AS-15

AS15 is a novel covalent nanomolar inhibitor of protein disulfide isomerase (PDI).

Batanopride is a antiemetic 5-HT3 receptor antagonist.

AS1517499 是可透过血脑屏障的STAT6磷酸化抑制剂，IC50为 21 nM。

TAS1553是一种高效的可口服蛋白质-蛋白质相互作用(PPI)抑制剂，其IC50值为0.0396 μM。TAS1553 有效地阻碍DNA复制并减少细胞内dATP池。此外，TAS1553诱导凋亡，[1]使其在癌症研究中极具价值。

Sorafenib (Bay 43-9006) 是一种多激酶抑制剂，抑制 Raf-1、B-Raf、VEGFR2、VEGFR3、VEGFR4、PDGFRβ、FLT3、c-Kit 等 (IC50=6 22 90 15 20 20 57 58 nM)，具有口服活性。Sorafenib 具有抗肿瘤活性，可以诱导细胞自噬和凋亡，也可以激动铁死亡。

B-Raf IN 15 是一种 BRAF 抑制剂，抑制 BRAFWT 和 BRAFV600E，可用于研究黑色素瘤和癌症，可用于优化成效果更好的BRA F抑制剂。

(S)-Coriolic acid (13(S)-HODE) 是一种重要的细胞内信号剂，是亚油酸与植物和哺乳动物脂氧合酶反应生成的，在各种生物系统中参与细胞增殖和分化。(S)-Coriolic acid 在 1 μM 左右时，它能抑制肿瘤细胞与血管内皮的粘附，能下调 IRGpIIb IIIa 受体的表达。(S)-Coriolic acid 是15-脂氧合酶 (15-LOX) 代谢产物，常作为内源性配体激活 PPARγ。(S)-Coriolic acid 诱导线粒体功能障碍 和气道上皮损伤。

CCT241161是一种口服活性的全RAF抑制剂，对LCK、CRAF、SRC、V600E-BRAF和BRAF的IC50值分别为3、6、10、15和30 nM。它对BRAF和NRAS突变的黑色素瘤显示出显著活性，并且展现了抗癌细胞增殖效应[1]。

STK-15 可作为脂肪酸结合蛋白 5 （FABP5） 抑制剂的候选化合物。

Sorafenib tosylate (Bay 43-9006) 是一种多激酶抑制剂，抑制 Raf-1、B-Raf、VEGFR2、VEGFR3、VEGFR4、PDGFRβ、FLT3、c-Kit 等 (IC50=6 22 90 15 20 20 57 58 nM)，具有口服活性。Sorafenib 具有抗肿瘤活性，可以诱导细胞自噬和凋亡，也可以激动铁死亡。

Cholesteryl linoleate 是低密度脂蛋白和动脉粥样硬化病变中主要的胆固醇酯。它存在于 LDL 中的胆固醇酯，利用 LDL 受体相关蛋白转移到表达 15-脂氧合酶的巨噬细胞和 CHO 细胞的质膜，被氧化形成胆固醇亚油酸氢过氧化物。

Flumazenil (Ro 15-1788) 是一种有竞争性的GABAA 受体拮抗剂，以剂量依赖的方式逆转苯二氮卓类药物诱导的作用，包括镇静、精神运动缺陷、健忘和换气不足。

cis-1-(3-Chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride (Quaternium-15 cis-form) 是一种抗菌剂，用于化妆品中作为化妆品防腐剂和抗静电剂。cis-1-(3-Chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride 是一种口服致畸剂，但不是皮肤致畸剂，在大鼠中剂量超过了化妆品的预期累积暴露量。

PD 128042 (CI 976) 是口服有效的ACAT (酰基辅酶 A: 胆固醇酰基转移酶)选择性抑制剂。它也是LPAT(溶血磷脂酰基转移酶) 抑制剂。它抑制高尔基体相关 LPAT 活性 (IC50=15 μM)。它抑制多种膜运输步骤，包括在内吞和分泌途径中发现的步骤。

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.

AS601245.2TFA (345987-15-7 free base) (AS601245.2TFA) 是一种可渗透细胞的 JNK 抑制剂（对 hJNK1、hJNK2 和 hJNK3 的 IC50 分别为 150、220 和 70 nM）。

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。

Neurotensin TFA (39379-15-2 free base) 是一种内源性 13 个氨基酸的神经肽，具有显着的阿片类非依赖性镇痛作用。它在大脑中充当神经递质，在肠道中充当激素，也充当神经调节剂。由于它与多种神经递质系统如多巴胺能、血清素能、谷氨酸能、GABA 能和胆碱能系统。它具有作为人体代谢物、有丝分裂原、神经递质和创伤的作用。

15-SAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), is recognized for its involvement in metabolic regulation. This compound comprises stearic acid esterified to 5-hydroxy stearic acid and is notably influenced by dietary changes, such as fasting and high-fat consumption, with a link to insulin sensitivity. SAHSA levels are specifically found to be moderately increased in the serum of AG4OX mice, which are characterized by their glucose tolerance through the overexpression of the Glut4 glucose transporter in adipose tissue. Given the established functions of FAHFAs in enhancing glucose tolerance, prompting insulin secretion, and exerting anti-inflammatory properties, 5-SAHSA emerges as a potential bioactive lipid implicated in the management of metabolic syndrome and inflammation.

15(S)-Fluprostenol, an isomer of the FP receptor agonist fluprostenol, serves as a potential active metabolite of 15(S)-fluprostenol isopropyl ester. It can function as an agonist at FP receptors, though with lower potency compared to its 15(R) epimer, fluprostenol.

TopoisomeraseIIα-IN-8 (compound 15)，作为人DNA拓扑异构酶IIa (htIIa) 的抑制剂，其IC50值为462 ± 38.0 μM，显示出较弱的抑制效果。

FGFR-IN-15 (compound 18i)，作为一种泛FGFR抑制剂，对FGFR1-4显示出显著的抑制效果。

HSP70-IN-6(Compound JL-15)作为一种Hsp70-Bim蛋白质相互作用(PPI)的抑制剂,其IC50值为70 nM.它能有效诱导慢性粒细胞白血病(CML)细胞的凋亡(Apoptosis),其EC50值在不同细胞株中有所不同：BV173为0.43 μM、K562为0.88 μM、K562-R3为0.19 μM.

MNK1 2-IN-7（compound 20j）是一种口服有效的 MNK1 2 抑制剂，具有抗癌活性和 hERG 安全性。它还能抑制 eIF4E 的磷酸化，并阻断 MNK eIF4E 信号通路以及癌细胞增殖。MNK1 2-IN-7 与 Ibrutinib 显示出协同作用。