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17

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8550 NDMC101

Others; NF-κB; Proteasome NF-κB; Others; Proteases/Proteasome; Ubiquitination
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。
T4282 S-methyl-KE-298

MMP; Drug Metabolite Metabolism; Proteases/Proteasome
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。
T73425 CFT8634

CFT8634 是一种靶向 BRD9的降解剂,可用于滑膜肉瘤和 SMARCB1 缺失实体瘤的研究。
T19771 SXT1596

NSC-65667,SXT-1596,NSC 65667,SXT 1596,NSC65667

SXT1596 is a novel SS18-SSX/TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.
T35480 dBRD9-A

dBRD9-A

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.
T70230 FPTI

FPTI is an inhibitor against SYT-SSX1 fusion protein in synovial sarcoma which down-regulates SYT-SSX1 and modulates its downstream target genes.
T31751 Fce 21258

Ddh-carbo pgl2

Fce 21258 is used to stimulate the adenylate cyclase of synovial fluid macrophages.
T82239 HAP-1

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。
T76989 Tabituximab barzuxetan

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。
T68344 AGG-523

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.
T70834 BE-16627B

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 mi...
T71525 AB05831

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. ...
T38143 Elaidamide

Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-150...
T60979 Oxaprozin potassium

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。
T37606 Resolvin D5

7(S),17(S)-diHDHA

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid . [1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D5 (RvD5) is a DHA-derived resolvin generated by a double dioxygenation mechanism.[3] RvD5 has been identified in media from ionophore-stimulated trout brain cells, in human synovial fluid from patients with rheumatoid arthritis, and in...
T68321 AS1940477

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 c...
T80242 TNO211

MMP Proteases/Proteasome
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。

化合物

NDMC101
Cat.No: T8550
Synonym:
Target: Others, NF-κB, Proteasome
S-methyl-KE-298
Cat.No: T4282
Synonym:
Target: MMP, Drug Metabolite
CFT8634
Cat.No: T73425
Synonym:
Target:
SXT1596
Cat.No: T19771
Synonym: NSC-65667,SXT-1596,NSC 65667,SXT 1596,NSC65667
Target:
dBRD9-A
Cat.No: T35480
Synonym: dBRD9-A
Target:
FPTI
Cat.No: T70230
Synonym:
Target:
Fce 21258
Cat.No: T31751
Synonym: Ddh-carbo pgl2
Target:
HAP-1
Cat.No: T82239
Synonym:
Target:
Tabituximab barzuxetan
Cat.No: T76989
Synonym:
Target:
AGG-523
Cat.No: T68344
Synonym:
Target:
BE-16627B
Cat.No: T70834
Synonym:
Target:
AB05831
Cat.No: T71525
Synonym:
Target:
Elaidamide
Cat.No: T38143
Synonym:
Target:
Oxaprozin potassium
Cat.No: T60979
Synonym:
Target:
Resolvin D5
Cat.No: T37606
Synonym: 7(S),17(S)-diHDHA
Target:
AS1940477
Cat.No: T68321
Synonym:
Target:
TNO211
Cat.No: T80242
Synonym:
Target: MMP
Cat. No. Product Name Target Signaling Pathways
TN4893 Rapanone

拉帕酮,2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone,2,5-Dihydroxy-3-tridecylcyclohexa-2,5-diene-1,4-dione,酸藤子醌

Apoptosis; Phospholipase; Antibacterial; Parasite Apoptosis; Metabolism; Microbiology/Virology
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。
T3762 Hyaluronic acid

透明质酸,Hyaluronate,玻尿酸,hyaluronan

Others; Endogenous Metabolite Metabolism; Others
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。
TN4505 Masticadienolic acid

Others Others
Masticadienolic acid is a specific competitive inhibitor of secreted phospholipase A2, it not only protects the active site histidine from alkylation but also inhibits the action of secreted from pancreas, synovial fluid, and bee venom. Masticadienolic ac
T21893 Luffariellolide

Luffariellolide 是人滑膜蛋白磷脂酶A2 (HSF-PLA2) 抑制剂 (IC50=5 μM)。Luffariellolide (ED50=50 μg/耳)可有效抑制佛波酯 (PMA) 引起的耳水肿。

天然产物

Rapanone
Cat.No: TN4893
Synonym: 拉帕酮,2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone,2,5-Dihydroxy-3-tridecylcyclohexa-2,5-diene-1,4-dione,酸藤子醌
Target: Apoptosis, Phospholipase, Antibacterial, Parasite
Hyaluronic acid
Cat.No: T3762
Synonym: 透明质酸,Hyaluronate,玻尿酸,hyaluronan
Target: Others, Endogenous Metabolite
Masticadienolic acid
Cat.No: TN4505
Synonym:
Target: Others
Luffariellolide
Cat.No: T21893
Synonym:
Target:
TargetMol Loading
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