428497-71-6

428497-71-6 structure

Name: DT204
Chemical Name: (4-Bromo-2-{(Z)-[3-(4-chlorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}phenoxy)acetic acid
CAS Number: 428497-71-6
Molecular Formula: C₁₉H₁₃BrClNO₅S
Molecular Weight: 482.732
Create Date: 2020-01-11 15:58:00
Modify Date: 2023-01-11 18:58:49
DT204 (DT-204) is a novel SCFSkp2 inhibitor that reduces Skp2 binding to Cullin-1 and Commd1, synergistically enhances BTZ-induced apoptosis; stablizes and increases p27 levels, does not increase the level of p53, demonstrates potential synergy with CI values of 0.7, 0.8 and 0.7 for RPMI8226, U266 and MM1.S respectively combined with 1 nM BTZ, co-treatment induces apoptosis in cells resistant to the proteasome inhibitors BTZ, carfilzomib or ixazomib; overcomes drug resistance and reduces the in vivo growth of myeloma tumors in murine models.

Name	(4-Bromo-2-{(Z)-[3-(4-chlorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}phenoxy)acetic acid
Synonyms	(4-Bromo-2-{(Z)-[3-(4-chlorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}phenoxy)acetic acid Acetic acid, 2-[4-bromo-2-[(Z)-[3-[(4-chlorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]-

Description	DT204 (DT-204) is a novel SCFSkp2 inhibitor that reduces Skp2 binding to Cullin-1 and Commd1, synergistically enhances BTZ-induced apoptosis; stablizes and increases p27 levels, does not increase the level of p53, demonstrates potential synergy with CI values of 0.7, 0.8 and 0.7 for RPMI8226, U266 and MM1.S respectively combined with 1 nM BTZ, co-treatment induces apoptosis in cells resistant to the proteasome inhibitors BTZ, carfilzomib or ixazomib; overcomes drug resistance and reduces the in vivo growth of myeloma tumors in murine models.
References	References 1. Malek E, et al. Leukemia. 2017 Mar;31(3):645-653. View Related Products by Target E3 Ubiquitin Ligase