T27499
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HCV Protease
PI4K
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GSK-A1 是 III 型磷脂酰肌醇 4-激酶 PI4KA 选择性抑制剂,pIC50为 8.5-9.8,抑制 PtdIns(4,5)P2 再合成,IC50约为 3 nM。GSK-A1有效降低 PtdIns(4)P 的水平,而对 PtdIns(4,5)P2 没影响。GSK-A1在抗丙型肝炎病毒方面有研究的潜力。 |
T19840
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PI4K
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GSK-F1 (PI4KA inhibitor-F1) 是一种新型强效 PI4KA 抑制剂。 |
T61971
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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。 |
T13246
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Parasite
PI4K
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UCT943是恶性疟原虫PI4K 的抑制剂(IC50 = 23 nM)。 |
T2685
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ATM/ATR
DNA-PK
PI3K
mTOR
Autophagy
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KU-55933 (ATM Kinase Inhibitor) 是一种 ATM 抑制剂,IC50和 Ki 值分别为 12.9 和 2.2 nM。它对 ATM 的选择性比对 PI3K/PI4K、 DNA-PK、ATR 和 mTOR 高。 |
T71694
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BRD73842 is an inhibitor of Plasmodium PI4K. |
T79876
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PI4K
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EDI048(化合物1.16)作为一种针对Cryptosporidium PI4K的有效口服抑制剂,其主要应用于隐孢子虫病研究领域。 |
T15651
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Others
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KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety. KDU731is an orally active C. parvum inhibitor of PI4K (IC50: 25 nM). KDU731 blocks Cryptosporidium infection in vitro and in vi |
T25826
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MMV024101 is a PI4K inhibitor. MMV024101 exhibits submicromolar potency against P. falciparum NF54 (IC50 =543 nM), low aqueous solubility (<5 μM), and rapid clearance by mouse liver microsomes with only 2% of parent compound remaining after 30 min of incu |
T68485
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Apilimod dimesylate is a potent and selective PIKfyve inhibitor. It exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Apilimod dimesylate inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. It reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. It also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells and inhibits production of IL-12 and IL-23. Apilimod dimesylate is also anti-inflammatory and water-soluble. |