genomic

Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂，IC50值为 7 nM。它具有抗肿瘤活性，可研究实体瘤和淋巴瘤。

Glecaprevir (ABT-493) 是一种新型的 HCV NS3 4A 蛋白酶抑制剂，其 IC50值在 3.5 和 11.3 nM 之间。它也是 SARS-CoV 3CLpro 的抑制剂，IC50为 4.09 μM。

Isothiafludine (NZ‐4) 是一种具有口服活性的抗 HBV 化合物。Isothiafludine 通过阻断基因组前RNA（pgRNA）的包封和干扰核衣壳组装来发挥作用，可用于研究 HBV 感染。

Niraparib tosylate monohyrate 也称为 MK-4827，是一种聚 (ADP-核糖) 聚合酶 (PARP) 抑制剂，具有潜在的抗肿瘤活性。 MK4827 抑制 PARP 活性，增强 DNA 链断裂的积累，促进基因组不稳定性和细胞凋亡。 PARP 蛋白家族通过碱基切除修复 (BER) 途径检测和修复单链 DNA 断裂。

ZIM，一种从4-Aminoantipyrine衍生的降冰片烯，有效诱导DNA损伤，造成基因组及染色体损害，进而引发细胞死亡和激活吞噬。其化疗潜力适用于癌症研究。

GLP-26 是一种HBV 衣壳组装调节剂，抑制 Hep AD38 系统中的 HBV DNA 复制，IC50值为3 nM。 在 1 μM 时，使 cccDNA 降低> 90％。它破坏前基因组 RNA 的衣壳化，导致核衣壳解体，并减少 cccDNA 库。

XMD16-5 是TNK2抑制剂，对D163E 和R806Q 突变体的IC50值分别为16和77nM。

Pamiparib is a highly potent and selective PARP inhibitor. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, pro

TEI-9647 is a 1α,25-dihydroxy vitamin D3-26,23-lactone (1α,25-lactone) analog and is an effective VDR vitamin D-responsive element (DRE)-mediated genomic actions antagonist.

Anti-MRSA agent 2 (compound 14) 能够较好的抑制耐甲氧西林金黄色葡萄球菌 (MRSA) (MIC: 0.098 μg ml)，对正常细胞的毒性相对较低。Anti-MRSA agent 2 能够较强的破坏细菌膜，并具有较好的与细菌基因组DNA 结合的能力。

Anti-MRSA agent 3 能够明显的抑制耐甲氧西林金黄色葡萄球菌 (MRSA) 的活性 (MIC: 0.098 μg ml)，并且对正常细胞毒性较低。Anti-MRSA agent 3 对细菌基因组 DNA 具有较高的结合亲和力，对细菌细胞壁和细胞膜具有较强的破坏能力。

HM-cytosine (5hmC) (5hmC) 是哺乳动物基因组 DNA 中天然存在的成分，被认为是 DNA 的第六个碱基。HM-cytosine 是活性 DNA 去甲基化的中间代谢物。HM-cytosine 是已知会影响哺乳动物全局基因表达的表观遗传标记。

AB-506 是一种具有口服活性的，靶向病毒核心蛋白 HBV 复制的抑制剂。AB-506 可以与 HBV 核心蛋白结合，加速衣壳组装并抑制 HBV pgRNA 包壳。AB-506 可用于慢性乙型肝炎 (CHB)研究。

Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.

Niraparib hydrochloride (MK-4827 hydrochloride) 是一种具有口服活性的PARP1和PARP2抑制剂，IC50值分别为 3.8 nM 和 2.1 nM。它抑制 DNA 损伤修复，诱导凋亡并具有抗肿瘤活性。

5-Methylcytosine hydrochloride 在基因表达调节、基因组印记促进及转座因子抑制中扮演关键角色，亦与翻译保真度和 tRNA 识别有密切关联。

SGK1-IN-3 是有效的、口服具有活力的 SGK1 抑制剂。其中丝氨酸 苏氨酸激酶 SGK1 是 β-连环蛋白途径的激活剂，也是强大的软骨降解刺激剂，在患病的骨关节炎软骨中被发现在基因组控制下被上调。SGK1-IN-3 对骨关节炎表现出研究潜力。

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.

DN59 是一个包含 33 个氨基酸的肽，模拟登革热病毒 2 型 E 蛋白的茎区。DN59 能够抑制所有四种血清型的登革热病毒（IC50: 2-5 μM），同时也有效对抗其他黄病毒。其作用机制是通过直接与病毒颗粒相互作用，诱导基因组 RNA 的释放。DN59 展示了抗病毒活性。

PF-3837作为Mps1激酶抑制剂，具有0.33 nM的Ki值和5.5 nM的IC50值。该化合物能够通过抑制Mps1的催化活性，干扰细胞周期检查点并降低基因组稳定性，进而促使癌细胞发生凋亡（Apoptosis）。PF-3837主要应用于乳腺癌的研究领域。

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2]. TEI-9648 (10-1000 nM) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3[1]. TEI-9648 has consistently weaker suppressive effect than TEI-9647[1]. TEI-9648 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell[1]. TEI-9648 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9648 markedly suppresses the up-regulation induced by 1α,25(OH)2D3 (0.1 nM) in HL-60 cells[1]. [1]. Miura D, et al. Antagonistic action of novel 1α,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1α,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9. [2]. Kazuya Takenouchi, et al. Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D3 antagonists. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):31-4.