SN-28049 SN is a DNA intercalating drug that binds selectively to GC-rich DNA and shows curative activity against the Colon 38 adenocarcinoma in mice. SN 28049 has a complex action that may involve poisoning of topo IIalpha, suppression of topo I and inhibition of gene transcription from promoters with SP-1 sites. These actions may contribute to the promising experimental solid tumour anticancer activity of SN 28049.
DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.
Senexin A hydrochloride是一种专门针对CDK8 19(IC50为280 nM,针对CDK8)的抑制剂,同时针对p21转录活性下游展现抑制作用。该化合物特异性抑制由p21诱导的转录活性,而不干扰p21的其他生物功能。此外,Senexin A hydrochloride能够抑制CMV-GFP引发的活性及p21激活的、具NF-κB依赖性启动子的表达。
20-Deoxyingenol 3-angelate and ingenol 20-acetate 3-angelate are known as promoters of tumors of mouse skin. 20-Deoxyingenol 3-angelate can induce significant platelet aggregation accompanied by induction of phosphorylation of PKC substrates in platelets,