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15

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2125	Trametinib GSK1120212,曲美替尼,JTP-74057	Apoptosis; MEK; Autophagy	Apoptosis; Autophagy; MAPK
	Trametinib (GSK1120212) 是一种 MEK 抑制剂，抑制 MEK1 和 MEK2 (IC50=0.7/0.9 nM)，具有 ATP 非竞争性和口服活性。Trametinib 可以激活自噬，诱导凋亡。
T5857	Trametinib (DMSO solvate) Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate)	Apoptosis; MEK	Apoptosis; MAPK
	Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) 是一种口服有效的 MEK 抑制剂，抑制 MEK1 和 MEK2 的 IC50分别为 2 nM。它还能激活自噬，诱导凋亡。
T19967	Fendosal 芬度柳,HP 129,P 71-0129,P71-0129,P-71-0129,HP129,HP-129	Immunology/Inflammation related	Immunology/Inflammation
	Fendosal (HP-129) 是一种非甾体抗炎药。在预防性和治疗性辅助诱导的慢性炎症多关节炎模型中，它的活性是阿司匹林的 6.9 至 9.5 倍。
T21543	AP 18	TRP/TRPV Channel	Membrane transporter/Ion channel
	AP-18 是选择性的 TRPA1 抑制剂。AP-18 可以抑制 50 μM 肉桂醛诱导的 TRPA1 激活，在小鼠和人中的 IC50 分别为 4.5 μM 和 3.1 μM。AP-18 可以逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 可以浓度依赖的方式减弱 30 μM AITC 诱导的 Yo-Pro 摄取(IC50= 10.3 μM)。
T39527	Se-DMC
	Se-DMC effectively reduces the inflammatory response, nociception, and neurobehavioral deficits induced by complete Freund's adjuvant (CFA) in mice.
T69385	Baicalein monohydrate
	Baicalein monohydrate is an inhibitor of 12-lipoxygenase, leukotriene biosynthesis and release of lysosomal enzymes. It also inhibits cellular Ca2+ uptake and mobilization and adjuvant-induced arthritis.
T69451	R-130823
	R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated ...
T38327	Cryogenine
	Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity.1 It inhibits prostaglandin synthetase (IC50 = 424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.2 \|1. Lema, W.J., Blankenship, J.W., and Malone, M.H. Prostaglandin synthetase inhibition by alkaloids of Heimia salicifolia. J. Ethnopharmacol. 15(2), 161-167 (1986).\|2. Kosersky, D.S., Brown, J.K., and Malon...
T78672	I-287
	I-287为一种口服活性PAR2选择性抑制剂，能对Gαq和Gα12/13的活性以及其下游效应物施加负异构调控。该化合物能够减轻Complete Freund's adjuvant引发的小鼠炎症，适用于免疫炎症研究。
T23676	AHR-10037
	AHR-10037是一种非甾体抗炎药，具有镇痛和解热特性以及高治疗指数，低胃毒性，它在抑制急性（伊文思蓝卡拉胶胸腔积液）和慢性（佐剂诱导的关节炎）炎症方面与吲哚美辛相当。研究表明，它在体内转化为环氧合酶抑制剂的前药。
T71510	MF-592
	MF-592 is a potent and selective antagonists of the EP4 receptor. MF-592 demonstrated good functional potency (hEP4 IC50 = 3 nM) and potent inhibition of PGE2 modulated TNFa release in LPS stimulated human whole blood (hWB) (IC50 = 78nM). In addition, it showed an excellent oral pharmacokinetic (PK) profile and in vivo efficacy in a rat chronic adjuvant-induced-arthritis model (ED50 = 0.1 mg/kg/day).. MF-592 has a desirable overall preclinical profile that suggests it is suitable for further de...
T65440	Sodium Thiosulfate Pentahydrate
	Sodium thiosulfate (Pentahydrate) is an antioxidant and antifungal. Sodium thiosulfate protects against cisplatin-induced hearing loss in children and is not associated with serious adverse events attributed to its use[3]. The addition of sodium thiosulfate, administered 6 hours after cisplatin chemotherapy, resulted in a lower incidence of cisplatin-induced hearing loss among children with standard-risk hepatoblastoma, without jeopardizing overall or event-free survival[4]. Calciphylaxis is a p...
T35406	α-MSH TFA
	α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo...
T38106	JC-171
	JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...
T83674	K 41498 TFA
	K 41498 是一种针对皮质酮释放因子受体2α（CRF2α）和CRF2β的肽拮抗剂，其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性，与CRF1相比（在表达人类受体的HEK293细胞中Ki值为425 nM）。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药，K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。

化合物

Cat.No: T2125

Synonym: GSK1120212,曲美替尼,JTP-74057

Target: Apoptosis, MEK, Autophagy

Trametinib (DMSO solvate)

Cat.No: T5857

Synonym: Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate)

Target: Apoptosis, MEK

Cat.No: T19967

Synonym: 芬度柳,HP 129,P 71-0129,P71-0129,P-71-0129,HP129,HP-129

Target: Immunology/Inflammation related

Cat.No: T21543

Target: TRP/TRPV Channel

Cat.No: T39527

Baicalein monohydrate

Cat.No: T69385

Cat.No: T69451

Cat.No: T38327

Cat.No: T78672

Cat.No: T23676

Cat.No: T71510

Sodium Thiosulfate Pentahydrate

Cat.No: T65440

Cat.No: T35406

Cat.No: T38106

Cat.No: T83674

Cat. No.	Product Name	Target	Signaling Pathways
T24403	Folinic acid HSDB 6544,Leucovorin	Endogenous Metabolite; Antifolate	Cell Cycle/Checkpoint; Metabolism
	Folinic acid (Leucovorin) 是一种可用于治疗甲氨蝶呤的生物叶酸，通常与 Methotrexate (MTX) 联用来降低 MTX 诱导的毒性，可用于辅助治疗结肠癌。
T5781	taraxasteryl acetate 蒲公英甾醇醋酸酯,醋酸蒲公英酯	Antibacterial	Microbiology/Virology
	Taraxasteryl acetate 是分离自矢状疟原虫中，具有广谱的抗炎活性。它能够改善右旋糖酐、酵母聚糖及花生四烯酸诱导的大鼠后爪水肿。它可用于研究局部炎症。
T6S0735	Flavokawain B 黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone	Apoptosis; Others	Apoptosis; Others
	Flavokawain B (Flavokavain B) 是从卡瓦醉椒的根提取物中，分离出的查尔酮。它是一种凋亡诱导剂，可抑制各种癌细胞株生长。它以极低的无毒浓度抑制人脑内皮细胞的迁移和血管形成，具有抗血管生成活性。
T78492	D-Mannuronic acid sodium
	D-Mannuronic acid sodium，一种可从Macrocystis pyrifera中分离得到的化合物，显示出在自身免疫性脑脊髓炎(EAE)、佐剂性关节炎(AIA)、肾病综合征以及急性肾小球肾炎的研究中具有潜在应用价值。
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...

天然产物

Cat.No: T24403

Synonym: HSDB 6544,Leucovorin

Target: Endogenous Metabolite, Antifolate

taraxasteryl acetate

Cat.No: T5781

Synonym: 蒲公英甾醇醋酸酯,醋酸蒲公英酯

Target: Antibacterial

Cat.No: T6S0735

Synonym: 黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone

Target: Apoptosis, Others

D-Mannuronic acid sodium

Cat.No: T78492

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

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