CC-3060 is a cell-permeable pomalidomide analog that acts as a potent, efficacious and dose-dependent promoter of CRL4CRBN-mediated ZBTB16 (Promyelocytic Leukemia Zinc Finger protein or PLZF) proteasomal degradation (DC50 = 0.47 nM and a ymin of 28 in HT-1080 ZBTB16-ePL cells). CC-3060 is shown to directly interact with the C2H2 ZnF1 domain, form a ternary complex with CRBN/ZBTB16 and stimulate ZBTB16-RARα robust degradation (Ymin of 20 in RAR?-ZBTB16-ePL cells). Also facilitates degradation of CRBN neosubstrates IKZF1, ZFP91, and ZNF276 with no effect on GSPT1 and CSNK1A1.
cell-permeable pomalidomide analog that acts as a potent, efficacious and dose-dependent promoter of CRL4CRBN-mediated ZBTB16 proteasomal degradation
Drug metabolism and disposition: the biological fate of chemicals, 37(6), 1164-1171 (2009-03-03)
Saxagliptin is a potent, selective, reversible dipeptidyl peptidase 4 (DPP4) inhibitor specifically designed for extended inhibition of the DPP4 enzyme and is currently under development for the treatment of type-2 diabetes. The pharmacokinetics of saxagliptin were evaluated in rats, dogs
ACS chemical biology, 15(12), 3149-3158 (2020-11-19)
There is a growing interest in using targeted protein degradation as a therapeutic modality in view of its potential to expand the druggable proteome. One avenue to using this modality is via molecular glue based Cereblon E3 Ligase Modulating Drug
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