hGGPPS-IN-3 (Compound 13h) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-3 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-3 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo.

Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin significantly improves cell viability and suppresses mitochondria-mediated apoptosis. Tricetin also induced the protein expression of Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and its transcriptional activation, resulting in the up-regulated expression of heme oxygenase-1 (HO-1), which conferred neuroprotection against 6-OHDA-induced oxidative damage. Tricetin has the potential for the research of Parkinson's disease (PD).

NCX4040 (NO-Aspirin), a non-steroidal anti-inflammatory drug (NSAID), is a nitric oxide (NO) releasing form of Aspirin. NCX4040 induces apoptosis in PC3 metastatic prostate cancer cells. NCX4040 has anti-inflammatory and anti-cancer effects.

Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrial membrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM.

Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer.

Physalin A is a withanolide isolated from Physalis alkekengi var. franchetii. Physalin A induces apoptosis associated with up-regulation of caspase-3 and caspase-8 expression. Physalin A induces autophagy, found to antagonize apoptosis in HT1080 cells. Physalin A has the potential for the research of cancer disease.

hGGPPS-IN-2 (Compound 16g) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-2 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-2 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo.

Petromurin C is a bisindolylbenzenoid compound isolated from the ascostromata of Petromycesmuricatus. Petromurin C induces protective autophagy and apoptosis in FLT3-ITD-positive AML.

27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively.

hGGPPS-IN-1 (Compound 18b) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-1 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-1 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo.

27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells.

AK-778-XXMU is a potent inhibitor of DNA Binding 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and more importantly, slow down the tumor growth.

αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist. RBD: receptor-binding domain

Antiviral agent 15 (Compound 15f) is a Clofazimine derivative with antiviral effects. Antiviral agent 15 inhibits both rabies virus and pseudo-typed SARS-CoV-2 with EC50 values of 1.45 μM and 14.6 μM, respectively.

Antimalarial agent 10 (Compound 17b) is an aminoalcohol quinoline compound. Antimalarial agent 10 is an antimalarial agent with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is.

HDAC1-IN-4 (JX34) is a potent Plasmodium falciparum HDAC1 inhibitor shows antimalarial activity (IC50 < 5 nM) and lower cytotoxicity.

CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively).

Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human.

Cycloaspeptide A, isolated from the endophytic fungus Penicillium janczewskii, has antiparasitic activity.

Neuraminidase-IN-4 (Compound 4b) is a potent inhibitor of neuraminidase with an EC50 of 1.59 μM. Neuraminidase (NA) is an important target for the treatment of influenza. Neuraminidase-IN-4 exhibits excellent antiviral activity against A/chicken/Hubei/327/2004 (H5N1-DW).

Herquline A (Herqueline A) is a fungal piperazine alkaloid. Herquline A is a fungal metabolite that inhibits platelet aggregation and replication of the influenza virus.

Cap-dependent endonuclease-IN-23 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-23 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-23 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8A or 8B).

Cap-dependent endonuclease-IN-21 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-21 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-21 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8B or 8A).

Cap-dependent endonuclease-IN-14 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-14 inhibits the replication of influenza virus. Cap-dependent endonuclease-IN-14 has the potential for the research of viral infections caused by influenza viruses (extracted from patent CN113620948A, compound 1-c).

Neuraminidase-IN-6 (Compound 5c) is a potent inhibitor of neuraminidase with an IC50 of 0.11 μM. Neuraminidase-IN-6 is a 1,3,4-triazole-3-acetamide derivative. Neuraminidase (NA) is an ideal target for the development of anti-influenza drugs.

Cap-dependent endonuclease-IN-13 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-13 has the potential for the research of influenza virus infection (only influenza A) (extracted from patent WO2021180147A1, compound I-1).

Neuraminidase-IN-3 (compound 23d) is a potent influenza neuraminidase (NA) inhibitor with IC50 values of 0.73, 0.26, and 0.63 nM against H1N1, H5N1, and H5N8 NAs, respectively.

Cap-dependent endonuclease-IN-10 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-10 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo pharmacokinetic and in vivo pharmacodynamic properties, and better hepatic microsomal stability. Cap-dependent endonuclease-IN-10 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2021129799A1, compound 1-1).

Cap-dependent endonuclease-IN-11 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-11 has the potential for the research of viral infections (extracted from patent WO2021129602A1, compound DSC126).

Cap-dependent endonuclease-IN-20 is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-20 shows antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC50 of 4.82 μM (CN112940009A; DSC801).