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Organic compounds that consists entirely of hydrogen and carbon elements usually organized in a chain; some may have a cyclic structure. Includes hydrocarbons that have additional functional groups such as aromatic rings.
I-BET-762 (CAS 1260907-17-2) is a small-molecule inhibitor targeting the BET (bromodomain and extra-terminal) family of proteins It acts by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains thereby displacing acetylated histones with an IC50 ranging from 32 5 to 42 5 nM and a dissociation constant (Kd) between 50 5 and 61 3 nM I-BET-762 displays high selectivity exhibiting no interaction with non-BET bromodomain-containing proteins In cellular studies it downregulates LPS-induced gene expression resulting in reduced production of pro-inflammatory cytokines and chemokines In vivo models demonstrate its potential to attenuate features of established inflammatory disease supporting its utility in epigenetic and inflammation-related research
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VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays shows inhibition of H2AX phosphorylation minimal activity against PIKKs ATM DNA-PK mTOR and PI3K
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NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) hydrochloride is a topoisomerase I inhibitor that demonstrates good ADC (Antibody-Drug Conjugate) activity both in vivo and in vitro, and can be delivered to cells through conjugated antibody targeting.
Functions as a topoisomerase I inhibitor.
Designed for targeted delivery to cells via conjugated antibodies.
Shows effective ADC activity both in vivo and in vitro.
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