Aquastatin A is an inhibitor of mammalian adenosine triphosphatases. Aquastatin A is isolated from a fungus identified as Fusarium aquaeductuum. Aquastatin A inhibits Na+/K(+)-ATPase with an IC50 value of 7.1 μM, and H+/K(+)-ATPase with an apparent IC50 value of 6.2 μM.

Roridin A is an inhibitor of pollen development in Arabidopsis thaliana. Roridin A is isolated from the fungus Cylindrocarpon sp. Roridin A inhibits the pollen development at concentrations of 2 μM.

Agistatin D is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.

MC 304 is a β-resorcylate isolated from cultures of Phanerochaete chrysosporium. MC 304 has antibacterial activity. MC 304 shows a stimulatory effect on root elongation of Lepidium satiuum.

4-epi-Withaferin A (compound 28) is the analogue of Withaferin A. 4-epi-Withaferin A enhances cytotoxicity and cytoprotective heat-shock-inducing activity (HSA). 4-epi-Withaferin A has the potential for the research of protein aggregation-associated diseases by stimulating cellular defense mechanisms.

Methyl jasmonate is a phytohormone involved in plant defenses under stress conditions. Methyl jasmonate can improve antioxidant properties of blueberry leaf extracts (mainly anthocyanins), and decrease the viability and migration capacity of AGS cells. Anticarcinogenic activity.

(-)-(E)-α-Atlantone is a volatile constituent of Artemisia vestita oil.

Citalopram is marketed as a racemate mixture of the S(+)-enantiomer and R(-)-enantiomer and the active S(+)-enantiomer (Escitalopram) that possess inhibitory effects. Citalopram is an antidepressant and enhances serotoninergic neurotransmission through potent and selective inhibition of serotonin reuptake (selective serotonin reuptake inhibitor).

Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively).

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells.

CD73-IN-6 is a CD73 inhibitor extracted from patent WO2022007677A1 compound 2. CD73-IN-6 can be used for the research of cancer.

Deoxybrevianamide E, an indole alkaloid, is a biosynthetic precursor for advanced metabolites isolated from the marine-derived Aspergillus sp..

Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.

Agistatin B, isolated from fungus, is a mycotoxin. Agistatin B inhibits cholesterol synthesis.

Nangibotide TFA is a TREM-1 receptor inhibitor that can modulate innate immune response. Nangibotide TFA can reduce systemic and in situ inflammatory reaction in rodent models of myocardial ischaemia-reperfusion.

PAMP-12 is a potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM). PAMP-12 is an endogenous peptide that elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells.

Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization.

Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].

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Lefamulin acetate is a pleuromutilin antibiotic that is being developed by Nabriva Therapeutics for the treatment of acute bacterial skin and skin-structure infections.

A potent GSK3β inhibitor with IC50 of 22 nM.

ODM-203 (ODM203) is a potent, selective, dual inhibitor of FGFR and VEGFR tyrosine kinases with approximately equal potency towards recombinant FGFR1, 2, 3 and 4, as well as VEGFR1, 2 and 3 (IC50=5-35 nM).

Deferasirox (Exjade)

Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

CP-31398 is a small molecule p53 reactivator that protects p53 from thermal denaturation, not only reactivates mutant p53 but also induces stabilization of wild type p53.

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro.

SNAP-94847 is a selective, high-affinity, and competitive MCH1 receptor (MCH1-R) antagonist with Ki of 1.69 nM.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP).