aTAG 4531

aTAG 4531 binds to the purified CRBN/DDB1 complex with a K_D value of 385 nM^[1].
aTAG 4531 potently inhibits the enzymatic activity of purified human MTH1 aTAG, with a K_i value of 1.8 nM^[1].
The degradation of SMART-CAR and MTH1 induced by aTAG 4531 (10 nM; 4 h) in Jurkat T cells is reversible, and protein levels recover to basal levels within 72 h after degradation 剂 elution^[1].
aTAG 4531 (4 h) potently degrades SMART-CAR-HiBiT in Jurkat T cells, with a DC₅₀ of 0.28 nM and an E_max of 11% after 4 h of treatment^[1].
Treatment of Jurkat T cells with aTAG 4531 (1-10000 nM; 6 h) induces concentration-dependent degradation of SMART-CAR-HA and MTH1^[1].
The degradation of SMART-CAR and MTH1 induced by aTAG 4531 (100 nM; 6 h) in Jurkat T cells is mediated via the CRBN-dependent proteasomal pathway, which is confirmed by rescue experiments using pathway-specific inhibitors and competitors^[1].
aTAG 4531 (0.1-1000 nM) regulates CAR-T-mediated target cell killing in a concentration-dependent manner, with the peak inhibitory effect on Raji cell killing and the maximum degradation of SMART-CAR both occurring at 10 nM^[1].
aTAG 4531 (1-10000 nM) regulates CAR-T-mediated IL-2 cytokine release in a concentration-dependent manner, with the inhibitory effect peaking at 1 and 10 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.