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].
Nigericin . sodium salt Reference: AG-CN2-0020 Antibiotic [1]. High affinity ionophore for monovalent cations such as H+, K+, Na+, Pb2+ [2, 3, 4, 7, 10]. Shows antibacterial (Gram-positive), antifungal, antitumor and antiviral activity [3, 6]. Disrupts membrane potential of mitochondria [2]. NLRP3/NALP3 activator. Signals through pannexin-1 to induce caspase-1 maturation and IL-1beta processing and release [5, 8, 11, 12]. Autophagy modulator [13]
Radicicol Reference: AG-CN2-0021 Antibiotic [1]. Protein tyrosine kinase inhibitor [1]. Has antifungal [4], antimalarial [6], antiangiogenic (in vivo) [2], anti-inflammatory [5] and antiviral activity. Cyclooxygenase-2 (COX-2) expression inhibitor without affecting COX-1 expression in LPS-stimulated macrophages [3, 5]. Induces the differentiation of HL-60 cells into macrophages [4]. Potent HSP90 inhibitor [7, 9, 12]. Anticancer compound [7, 9, 12]. In vivo Rad/Raf interaction inhibitor [8]. Inhibitor of AP-1-, NF-kappaB- and serum response factor (SRF)-mediated transcription. Suppresses expression of iNOS (NOS II) [10]. Non-competitive inhibitor of ATP citrate lyase [11]. DNA topoisomerase VI and type II DNA topoisomerase inhibitor [13]. Protects against LPS/IFN-gamma-induced neuronal cell death [14]. Apoptosis inducer [16]. Pyruvate dehydrogenase kinase 3 (PDK3) inhibitor, by binding directly to the ATP-binding pocket [15].
Staurosporine Reference: AG-CN2-0022 Antibiotic. Antifungal and anti-yeast activity [1]. Inhibits platelet aggregation induced by collagen or ADP. Has no effect on thrombin-induced platelet aggregation [2]. Potent, cell permeable, reversible, ATP-competitive and broad spectrum inhibitor of protein kinases. Inhibits protein kinase A, CaM kinase, myosin light chain kinase, protein kinase C, protein kinase G, CDK1/cyclin B, CDK2/cyclin A, CDK4/cyclin D, CDK5/p25, GSK-3beta and Pim-1 kinase [3, 4, 5, 6, 12]. DYRK1A inhibitor (IC50=20nM) [13]. Key apoptosis inducer [7, 8, 10, 11]. Topoisomerase II (Topo II) inhibitor [9].