Cereblon modulator 1 是一种 GSPT1 选择性cereblon (CRBN)E3 连接酶调节剂，以分子胶的方式作用。它通过 CRL4CRBN选择性靶向 GSPT1 进行泛素化和蛋白酶体降解。

Cereblon modulator 1 is a cereblon (CRBN) E3 ligase modulator. It specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex.

Cereblon modulator 1 (compound F) that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 μΜ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold [1].

1860875-51-9

C22H18ClF2N3O4

461.85

Cereblon modulator 1

DMSO:240 mg/mL (519.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years