cpg 2

2-PMPA (2-(Phosphonomethyl)pentanedioic acid) 是谷氨酸羧肽酶II 的选择性抑制剂(IC50:300 pM)。

2-Benzylsuccinic acid (DL-Benzylsuccinic acid) 是羧肽酶 A (CPA) 抑制剂。

Carboxypeptidase G2 (CPG2) Inhibitor (CPG2 Inhibitor) 是新型的羧肽酶 G2(CPG2)抑制剂，显示出抗癌活性。

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

WEHI-150是一种米托蒽醌类似物，作为DNA链间交联剂，具有12.5小时的半衰期。该化合物能够在CpG序列上形成共价加合物，对甲基化CpG位点表现出选择性。甲醛激活的WEHI-150能够诱导DNA链间交联，并表现出浓度依赖性的转录阻断作用。此外，WEHI-150还能在新的DNA序列中形成加合物，这不涉及与鸟嘌呤N-2的相互作用。

GSK3735967为选择性、可逆的非核苷类DNMT1抑制剂，具备平面二氰基吡啶核心，专一性嵌入DNMT1所结合的半甲基化CpG双核苷酸中。该化合物包含三个结合位点，其中之一可与组蛋白H4K20me3相结合。

KCC-07 是一种甲基-CpG 结合域蛋白 2 (MBD2) 的选择性、强效和脑渗透抑制剂，具有抗癌活性。它阻止 MBD2 与甲基化 DNA 结合并激活脑特异性血管生成抑制剂 1，诱导抗增殖 BAI1 p53 p21 信号传导。