Ferutinin (high purity) Reference: AG-CN2-0007 Potent, naturally occuring non-steroid estrogenic compound. Tool to promote mitochondrial calcium overload and to promote calcium-dependent opening of the mitochondrial permeability transition pore (mPTP) [1, 3, 4]. Strong agonist for estrogen receptor (ER)alpha and agonist/antagonist for ERbeta [2, 8]. Calcium ionophoretic [4, 11] Apoptosis modulator [4]. Antiproliferative [5, 7]. Increases nitric oxide synthase activity and phosphoinositides breakdown in nervous tissue [6]. Shows aphrodisiac and anti-sexual impotence activities [6]. Anti-osteoporotic. Prevents osteoporosis caused by severe estrogen deficiency [9]. Modest AChE inhibitor [10].
Hyperforin . DCHA Reference: AG-CN2-0008 Key constituent of St. John's wort. Shows properties of potential pharmacological interest, including antibacterial [1], anti-malarial [13], anti-inflammatory [7, 14], anti-cancer and anti-angiogenic effects [5, 10]. Anti-depressant and anxiolytic compound [3]. Specific activator of TRPC6 channels [11]. Inhibits the re-uptake of neurotransmitters in synapses (serotonin, norepinephrine, dopamine, GABA, glutamate) [4]. Activator of the pregnane X receptor (PXR) [2]. Regulates expression of the cytochrome P450 CYP3A4 and CYP2C9 and hepatic drugs metabolism [8]. Potential anti-Alzheimer compound [6, 9, 15]. Potent SIRT1 (sirtuin 1) and SIRT2 (sirtuin 2) inhibitor [12]. Based on the anti-inflammatory activity of Hyperforin and its simultaneous blockade of multiple signaling pathways, such as IFN‐gamma/IL‐1beta/TNF‐alpha, JAK/STAT, NF‐kappaB and MAPK it has been suggested a valuable agent for cytokine storm treatment during COVID-19 [16].
Pellitorine Reference: AG-CN2-0009 Tingling-inducing agent. Excellent stable model compound for sensory studies [3]. Exerts same profile as the unstable compound hydroxy-alpha-sanshool. Shows larvicidal, antimycobacterial and antituberculosis activity [1, 2, 4]. alpha-Glucosidase inhibitor used in diabetes mellitus, cancer, infection and inflammatory research [5]. ACAT (Acyl-CoA cholesteryl acyl transferase) inhibitor [6]. Potential anti-cancer lead compound [7]. Anti-thrombotic [8]. Anti-septic [9]. Antiprotozoal, antimalarial activity [10]. Antagonist of the TRPV1 [11].
Phorbol 12-myristate 13-acetate Reference: AG-CN2-0010 PMA/TPA is the most commonly-used phorbol ester [1,2]. Binds to and activates protein kinase C (PKC) at nM concentrations [1,2,9]. Induces cell growth arrest through a variety of pathways including the mitogen-activated protein kinases (MAPKs), p38 and c-Jun N-terminal kinase (JNK) pathways mediated by cyclin dependent kinase (CDK) inhibitors such as p21WAF1/CIP1, p27KIP1, p15 and p16. Potent mouse skin tumor promoter [3,4]. Promoter of inducible NOS (iNOS; NOS II) [5]. Apoptosis inducer [6]. Potential effective cancer therapeutic agent [7,8]. Inhibitor of anti-lipolytic activity of insulin [10]. PMA treatment stimulates THP-1 cells and generates M0 macrophages (M0).
Ferulenol Reference: AG-CN2-0011 Prenylated 4-hydroxycoumarin. Anti-tumor compound [2]. Cytotoxic [2]. Stimulator of tubulin polymerization in vitro [2]. Inhibitor of colchicine binding to tubulin [2]. Antitubercular antibiotic with potent antibacterial activity [3]. Anti-coagulant, pro-haemorrhagic compound with higher activity than warfarin [4]. Shows hepatocyte toxicity [1, 4]. Disrupts mitochondrial membrane potential [5, 6]. Potent L-malate:quinone oxidoreductase (PfMQO) inhibitor in Plasmodium falciparum. Antimalarial.
Ingenol-3-angelate Reference: AG-CN2-0012 Specific protein kinase C (PKC) activator [1]. Selective activator of PKC isoforms, like PKCtheta in T cells [1, 5, 8]. Antiproliferative and proapoptotic (necrotic) [2, 3, 5]. Immunostimulant [6]. Chemotherapeutic [4, 6]. Anticancer compound [2, 3, 5]. Efficacious agent against actinic keratosis [7]. Antileukemic [8].
alpha-Galactosylceramide Reference: AG-CN2-0013 Immunostimulant [1, 2, 3]. Potent stimulator of natural killer T (NKT) cells [4, 5]. Specific ligand of the lipid-binding MHC class I-like protein CD1d in human and mouse NKT cells [5]. Protects against LPS-induced shock [7]. Potent antitumor compound [2, 6, 8].
(25S)-Delta7-Dafachronic acid Reference: AG-CN2-0014 Ligand of DAF-12, an orphan nuclear receptor, that regulates dauer diapause, reproductive development, fat metabolism, and life span (life cycle) in parasitic nematodes [1, 2, 3]. Sterol-derived hormone. Blocks formation of infective larvae in several parasitic nematodes [4, 5]. Inhibits the dauer-promoting activity of DAF-12 [4, 5]. Supports the reproductive development [4, 5].
(-)-Ageloxime D Reference: AG-CN2-0016 Quaternary ammonium compound. Antifouling compound. Inhibits biofilm formation but not bacterial growth of Staphylococcus epidermidis. Anticancer compound. Cytotoxic against L5178Y mouse lymphoma cells.
Phomoxanthone A Reference: AG-CN2-0017 Anticancer compound. Shows antimalarial and antitubercular activity. Cytotoxic against several cancer cell lines. Antibacterial against Gram-positive bacteria and antifungal. Activator of murine T lymphocytes, NK cells and macrophages. Mitochondrial toxin with a mode of action distinct from known electron transport chain (ETC) inhibitors, OXPHOS uncouplers and ionophores. Shows rapid inhibition of both ETC and DeltaPsim, the release of mitochondrial Ca2+ and fission of the inner but not the outer mitochondrial membrane independent from the mitochondrial fission and fusion regulators DRP1 and OPA1.
(+)-Brefeldin A Reference: AG-CN2-0018 Protein transport from ER to Golgi inhibitor [2, 3]. ADP-ribosylation factor (Arf) inhibitor [6]. Cytotoxic [1]. Antibiotic [8]. Antiviral [8]. Apoptosis inducer [5]. Antitumor compound [9]. Intracellular collagen degradation inhibitor [7]. Reviews [4, 7, 8].
K-252a Reference: AG-CN2-0019 Antibiotic [1]. PKC, PKA and PKG inhibitor [1, 2, 4]. Shows neurotropic activity by inducing neurite outgrowth [3, 8, 11,16]. Highly potent cell permeable CaM kinase [6] and phosphorylase inhibitor [5]. Tyrosine protein kinase inhibitor of the TRK family [7]. Antiproliferative [9, 10, 13, 15]. Apoptosis inducer [12, 16]. Cell cycle arrest inducer [12]. Potential drug for psoriasis treatment [14].