inhibitor of dna binding 1

DB1976 是一种 DB270 的硒烯类似物，是一种高效且可渗透细胞的转录因子 PU.1 的抑制剂。在体外，DB1976 有效抑制 PU.1 结合 (IC50 为 10 nM)，可强烈抑制 PU.1 DNA 复合物 (具有高 DB1976-λB 亲和力，KD 为 12 nM)。DB1976 具有诱导细胞凋亡的作用。

Eicosapentaenoic Acid 是一种 ω-3 脂肪酸。

BK60106是一种选择性的跨膜蛋白CD99的抑制剂，通过直接结合CD99的胞外结构域导致Ewing Sarcoma (尤因肉瘤)细胞死亡。

COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑，是人类核糖核苷酸还原酶 (RNR) 的抑制剂，具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。

FUBP1 - in-1, with an IC50 value of 11.0 M, is an effective FUSE binding protein 1 (FUBP1) inhibitor that can interfere with the binding of FUBP1 to its SINGLE-strand target DNA FUSE sequence.

EGR-1-IN-3 (Compound 36) 是一种干扰早期生长反应 1 (EGR-1)-DNA 结合的化合物。它能抑制 TNFα 诱导的 EGR-1 与 DNA 的结合以及与炎症相关基因（如 TSLP、IL-31、IL-6 和 CCL2）的表达。EGR-1-IN-3 可用于研究炎症性疾病。

BUR1 是一种酿酒酵母细胞周期蛋白依赖性激酶 (CDK)，与在转录延伸中起作用的哺乳动物 Cdk9 同源。

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2]. Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1 2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1 2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2 M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells [1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.

T-5224 是选择性的转录因子c-Fos activator protein (AP)-1抑制剂，具有抗炎作用，能够特异性抑制 c-Fos c-Jun 的 DNA 结合活性，但对其他转录因子的结合活性无影响。它抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。

Mithramycin A (Plicamycin) 是一种dna 结合的抗肿瘤抗生素，选择性特异性蛋白1 (Sp1)抑制剂，通过降低Sp1蛋白抑制多种肿瘤的生长。特异性蛋白1 (Sp1)是一种锌指转录因子，调节多种细胞功能，促进肿瘤进展。

HBV-IN-21 (Compound II-8b) is a potent inhibitor of HBV DNA replication, exhibiting an IC50 of 2.2 μM. It demonstrates a favorable binding affinity (K D = 60.0 μM) for the HBV 4 capsid protein, thereby enabling effective interaction [1].

Topoisomerase IIα-IN-1 (compound 2) 是一种 DNA 结合配体 (DNA-binding ligands)，也是一种拓扑异构酶TopoIIα的有效抑制剂。Topoisomerase IIα-IN-1 对人类癌症细胞株表现出较好的抗增殖作用。

EBNA1-IN-SC7 (compound SC7) 是一种 Epstein-Barr nuclear antigen 1 (EBNA1) 的选择性抑制剂，能够干扰 EBNA1-DNA 结合活性 (IC50: 23 μM)。EBNA1-IN-SC7 能够用于研究 EBV (Epstein-Barr virus) 相关癌症。

DNA gyrase B-IN-1 是 DNA gyrase B 的有效抑制剂，表现出良好的结合亲和力和稳定性。DNA gyrase B-IN-1 能够抑制 P. aeruginosa i> DNA gyrase B (IC50: 2.2 μM)。

HIV-IN-5 (compound 5r) 是 HIV-1 的有效抑制剂 (IC50: 0.16 μM)。HIV-IN-5 能够与 NNIBP (NNRTIs (非核苷逆转录酶抑制剂) 结合位点) 相结合。HIV-IN-5 能够抑制 HIV DNA 依赖的 DNA 聚合作用 (IC50: 2.18 μM)。

NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.

INDOPY-1 is a Nucleotide-Competing Reverse Transcriptase Inhibitor. INDOPY-1 was the first NcRTI discovered, displaying reversible competitive inhibition of dNTP binding. 3,4 Biochemical studies showed that INDOPY-1 arrests RT DNA in a post-translocated (P site) complex.

Ginsenoside Rg5 是红参的主要成分，可阻断IGF-1与其受体的结合，IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压，具有抗炎和治疗阿尔茨海默病的潜力。

NSC194598是一种p53 DNA结合抑制剂，其体外和体内抑制p53序列特异性DNA结合的IC50值分别约为180 nM和2-40 μM。在人甲状腺髓样癌TT细胞中，NSC194598能够干扰突变RET基因的转录激活。该化合物可应用于研究放射及化学疗法对正常组织造成的急性毒性。

VK-1727为EBNA1的选择性小分子抑制剂，减弱其DNA结合活性。该化合物专一性抑制EBV+细胞的增殖与代谢功能，对EBV-细胞则无影响。VK-1727在多发性硬化症的研究中有潜在应用价值。

FTO-IN-10（化合物7）是一种针对人类去甲基酶FTO（脂肪量和肥胖相关蛋白）的有效抑制剂，其IC50值为4.5 μM。该化合物通过疏水作用和氢键相互作用与FTO的结构域II的结合口袋相结合。在A549细胞中，FTO-IN-10能够诱导DNA损伤和自噬性细胞死亡。

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。

GSK_WRN3 是 WRN 蛋白酶的选择性抑制剂 (IC50 = 8.6 μM)。通过与 WRN 蛋白的 Cys727 残基形成共价结合，显示出高度选择性。通过抑制 WRN 蛋白酶的活性，减少对 MSI 肿瘤细胞的生长支持，导致这些细胞 DNA 双链断裂的增加和细胞生长的抑制。

SAV13 是 SaeR 的抑制剂，也是 HR3744 的类似物。SAV13 抑制 SaeR-DNA 探针结合，并具有抗病毒特性。