t-100

ABT-100 is a potent, highly selective, and orally active farnesyl transferase inhibitor with broad-spectrum antitumor activity.

ST-1006是一种强效组胺 H4受体激动剂（pKi：7.94）。ST-1006具有抗炎作用。ST-1006是一种有效的嗜碱性粒细胞迁移诱导剂，可诱导嗜碱性粒细胞迁移。 ST-1006 具有抗炎作用和止痒作用。

Antitumor agent-100 (compound A6) 是一种有效的口服凋亡诱导剂，靶向 PDE3A-SLFN12 分子胶 (IC50: 0.3 μM)，显示出显著的抗肿瘤活性。该化合物通过结合 PDE3A 酶口袋，招募并稳定 SLFN12，进而抑制蛋白质翻译并诱导细胞凋亡 (apoptosis)。

Antitumor agent-100 hydrochloride (compound A6) 作为细胞凋亡诱导剂和分子胶，展现了显著的抗肿瘤活性。

ACT-1004-1239 是一种可口服且具有选择性和高效性的 CXCR7 拮抗剂，具有免疫调节和髓鞘促生作用，用于研究炎性脱髓鞘疾病。

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

AT-1002 TFA is a tight junction regulator and absorption enhancer. It is a 6-mer synthetic peptide.

AT-1002 is a tight junction regulator and absorption enhancer. It is a 6-mer synthetic peptide.

AT-1002 TFA 是一种 6 聚体合成肽，是一种紧密连接 (junction) 的调节剂和吸收增强剂。

ALT-100 (HumanIgG1) 是一种靶向NAMPT的人源IgG1单克隆抗体。ALT-100 (HumanIgG1) 的同型对照为HumanIgG1kappa, Isotype Control。

Edasalonexent (CAT-1004) 是一种可口服的 NF-κB 抑制剂，可用于改善杜氏肌营养不良症。

Antifungalagent 100 (compound 3i) 展现出对S. sclerotiorum的显著抗真菌活性，其EC50值为0.33 mg L。同时，Antifungalagent 100 对S. sclerotiorum琥珀酸脱氢酶 (SDH) 的IC50为0.63 mg mL。

GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.

Kahweol oleate is emi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

BT100 为一核酸适配体，能够抑制血管性血友病因子(von Willebrand factor, VWF)与血小板糖蛋白GPIb之间的结合，旨在预防动脉血栓的形成。

Antibacterial agent 100 (Compound 7c) 是一种抗细菌和真菌剂，能够作用于 Staphylococcus aureus (MIC: 4 μg mL)、Candida albicans (MIC: 4 μg mL) 和 Cryptococcus neoformans (MIC: 8 μg mL)。

T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.

GL-1001 disodium tetrahydrate is an ACE2 inhibitor.

Avasimibe sodium is an acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitor.

Anticancer agent 100 是一种丁卡因衍生物，具有抗癌活性，可用于癌症研究。

KRN2 bromide 是有效的、选择性的 T 细胞激活核因子 (NFAT5) 的抑制剂 (IC50= 100 nM)。KRN2 bromide 可用于研究 NFAT5-介导的慢性关节炎。

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。

FGFR1 VEGFR2-IN-2 (compound 6) 属于一种针对VEGFR2和FGFR1的双重抑制剂，其对VEGFR2的IC50为0.025 µM，对FGFR1的IC50为0.026 µM。该化合物对EGFR和PDGFR-β的IC50分别为0.106 µM和0.077 µM。在NCI-60细胞系中，FGFR1 VEGFR2-IN-2展现出显著的抗肿瘤活性 (GI=60.38%)，在T-47D细胞株中的IC50达到8.51 µM，能有效抑制细胞迁移，导致细胞周期在G1期停滞，并促进细胞凋亡与坏死。同时，对MCF-7细胞株的IC50超过100 µM，对MDA-MB-231细胞株的IC50为69.17 µM，且对正常细胞无明显毒性。