ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].

ZXH-4-130 TFA at a concentration of 100 nM and pre-treatment for 2 hours significantly inhibited the cytotoxic effects of pomalidomide (1 μM) when cells were subsequently treated for 96 hours, displaying a statistically significant protective effect [1]. Additionally, a pre-treatment with ZXH-4-130 TFA at 50 nM was able to rescue the degradation of GSPT1 in MM1.S cells induced by CC-885 [1]. Furthermore, ZXH-4-130 TFA (100 nM; pre-treated for 2 hours, followed by treatment with THAL-SNS-032 for 6 hours) nearly completely induced the degradation of CRBN, whereas THAL-SNS-032 only partially inhibited CDK9 activity [1].