synovial

Rapanone (2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone) 是一种具有广泛生物活性的天然苯醌，如抗肿瘤、抗氧化、抗炎、抗菌和抗寄生虫活性。它还是选择性人滑膜 PLA2抑制剂，IC50值为 2.6 μM。

NDMC101 是有效的破骨细胞形成抑制剂，通过下调 NFATc1 调控基因表达抑制破骨细胞分化。它与 DPP4底物相似，通过抑制DPP4抑制早期 T 细胞激活。它能够用于骨疾病的研究，如类风湿关节炎、滑膜炎等。

Hyaluronic acid (hyaluronan) 由玉米发酵得到，是由二糖的重复单元组成的生物聚合物，应用领域广泛。

DNJNAc（亦称 2-Acetamido-1,2-dideoxynojirimycin）是一种高效且特异性的 β-己糖胺酶 (HEX) 抑制剂。HEX 酶催化糖蛋白、神经节苷脂及糖胺聚糖等糖结合物中末端非还原 N-乙酰-β-D-葡萄糖胺 (GlcNAc) 和 N-乙酰-β-D-半乳糖胺 (GalNAc) 的水解。软骨细胞分泌的 HEX 进入细胞外空间，可导致软骨基质降解，使骨关节炎滑液中的 HEX 活性升高。

SXT1596 is a novel SS18-SSX/TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.

Anti-inflammatory agent 79 (compound 17q) 是一种基于异喹啉酮衍生物的HIF-1抑制剂 (IC50: 0.55 μM)，能够有效抑制HIF-1信号并促进HIF-1α的降解。它可以抑制滑膜的侵袭和迁移，以及血管生成。在小鼠炎症模型中，Anti-inflammatory agent 79 还有效减少足部肿胀和关节炎，降低体内的炎症因子水平和血管增生。

SB-505124 hydrochloride (SB505124 hydrochloride) 是一种可口服且具有选择性和高效性的 TGF-βI 型受体(ALK4，ALK5，ALK7) 抑制剂，对 ALK4，ALK5 的IC50值分别为 129 nM 和 47 nM。SB-505124 hydrochloride 抑制滑膜外植体产生 IL-6，通过降低 Il17a 和 Rorc 基因表达以及 IL-17 蛋白的产生减少小鼠 Th17 分化。SB-505124 hydrochloride 可用于研究结直肠癌。

Fce 21258 is used to stimulate the adenylate cyclase of synovial fluid macrophages.

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

Resolvin D5是一种从DHA中提取的氧化脂质介质，具有抗炎作用，在LPS刺激的THP-1细胞中通过ERK-NF-κB信号通路抑制IL-6和CCL5的产生。

9(E)-Octadecenamide(Elaidamide)是一种脂肪酸酰胺和内源性代谢物，能够抑制大鼠的mEH（microsomal epoxide hydrolase），Ki=70 nM。

S-methyl-KE-298 是 KE-298 的活性代谢物。KE-298 抑制类风湿关节炎滑膜细胞产生基质金属蛋白酶。

Oxaprozin potassium 是具有口服活性的COX 的抑制剂，其对人血小板COX-1 的IC50值为 2.2 μM，对 IL-1 刺激的人类滑膜细胞COX-2的IC50值为 36 μM。Oxaprozin potassium 诱导细胞凋亡。Oxaprozin potassium 还抑制 NF-κB 活化，Oxaprozin potassium 介导的Akt/IKK/NF-κB 通路抑制有助于其抗炎特性。

AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg/kg (ED(50)=0.053 mg/kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......

AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury.

FPTI is an inhibitor against SYT-SSX1 fusion protein in synovial sarcoma which down-regulates SYT-SSX1 and modulates its downstream target genes.

BE-16627B is a novel metalloproteinase (MP) inhibitor isolated from Streptomyces sp. BE16627B selectively inhibited MPs such as human stromelysin and 92 kD gelatinase. After the cells were cultured with BE16627B for 5 days, BE16627B inhibited MP activity in the primary culture supernatants from synovial cells in a dose-dependent fashion without showing apparent cytotoxicity or affecting the production and secretion of MPs. Its IC50 for active collagenolysis before activation by trypsin was 25 microM.

FHD-609是一个有效的BRD9抑制剂和PROTAC降解剂，靶向非经典BAF(ncBAF)亚基BRD9，从而消耗SS18-SSX融合蛋白，可用于研究滑膜肉瘤（SS）。

Tabituximab barzuxetan (OTSA101-DTPA-90Y) 是一种放射免疫偶联物，由靶向FZD-10 (OTSA-101)的人源化单克隆抗体组成，并用钇 90 标记。Tabituximab barzuxetan 具有抗肿瘤活性。Tabituximab barzuxetan 可用于滑膜肉瘤的研究。

TNO211为具备生物活性的肽，主要研究对象是基质金属蛋白酶（MMP），一类能够降解多种细胞外基质蛋白并调控诸多生物活性分子的肽链内切酶家族。MMP在细胞表面受体裂解、凋亡配体释放及趋化因子/细胞因子失活等过程中起作用，同时与细胞增殖、迁移（粘附/分散）、分化、血管生成、细胞凋亡及宿主防御等生物行为密切相关。TNO211可靶向MMP-2、8、12、13和14，包含MMP特定可裂解的Gly-Leu键，并具有EDANS/DABCYL荧光标记，其荧光检测在监测内皮细胞培养基和患者滑液中的MMP活性方面表现出高灵敏度。吸光度/电磁场测量参数为340/490 nm。

HAP-1为针对滑膜细胞的转导肽，可促进蛋白质复合物在人类及兔子滑膜细胞中的特异性内吞作用。当HAP-1与抗菌肽(KLAK)2融合时，形成促进细胞凋亡的肽DP2。

1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.

PDE4-IN-18 (compound 1l) 作为PDE4抑制剂 (IC50=1.55 μM),展现了显著的抗炎效果.该化合物通过减少免疫细胞的过度浸润和肠膜形成,以及显著降低滑膜组织内如TNF-α和IL-6等促炎细胞因子的mRNA水平,有效抑制炎症.PDE4-IN-18 主要用于类风湿性关节炎和银屑病的相关研究.

Pronqodine A 是一种从 Streptomyces 中发现的醌类化合物，具有酶抑制和抗炎活性。它抑制NAD(P)H:醌受体氧化还原酶1 (NQO1; IC50 = 131.5 nM)。在SW 982人类滑膜肉瘤细胞中，Pronqodine A 抑制由缓激肽诱导的前列腺素E2 (PGE2)、6-keto PGF1α 和 PGD2 的产生 (IC50 分别为9, 19, 和 7 nM)。此外，它还能在SW 982细胞中诱导活性氧(ROS)的产生。