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21

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7700	Lersivirine 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈,Lersivirine(UK 453061),UK-453061	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Lersivirine (UK-453061) 是非核苷逆转录的抑制剂 (NNRTI)，有效抑制 NNRTI 耐药病毒。它对野生型人类免疫缺陷病毒和临床相关 NNRTI 耐药菌株显示出强大的抗逆转录病毒活性。
T15409	GNF179	Parasite	Microbiology/Virology
	GNF179 是8,8-二甲基 IP 类似物。它表现出对多药耐药菌株 W2 的效力，具有良好的体外代谢稳定性和体内口服生物相容性。
T11888	LtaS-IN-1	Others; Antibacterial	Microbiology/Virology; Others
	LtaS-IN-1 是多药耐药粪肠球菌中脂磷壁酸合成的有效抑制剂，可改变细胞壁形态。 LtaS-IN-1 对抗肠球菌属 28 菌株，MIC 值从 0.5 μg/mL 到 64 μg/mL 不等。 LtaS-IN-1 抑制菌株 E1630 和 E1590，MIC 值为 0.5 μg/mL。
T11445	GNF179 (Metabolite) GNF179 Metabolite	Others	Others
	GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability.
T80395	Abaecin
	Abaecin是一种具有针对Apidaecin抗性黄单胞菌菌株的特异活性的抗菌肽。
T72717	Anti-IAV agent 1
	Anti-IAV agent 1-1a) 是一种口服抗甲型流感病毒(IAV)剂，对IAV H1N1及Oseltamivir抗性IAV H1N1的IC50值分别是0.03μM与0.06μM。
T62600	RYL-552S
	RYL-552S 是一种可杀死恶性疟原虫 Plasmodium falciparum 的耐药菌株，其可在体外有效杀灭无性血内阶段的寄生虫。
T63865	Antimycobacterial agent-3
	Antimycobacterial agent-3 是一种抗分枝杆菌 (antimycobacterial) 剂，细胞毒性较低。Antimycobacterial agent-3 能够有效作用于药敏的 MTB 菌株 H37Rv 和耐药的临床分离株 (MIC< 0.029-0.110 μM)。
T35485	6-Prenylindole
	6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 \|1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity o...
T60302	4,4'-Dicyanostilbene
	4,4'-Dicyanostilbene (化合物 43) 是一种有效的抗疟药，可抗 Dd2 菌株，EC50值为 27 nM。4,4'-Dicyanostilbene 对耐甲氧西林金黄色葡萄球菌具有体内功效。
T79440	DprE1-IN-5
	DprE1-IN-5（Compound 10）为一种DprE1抑制剂，对Mtb H37Rv菌株表现出抗结核活性（MIC: 4 μM），并对耐药菌株具有抗分枝杆菌效果，同时展现出较高的微粒体稳定性。
T79379	Antitubercular agent-39
	Antitubercular agent-39 (Compound P1)为高效抗结核药物，活跃于耐药及药敏感临床分离菌株。其对Mtb菌株H37Rv的MIC值低于1 μM。
T79441	DprE1-IN-6
	DprE1-IN-6（Compound 56）是DprE1的一种抑制剂，对Mtb H37Rv菌株表现出抗结核活性（MIC: 4 μM），同时也对耐药分枝杆菌株有抗菌效果。该化合物具有较强的微粒体稳定性以及中等的清除速率。
T36183	Neospiramycin I
	Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III...
T79281	Antimycobacterial agent-6
	Antimycobacterial agent-6 (compound 25) 是抗结核药物，针对野生型及氟喹诺酮耐药的结核分枝杆菌 (Mtb) 株有效。此化合物对 Mtb DprE1-C387S 突变具有抑制作用，其最小抑菌浓度（MIC90）对 H37Rv 和 MoxR 株均为 0.9 μM，对 DprE1-P116S 株为 0.5 μM。
T79632	Antileishmanial agent-21	Parasite	Microbiology/Virology
	Antileishmanial agent-21 (compound 4e)，是靶向利什曼原虫蝶啶还原酶1 (Lm-PTR1) 的抗利什曼虫试剂。该化合物通过抗叶酸机制发挥作用，且其抗利什曼活性能被叶酸和亚叶酸逆转。Antileishmanial agent-21 还能抑制对 Chloroquine 抗性的恶性疟原虫菌株 (RKL9)，IC50 范围为0.0198-0.096 μM。
T79442	DprE1-IN-7
	DprE1-IN-7 (Compound 64) 是一款具有抗结核活性的DprE1抑制剂，对Mtb H37Rv菌株表现出明显的功效（MIC: 4 μM），并对耐药分枝杆菌株也显示出活性。此化合物在微粒体中稳定性强，并具有中等的清除速率。
T80279	Urumin	Influenza Virus	Microbiology/Virology
	Urumin 对人类甲型流感病毒显示出抗病毒活性，通过靶向 H1 血凝素的保守茎部位，能有效中和耐药 H1 流感病毒。它在抑制 PR8 流感病毒的生长中的半抑制浓度（IC50）为 3.8 μM，并能保护幼鼠免遭致命流感病毒感染。
T83899	N-didesmethyl Loperamide R 21345
	N-didesmethyl Loperamide是loperamide的一个活性代谢产物，属于周围μ1-阿片受体激动剂。它能抑制孤立的豚鼠肠膜丛中由电刺激引起的收缩(IC50 = 370 nM)。N-didesmethyl Loperamide还能增强对氯喹产生抗药性的P. falciparum菌株对氯喹的敏感性(EC50 = 482 nM)，同时在A-10血管平滑肌细胞中未引起毒性(IC50 = >10,000 nM)。
T78925	HIV-1 inhibitor-58
	HIV-1inhibitor-58（Compound 10c）是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂，有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株，如K103N和E138K（EC50 < 50 nM）。此外，HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用（IC50分别为2.06 μM与1.91 μM），适用于HIV感染研究。
T35902	Milbemycin A4 oxime
	Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/ml. Milbemycin A4 oxime (2.5 μg/ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, ...

化合物

Cat.No: T7700

Synonym: 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈,Lersivirine(UK 453061),UK-453061

Target: HIV Protease, Reverse Transcriptase

Cat.No: T15409

Target: Parasite

Cat.No: T11888

Target: Others, Antibacterial

GNF179 (Metabolite)

Cat.No: T11445

Synonym: GNF179 Metabolite

Target: Others

Cat.No: T80395

Anti-IAV agent 1

Cat.No: T72717

Cat.No: T62600

Antimycobacterial agent-3

Cat.No: T63865

Cat.No: T35485

4,4'-Dicyanostilbene

Cat.No: T60302

Cat.No: T79440

Antitubercular agent-39

Cat.No: T79379

Cat.No: T79441

Neospiramycin I

Cat.No: T36183

Antimycobacterial agent-6

Cat.No: T79281

Antileishmanial agent-21

Cat.No: T79632

Target: Parasite

Cat.No: T79442

Cat.No: T80279

Target: Influenza Virus

N-didesmethyl Loperamide

Cat.No: T83899

Synonym: R 21345

HIV-1 inhibitor-58

Cat.No: T78925

Milbemycin A4 oxime

Cat.No: T35902

Cat. No.	Product Name	Target	Signaling Pathways
TN2027	Oxysanguinarine 8-Oxosanguinarine,氧化血根碱,Hydroxysanguinarine	Parasite	Microbiology/Virology
	Oxysanguinarine (Hydroxysanguinarine) 是一种来自Meconopsis simplicifolia 的小檗生物碱，具有抗疟和抗血小板聚集活性，对登革热病毒具有潜在的抑制作用。
T37341	N-Acetyltyramine	Antibacterial	Microbiology/Virology
	N-Acetyltyramine 是一种群体感应抑制剂，由溶藻弧菌 M3-10 产生。N-Acetyltyramine 可以抑制C. violaceumATCC 12472 的群体感应。它可以逆转阿霉素耐药白血病 P388 细胞的耐药性。
T3831	Licoricone	Antifection	Microbiology/Virology
	Licoricone exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains.
TN3583	Canophyllal	Antifection	Microbiology/Virology
	Canophyllal shows antiplasmodial activity against the W2 strain of Plasmodium falciparum which is resistant to chloroquine and other antimalarial drugs.
TMA2418	1-Methoxyphaseollidin	PAFR; Antifection	GPCR/G Protein; Microbiology/Virology
	1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.
TN3907	Pinosylvin monomethyl ether (E)-3-Hydroxy-5-methoxystilbene	Antifection	Microbiology/Virology
	(E)-3-Hydroxy-5-methoxystilbene possesses inhibitory activity against several Gram-positive bacteria, including isolates of methicillin-resistant Staphylococcus aureus (MRSA), Mycobacterium bovis BCG, and avirulent Bacillusanthracis (Sterne strain), among
TN2311	Wulignan A1 五脂素 A1	Antifection	Microbiology/Virology
	Wulignan A1 exhibits activity against leukemia P-388 in vitro; it also may have anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities.
T81318	R-30-Hydroxygambogic acid
	R-30-Hydroxygambogic acid是从藤黄提取的一种聚戊烯酰黄酮外聚体，对K562/R和K562/S两种人白血病细胞系的IC50分别为2.89 μM和1.27 μM。该化合物适用于癌症研究领域。
TN4113	Garcinone E	Antifection	Microbiology/Virology
	Garcinone E is active constituents in the anticomplement assay used. Garcinone E exhibits potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC50 values below 3 µM. It has potent cytotoxic effect on all hepatocellular carcinomas cell lines as well as on the other gastric and lung cancer cell lines included in the screen, may be potentially useful for the treatment of certain types of cancer.
T75522	Wychimicin C
	Wychimicin C为源自罕见放线菌Actinocrispum wychmicini菌株MI503-AF4的螺旋藻酸聚酮类化合物。此化合物展现出卓越的抗菌效果，尤其对耐甲氧西林的Staphylococcus. aureus（IC50=0.125-0.5 μg/mL）和Enterococcus. Faecalis/faecium（IC50=0.125-0.25 μg/mL）展现显著的抑制活性。
T75523	Wychimicin A
	Wychimicin A 是一种螺旋藻酸聚酮，可从罕见的放线菌 Actinocrispum wychmicini 菌株 MI503-AF4 中分离得到。Wychimicin A 具有强抗菌活性，显著抑制耐甲氧西林的金黄色葡萄球菌Staphylococcus. aureus(IC50=0.125-0.5 μg/mL) 和肠球菌Enterococcus. Faecalis/faecium(IC50=0.25 μg/mL)。
T35751	Violacein
	Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 &#181M, respectively). It is also active aga...

天然产物

Oxysanguinarine

Cat.No: TN2027

Synonym: 8-Oxosanguinarine,氧化血根碱,Hydroxysanguinarine

Target: Parasite

N-Acetyltyramine

Cat.No: T37341

Target: Antibacterial

Cat.No: T3831

Target: Antifection

Cat.No: TN3583

Target: Antifection

1-Methoxyphaseollidin

Cat.No: TMA2418

Target: PAFR, Antifection

Pinosylvin monomethyl ether

Cat.No: TN3907

Synonym: (E)-3-Hydroxy-5-methoxystilbene

Target: Antifection

Cat.No: TN2311

Synonym: 五脂素 A1

Target: Antifection

R-30-Hydroxygambogic acid

Cat.No: T81318

Cat.No: TN4113

Target: Antifection

Cat.No: T75522

Cat.No: T75523

Cat.No: T35751

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