aTAG 2139

aTAG 2139 potently inhibits purified human MTH1 with a K_i value of 2.1 nM^[1].
aTAG 2139 (1.5 h) binds to the purified CRBN/DDB1 complex with a K_d value of 1502 nM^[1].
aTAG 2139 (incubated with proteins for 1 h, followed by incubation with magnetic beads for 1 h) induces the formation of a dose-dependent ternary complex between purified CRBN/DDB1 and MTH1-MBP proteins^[1].
aTAG 2139 (4 h) potently and selectively degrades MTH1 aTAG in Jurkat T cells expressing SMART‑CAR, with a DC₅₀ of 1.1 nM and a maximum degradation rate of 18%^[1].
aTAG 2139 (250 nM; 20 h, followed by 8 h washout) reversibly attenuates the cytotoxic effect of CAR-T cells against CD19⁺ Raji target cells in a co-culture system, and the activity of CAR-T cells is restored after elution of the degrader^[1].
aTAG 2139 dose-dependently inhibits IL-2 cytokine release from SMART-CAR-expressing Jurkat T cells co-cultured with CD19⁺ Raji target cells^[1].

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