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23

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12103	MR-L2	PDE	Metabolism
	MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂，可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成，其EC50=1.2 µM。
T2394	Pixantrone dimaleate 匹克生琼来酸盐,BBR-2778,Pixantrone Maleate,BBR 2778 dimaleate,马来酸匹衫琼	Topoisomerase	DNA Damage/DNA Repair
	Pixantrone dimaleate (Pixantrone Maleate) 是一种拓扑异构酶 II 的抑制剂和 DNA 嵌入剂，是一种实验性抗肿瘤药物。
T26619	Amitivir LY217896,LY 217896,阿米替韦,LY-217896	Others; Influenza Virus	Microbiology/Virology; Others
	Amitivir (LY 217896) 是一种噻二唑衍生物，对 A 和 B 型流感病毒均有效，对正粘病毒和副粘病毒具有广泛的抗病毒活性。
T37466	CAY10766
	CAY10766 is an antiviral compound.1It inhibits entry of influenza virus-like particles pseudotyped with hemagglutinin A (HA) from H5N1 influenza A virus into A549 cells (EC50= 0.24 μM). CAY10766 (1 μM) reduces H1N1 and H5N1 influenza A viral titers in infected MDCK cells. It also exhibits synergy with oseltamivir carboxylate in MDCK cells infected with the influenza A reporter PR8-NS1-Gluc virus.
T36391	Spiro-Oxanthromicin A
	Spiro-oxanthromicin A is a polyketide that has been found inStreptomyces.1It induces mislocalization of K-RAS in MDCK cells (IC50= 26.7 μM). 1.Salim, A.A., Xiao, X., Cho, K.J., et al.Rare Streptomyces sp. polyketides as modulators of K-Ras localisationOrg. Biomol. Chem.12(27)4872-4878(2014)
T61904	HSP90-IN-14
	HSP90-IN-14 (compound 4) 是有效的Hsp90 抑制剂（Kd= 0.26μM）。在MDCK 细胞中，HSP90-IN-14 表现出抗流感病毒活性，抗 A/H3N2、A/H1N1 和 B 型流感病毒的EC50分别为 2.6、3.9 和 17 μM。
T39057	Rozanolixizumab UCB7665	Others	Others
	Rozanolixizumab（RYSTIGGO）是一种针对人类新生儿 Fc 受体（FcRn）的高亲和力人源化免疫球蛋白 G4 单克隆抗体，用于研究自身免疫和同种免疫疾病中致病性 IgG 。
T38340	10-Norparvulenone
	10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml. 1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000)
TP1990	Norleual
	Angiotensin IV analog. Highly potent HGF/c-MET inhibitor (IC50 = 3 pM). Inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Also AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic.
T79353	P-gp/BCRP-IN-2
	P-gp/BCRP-IN-2（化合物15）为恶二唑衍生物，作为ABC转运蛋白P-glycoprotein（IC50：1.6 nM）及BCRP（IC50：600 nM）的双重抑制剂。该化合物增强了Doxorubicin针对耐药型人腺癌结肠癌细胞系HT29/DX及MDCK-MDR1细胞的抗增殖效果。
T68568	Encequidar, HCl
	Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.
T36974	D-threo-PPMP hydrochloride
	D-threo-PPMP is a glucosylceramide (GlyCer) synthetase inhibitor.1,2It is the active enanantiomer and enzymatic inhibitory component of the racemic DL-threo-PPMP . In MDCK kidney epithelial cells, D-threo-PPMP induces a 70% reduction in cell growthin vitroat 20 μM and significantly inhibits DNA synthesis at 3 μM.3[Matreya, LLC. Catalog No. 1865] 1.Shen, W., Henry, A.G., Paumier, K.L., et al.Inhibition of glucosylceramide synthase stimulates autophagy flux in neuronsJ. Neurochem.129(5)884-894(201...
T60778	Anti-Influenza agent 3
	Anti-Influenza agent 3 (compound 11h) 是有效的抗流感药物，对 MDCK 上皮细胞显示出低细胞毒性。Anti-Influenza agent 3 抑制 M2 WT 和 S31N 离子通道的传导性。Anti-Influenza agent 3 对 A/HK/68 (H3N2, M2-WT) 菌株的 EC50值为 3.29 μM，对 A/WSN/33 (H1N1, M2-S31N) 菌株的 EC50值为 2.45 μM。
T73347	BCX-1898
	BCX-1898 是一种环戊烷衍生物，是口服有效的，选择性的流感病毒神经氨酸酶 (influenza virus neuraminidase) 抑制剂。BCX-1898 具有抗病毒活性，对 MDCK 细胞中的甲型流感病毒 (H1N1、H3N2、H5N1) 和乙型流感病毒复制的 EC50值为 <0.01-21 μM。BCX-1898 显示出对小鼠流感模型的保护作用。
T27038	CL385319 HCl CL-385319,CL385319 hydrochloride,CL 385319,CL385319
	CL385319 is a potent inhibitor of H5N1 avian influenza A virus infection by blocking viral entry. CL-385319 is effective in inhibiting infection of highly pathogenic H5N1 influenza A virus in Madin-Darby Canine Kidney (MDCK) cells with an IC50 of 27.03±2.
T38011	C2 Adamantanyl Globotriaosylceramide (d18:1/2:0)
	C2 Adamantanyl globotriaosylceramide (AdaGb3) is a bioactive sphingolipid and water-soluble form of globotriaosylceramide that contains an adamantanyl group in place of the fatty acyl chain. It inhibits Vero toxin binding to globotriaosylceramide in an ELISA assay when used at a concentration of 10 μM. AdaGb3 decreases cell surface expression of P-glycoprotein (P-gp) and reduces efflux of rhodamine 123 in MDCK cells. It also increases apical-to-basal transport of vinblastine in human intestinal ...
T79567	Antiviral agent 35	Influenza Virus	Microbiology/Virology
	Antiviralagent 35 (compound 4d) 作为一种口服抗流感病毒药物，针对流感病毒复制的早期阶段有效。该化合物能够阻断流感病毒引发的ROS积聚、自噬及细胞凋亡，同时在肺部感染的小鼠模型中，抑制RIG-1通路所介导的炎症响应。Antiviralagent 35展现出低细胞毒性（CC50>800 μM，MDCK细胞）且对H1N1（A/Weiss/43）展现出显著的抗病毒活性，EC50为2.28 μM。
T38103	Defensin HNP-3 (human) (trifluoroacetate salt)
	Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd...
T37843	Australine (hydrochloride)
	Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehal...
T36745	cDPCP
	cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad...
T36015	PDMP (hydrochloride)
	PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
T62469	RSV/IAV-IN-3
	RSV/IAV-IN-3 (compound 14'i) 是一种双重的呼吸道合胞病毒 (RSV) (EC50: 2.92 μM) 和甲型流感病毒 (IAV) (EC50: 1.90 μM) 的双重抑制剂。RSV/IAV-IN-3 对 H1N1 和 H3N2 表现出抗病毒作用，在 MDCK 细胞中的 EC50值分别为 3.25 μM 和 1.50 μM。RSV/IAV-IN-3 能够剂量依赖性地明显抑制荧光素酶的活性 (EC50: 3.89 μM)。RSV/IAV-IN-3 可以抑制 IAV 感染和 RdRp 活性，在进入后阶段抑制 IAV 和 RSV 复制。
T62812	RdRP-IN-4
	RdRP-IN-4 (compound 11q) 是一种芳基苯甲酰肼类似物，是一种口服具有活力的甲型流感病毒 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂，能够直接结合 RdRp 的 PB1 亚基。RdRP-IN-4 可有效抑制 H5N1 禽流感病毒株，在 MDCK 细胞的 EC50=18 nM。RdRP-IN-4 对 H1N1 (A/PR/8/34) Flu A 株和 Flu B 株 (B/Lee/1940) 具有抑制作用，其 EC50 值分别为 53 nM 和 20 nM。RdRP-IN-4 以剂量依赖性方式显著抑制病毒核蛋白 (NP) 的表达水平。RdRP-IN-4 在受感染的小鼠中具有明显的抗病毒作用。

化合物

Cat.No: T12103

Target: PDE

Pixantrone dimaleate

Cat.No: T2394

Synonym: 匹克生琼来酸盐,BBR-2778,Pixantrone Maleate,BBR 2778 dimaleate,马来酸匹衫琼

Target: Topoisomerase

Cat.No: T26619

Synonym: LY217896,LY 217896,阿米替韦,LY-217896

Target: Others, Influenza Virus

Cat.No: T37466

Spiro-Oxanthromicin A

Cat.No: T36391

Cat.No: T61904

Rozanolixizumab

Cat.No: T39057

Synonym: UCB7665

Target: Others

10-Norparvulenone

Cat.No: T38340

Cat.No: TP1990

Cat.No: T79353

Encequidar, HCl

Cat.No: T68568

D-threo-PPMP hydrochloride

Cat.No: T36974

Anti-Influenza agent 3

Cat.No: T60778

Cat.No: T73347

Cat.No: T27038

Synonym: CL-385319,CL385319 hydrochloride,CL 385319,CL385319

C2 Adamantanyl Globotriaosylceramide (d18:1/2:0)

Cat.No: T38011

Antiviral agent 35

Cat.No: T79567

Target: Influenza Virus

Defensin HNP-3 (human) (trifluoroacetate salt)

Cat.No: T38103

Australine (hydrochloride)

Cat.No: T37843

Cat.No: T36745

PDMP (hydrochloride)

Cat.No: T36015

Cat.No: T62469

Cat.No: T62812

Cat. No.	Product Name	Target	Signaling Pathways
T4S0779	D-tetrahydropalmatine	Others; Dopamine Receptor	GPCR/G Protein; Neuroscience; Others
	D-Tetrahydropalmatine 是一种主要存在于延胡索类植物中的异喹啉生物碱。它是有机阳离子转运蛋白 1 抑制剂。它是多巴胺受体拮抗剂，对 D1 受体具有优先亲和力。
TN5005	Shegansu B	Influenza Virus	Microbiology/Virology
	Shegansu B exhibits significant in vitro anti-influenza viral activity in MDCK cells.
T27380	FR-198248
	FR-198248, a new anti-influenza agent, shows antiinfluenza virus activity in Madin-Darby canine kidney (MDCK) cells in vitro.
T8521	Gnetin D
	Gnetin D exhibits significant in vitro anti-influenza viral activity in MDCK cells, with IC(50) values from 0.67 to 11.99 ug/mL.
T38015	Herquline A
	Herquline A is an alkaloid fungal metabolite originally isolated from P. herquei. It inhibits cell death induced by influenza A strain A/PR/8/34 in MDCK cells with an IC50 value of 10 μg/ml and inhibits viral replication in a plaque assay in a concentration-dependent manner. Herquline A also inhibits platelet aggregation induced by ADP and platelet-activating factor (PAF) in vitro (IC50s = 180 and 240 μM, respectively).

天然产物

D-tetrahydropalmatine

Cat.No: T4S0779

Target: Others, Dopamine Receptor

Cat.No: TN5005

Target: Influenza Virus

Cat.No: T27380

Cat.No: T8521

Cat.No: T38015

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