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20

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8767 PfDHODH-IN-2

Dehydrogenase; Parasite Metabolism; Microbiology/Virology
PfDHODH-IN-2 是一种二氢噻吩酮衍生物,是一种有效的恶性疟原虫二氢乳清酸脱氢酶抑制剂,其IC50值为 1.11 µM。它具有抗疟作用,可研究疟疾。
T10903 CWHM-1552

Parasite Microbiology/Virology
CWHM-1552 是一种有效的恶性疟原虫抑制剂。 对于 3D7 和 Dd2 菌株,IC50 分别为 51 nM 和 53 nM。
T12154L N-Desethyl amodiaquine dihydrochloride

Parasite Microbiology/Virology
N-Desethyl amodiaquine dihydrochloride 是一种抗寄生虫剂,是主要的生物活性阿莫地喹代谢物。它对菌株 V1/S 和 3D7 的 IC50值分别为 97 nM 和 25 nM。
T9741 INE963

Others Others
INE963 是快速有效的血液阶段抗疟剂,EC50为 3-6 nM。INE963 有单纯性疟疾的研究潜力。
T10902 CWHM-1008

Others Others
CWHM-1008 is an effective oral antimalarial drug. The EC50 values of the drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains are 46 and 21 nM, respectively.
T63413 Antimalarial agent 15

Antimalarial agent 15 是 parasite 抑制剂,表现出抗疟作用,对恶性疟原虫 3D7 的生长具有抑制作用,其 IC50值为20 nM。
T12154 N-Desethyl amodiaquine

Parasite Microbiology/Virology
N-Desethyl amodiaquine 是一种抗寄生虫剂,是主要的生物活性阿莫地喹代谢物。它对菌株 V1/S 和 3D7 的 IC50值分别为 97 nM 和 25 nM。
T71619 ST72

ST72 is a potent inhibitor of FP2. ST72 exhibited strong growth inhibition of chloroquine-sensitive (3D7; EC50 = 2.8 µM) and chloroquine-resistant (RKL-9; EC50 = 6.7 µM) strains of Plasmodium falciparum
T61971 CHMFL-PI4K-127

CHMFL-PI4K-127 (compound 15g) 是具有口服活性、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂(IC50= 0.9 nM)。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性(EC50= 25.1 nM)。CHMFL-PI4K-127 具有抗疟疾作用。
T61047 JMI-346

JMI-346 可用作抗疟疾剂,可抑制恶性疟原虫菌株的 CQS (3D7) 和 CQR (RKL-9) 菌株生长,IC50 值分别为 13 μM 和 33 μM。JMI-346 是恶性疟原虫 -2 蛋白酶(PfFP-2)的有效抑制剂。
T15173 DSM265

PfSPZ

Dehydrogenase; Parasite Metabolism; Microbiology/Virology
DSM265 (PfSPZ) 是一种具有抗疟活性的二氢乳清酸脱氢酶抑制剂(IC50:8.9 nM)。DSM265 抑制 Pf3D7 寄生虫的生长可用于治疗和预防疟疾感染。
T78184 MMV009085

MMV009085是一种针对恶性疟原虫己糖转运体PfHT1的特异性抑制剂,具有潜在的抗疟效果。它同时抑制人葡萄糖转运蛋白,强效抑制葡萄糖吸收(IC50:2.6 μM)及恶性疟原虫3D7株的生长(EC50:1.23±0.04 μM)。
T61058 JMI-105

JMI-105 具有用作抗疟剂的潜力。JMI-105 是恶性疟原虫 -2 蛋白酶(PfFP-2)的有效抑制剂,可抑制恶性疟原虫菌株的CQS 株 (3D7) 和 CQR 株 (RKL-9) 的生长,IC50值分别为8.8 μM 和14.3 μM。在伯氏疟原虫 ANKA 感染小鼠模型中,JMI-105 显著降低寄生虫血症并延长宿主存活期。
T63456 Antimalarial agent 12

Antimalarial agent 12 是有效的抗疟 (antimalarial) 药,能够抑制恶性疟原虫 Dd2 菌株、3D7 菌株生长,其 EC50值分别为155 nM、136 nM。Antimalarial agent 12 对大肠杆菌的 MIC>250,000 nM,也能够作用于 HEK-293 和 hPHep 细胞系,其 CC50值为 10,000-50,000 nM。
T38269 Purfalcamine

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...
T11039 Didesethyl chloroquine

Bisdesethylchloroquine

Drug Metabolite Metabolism
Didesethyl chloroquine (Bisdesethylchloroquine) 是一种有效的心肌抑制剂。Didesethyl chloroquine 是抗疟药氯喹的主要代谢产物。
T36649 AN3661

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is simi...
T12838 SARS-CoV-IN-2

Others Others
SARS-CoV-IN-2 is an effective SARS-CoV replication inhibitor
T12837 SARS-CoV-IN-1

Others Others
SARS-CoV-IN-1 is an effective SARS-CoV replication inhibitor(EC50 of 4.9 μM in Vero cells).
T12839 SARS-CoV-IN-3

Others Others
SARS-CoV-IN-3 is an effective SARS-CoV replication inhibitor.

化合物

PfDHODH-IN-2
Cat.No: T8767
Synonym:
Target: Dehydrogenase, Parasite
CWHM-1552
Cat.No: T10903
Synonym:
Target: Parasite
N-Desethyl amodiaquine dihydrochloride
Cat.No: T12154L
Synonym:
Target: Parasite
INE963
Cat.No: T9741
Synonym:
Target: Others
CWHM-1008
Cat.No: T10902
Synonym:
Target: Others
Antimalarial agent 15
Cat.No: T63413
Synonym:
Target:
N-Desethyl amodiaquine
Cat.No: T12154
Synonym:
Target: Parasite
ST72
Cat.No: T71619
Synonym:
Target:
CHMFL-PI4K-127
Cat.No: T61971
Synonym:
Target:
JMI-346
Cat.No: T61047
Synonym:
Target:
DSM265
Cat.No: T15173
Synonym: PfSPZ
Target: Dehydrogenase, Parasite
MMV009085
Cat.No: T78184
Synonym:
Target:
JMI-105
Cat.No: T61058
Synonym:
Target:
Antimalarial agent 12
Cat.No: T63456
Synonym:
Target:
Purfalcamine
Cat.No: T38269
Synonym:
Target:
Didesethyl chloroquine
Cat.No: T11039
Synonym: Bisdesethylchloroquine
Target: Drug Metabolite
AN3661
Cat.No: T36649
Synonym:
Target:
SARS-CoV-IN-2
Cat.No: T12838
Synonym:
Target: Others
SARS-CoV-IN-1
Cat.No: T12837
Synonym:
Target: Others
SARS-CoV-IN-3
Cat.No: T12839
Synonym:
Target: Others
Cat. No. Product Name Target Signaling Pathways
TQ0072 Warangalone

Scandenolone,攀登鱼藤异黄酮

PKA Tyrosine Kinase/Adaptors
Warangalone is an anti-malarial compound that can inhibit the growth of both strains of parasite 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively.
T2S2362 Dehydrocorydaline nitrate

去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱

BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome
Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax,Bcl-2蛋白表达,激活 caspase-7,caspase-8,并使 PARP 失活。它能增强 p38 MAPK 活化,具有抗炎、抗癌、抗疟疾等功效。
TN4449 Longistylin C

Antifection Microbiology/Virology
Longistylin A and longistylin C show some cytotoxic effects, with IC(50) values of 0.7-14.7 microM against the range of cancer cell lines. Longistylin A and longistylin C, and betulinic acid show a moderately high in vitro activity against the chloroquine

天然产物

Warangalone
Cat.No: TQ0072
Synonym: Scandenolone,攀登鱼藤异黄酮
Target: PKA
Dehydrocorydaline nitrate
Cat.No: T2S2362
Synonym: 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱
Target: BCL, Others, PARP, p38 MAPK, Caspase, Parasite, Autophagy
Longistylin C
Cat.No: TN4449
Synonym:
Target: Antifection
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