epigenetic regulation

D18 is an immune modulator that acts as a dual agonist for TLR7 8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1 PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

3-Phosphoglyceric acid barium is a metabolic intermediate in both glycolysis and the Calvin cycle. It is involved in alveolar macrophage epigenetic regulation.

3-Phosphoglyceric acid (Glycerate 3-phosphate) 属于糖酸类衍生物，参与糖酵解和卡尔文循环，参与肺泡巨噬细胞的表观遗传调控，是一种常见的生物标记物。

SKLB-03220 是一种口服活性的共价抑制剂，靶向组蛋白甲基转移酶 EZH2，该酶为已知的参与观遗传调控的肿瘤学化合物靶点。SKLB-03220 的结构基于临床批准的 EZH2 抑制剂 tazemetostat，并能够消除表观遗传 H3K27me3 标记，改变染色质状态及转录活性。SKLB-03220 是癌症表观遗传研究中强效的小分子工具化合物。

Fostriecin (free base) is an inhibitor of the serine threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antibiotic.

MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂，在 WDR5 结合检测中，IC50为 2.4 nM，Ki 小于 1 nM。