s-10

TNFalpha-IN-S10 is an inhibitor of TNF-α.

NS-102 是一种谷氨酸受体和 NMDA 受体拮抗剂，抑制红藻氨酸 (GluK2)， 可减少由 glur6 受体介导的电流，抑制与glur6受体的特异性结合。

NPS-1034 是一种AXL 和MET 的双重抑制剂，其IC50值分别为 10.3 和 48 nM。

BMS-1001 是一种有效的 PD-1 PD-L1 相互作用抑制剂（IC50：2.25 nM，在均相时间分辨荧光结合试验中）。

BMS-1001 hydrochloride 是一种人 PD-L1 PD-1免疫检查点的抑制剂，具有口服活性且细胞毒性低。

DS-1040 Tosylate 是一种具有口服活、选择性和高效性的凝血酶活化纤维蛋白溶解抑制剂 （TAFIa） 抑制剂 ，也是纤维蛋白溶解增强剂，抑制 TAFIa 和羧肽酶 N，减少肺中现有的纤维蛋白凝块，可用于研究血栓栓塞性疾病。

LS-102 是一种选择性的 E3 连接酶 synoviolin (Syvn1) 抑制剂，是 黄芪甲苷IV衍生物，通过抑制线粒体裂变来缓解心肌缺血再灌注损伤。LS-102 抑制 Syvn1 自泛素化，可改善阿霉咪唑诱导的心率减慢，有研究心血管疾病。

CTS-1027 is a small molecule inhibitor of MMPs (IC50s: 0.3 nM, 0.5 nM for MMP2, MMP13). It has > 1,000 fold selectivity over MMP1.

TES-1025 是一种有效且特异性的人 α-氨基-β-羧基粘康酸-ε-半醛脱羧酶 (ACMSD, IC50 = 13 nM) 抑制剂。

TAS-108（亦称SR-16234）是一种选择性雌激素受体调节剂（SERM），已报道具有针对雌激素受体（ER）α的拮抗活性，并对ERβ受体表现出强亲和力及弱部分激动活性。

DTS-108 是 SN38 (一种拓扑异构酶 I抑制剂) 的前药。作为一种偶联物，DTS-108 通过酯酶敏感的交联剂将 SN38 与人类寡肽相连接。DTS-108 展现出对结直肠癌、肺癌和乳腺癌的抗癌活性。

DS-103 是一种 HDAC 抑制剂，能够抑制 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8，其 IC50 分别为 0.029、0.123、0.022、0.367 和 9.26 μM。它还可抑制恶性疟原虫 Plasmodium falciparum 3D7，IC50 为 5.08 μM。在 A2780 和 Cal27 细胞中，DS-103 展示出细胞毒性，IC50 分别为 1.48 μM 和 1.47 μM，并能逆转这两种细胞对 Cisplatin 的耐药性，IC50 分别为 4.62 μM 和 2.23 μM。DS-103 和 Cisplatin 具有协同作用，增强 Cisplatin 诱导的细胞凋亡。

RS-104966 is an inhibitor of collagenase that acts by inducing the conformational change in the side-chains of the S1 pocket of MMP-1.

ADS-103317 is an inhibitor of EGF-EGFR Interactions.

MS-1020 is a JAK3 and STAT3 inhibitor. MS-1020 selectively blocks constitutively-active JAK3 and consistently suppressed interleukin-2-induced JAK3/STAT5 signalling. MS-1020 potently inhibits persistently-active STAT3 in a cell type-specific manner.

TAS-103 is a dual inhibitor of DNA topoisomerase I II, used for cancer research. TAS-103 is a dual inhibitor of DNA topoisomerase I II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability of HeLa cells, with an IC50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation[3]. TAS-103 (30 mg kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103[2]. [1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000 Sep 15;60(6):817-21. [2]. Shimizu K, et al. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. [3]. Yoshida M, et al. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epub 2007 Dec 18.

LS-104 is a JAK2 inhibitor.

TAS-108, also known as SR16234, is a synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues.

S-1033 is an FP receptor agonist.

PBS-1086 is a novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein substrate PDHA1 in a panel of PTEN-deficient cell lines.

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) 是可用于癌症研究的一种 DNA 拓扑异构酶 I II 双重抑制剂。

DS-1001b 是IDH-1(异柠檬酸脱氢酶-1) 突变体抑制剂。

trans-10-Heptadecenoic acid 是一种能在特定酶作用下参与生物合成与代谢过程的反式脂肪酸。在 2,4-二烯酰基-CoA 还原酶与 Delta3,Delta2-烯酰基-CoA 异构酶催化下，trans-10-Heptadecenoic acid 可合成聚羟基链烷酸酯。当缺乏 2,4-二烯酰基-CoA 还原酶时，该化合物则经由多功能酶 (MFE) 中的烯酰辅酶 A 水合酶 II 进行降解。此外，trans-10-Heptadecenoic acid 能通过还原酶依赖性与直接 MFE 依赖性途径引起细胞内的碳外流。

cis-10-Heptadecenoic acid 是反刍动物脂肪的次要成分。