of FKBP12(F36V) fusions by bridging them with VHL E3 ligase complex for ubiquitination.


dTAGV-1 is a degradation tag (dTAG) system heterobifunctional degrader composed of an E3 ubiquitin ligase von Hippel-Lindau (VHL)-binding ligand and an FKBP12(F36V) mutant-specific ligand AP1867 void of affinity for endogenous (wild-type) FKBP12, allowing selective degradation of target proteins of interest when expressed as an FKBP12(F36V) in-frame fusion by bridging them with VHL for ubiquitination. dTAGV-1 selectively induces cellular degradation of FKBP12F36V fusions in cultures (50-500 nM for 4-24 hrs) and in mice in vivo (35 mg/kg/day i.p.) with superior half-life and exposure than dTAG-13 (T1/2 = 4.43 vs. 2.41 h, AUC = 18517 vs. 6140 h*ng post 10 mg/kg i.p.).