n-Octyl-beta-D-glucopyranoside (ultrapure) Reference: AG-CC1-0008 Non-ionic detergent for the functional solubilization, isolation, purification and crystallograpy of membrane proteins. Mild, non-denaturing detergent that is used for the solubilization and reconstitution of membrane-bound proteins in their native state and for the preparation of lipid vesicles. Its well-defined chemical structure, small uniform micelles and high water solubility make it superior to most other non-ionic detergents for membrane solubilization. The high critical micelle concentration (0.7%) of n-octylglucoside facilitates ready removal from final protein extracts by dialysis or gel filtration. Used in lysis and solubilisation buffers for bacterial lipoprotein preparations, mitochondrial extracts or for determination of protein content by BCA assay. Can be used in 2D electrophoresis and to improve selectivity of immunoprecipitation of phosphotyrosine modified proteins and to increase the resolution of proteins in 2D gels.
Prostaglandin E2 Reference: AG-CL1-0001 One of the most typical lipid mediators produced from arachidonic acid (AA) by cyclooxygenase (COX) as the rate-limiting enzyme and acts on four kinds of receptor subtypes (EP1, EP2, EP3 and EP4) with high binding affinity (Kd values range between ~1-10nM). Regulator of numerous physiological functions ranging from reproduction to neuronal, metabolic and immune functions. Implied in the regulation of body temperature and sleep-wake activity. Regulating factor for bone formation and bone healing. Potent vasodilator. Influences smooth muscle relaxation, fertility and gastric mucosal integrity (first line of defense of the intestinal immune system). Acts as a pro-inflammatory mediator, but also exerts anti-inflammatory responses. As pro-inflammatory mediator, PGE2 contributes to the regulation of the cytokine expression profile of DCs and has been reported to bias T cell differentiation towards a T helper (Th) 1 or Th2 response. Exerts anti-inflammatory actions on innate immune cells like neutrophils, monocytes and NK cells. Implicated in various tumorigenic processes. Facilitates tumor progression through stimulation of angiogenesis via EP2, mediates cell invasion and metastasis formation via EP4 and promotes cell survival by inhibiting apoptosis via numerous signaling pathways. Tumor cell-produced PGE2 has been implicated in strategies of tumors for evasion of immune surveillance. Furthermore, it can enhance the inhibitory function of human regulatory T cells. Regulates vertebrate hematopoietic stem cell (HSC) homeostasis. Inhibits NLRP3 by acting through receptor EP4 activation that increases cAMP. cAMP activates PKA that phosphorylates NLRP3 at serine 295. PKA phosphorylation of NLRP3 inhibits the NLRP3 ATPase activity, which is required for assembly of NLRP3-ASC complexes.
Ageladine A . trifluoracetate Reference: AG-CMA-1001 Non-toxic, pH-sensitive fluorescent dye (blue-green range) for live imaging of pH alteration in acidic organelles, vesicles, cells, tissue and even small whole animals over several days without side effects [2,4,5,7-9]. Stronger fluorescent intensity under acidic conditions and barely detectable in alkaline solutions (wide range from pH 4 to pH 8) [2]. Highly cell/membrane permeable. Trapped within the cells and acidic organelles through hydrophobic interactions with the inner side of the membranes [2]. Barely metabolized and long-term stable, thus slow photobleaching [9]. Angiogenesis inhibitor [1,3,6]. Inhibitor of matrix metalloproteinases MMP-1,-2,-8,-9,-12,-13 [1, 3-6]. TYK2, DYRK2,Dyrk1A, YSK4 and RPS6KA1/2 inhibitor [3,5,6].
LysoGlow84™ Reference: AG-CMA-1005 Cell/membrane permeable, non-toxic, pH-sensitive fluorescent dye (blue-green range) for live imaging of pH alteration in acidic organelles, lysosomes, autophagolysosomes, vesicles, cells, tissue and even small, transparent whole animals without side effects. Useful as intracellular pH indicator with a wide range of fluorescence (pH 3 to pH 13). pH-dependent dual-emission peaks, can be used for ratiometric evaluation of pH (F400/440). No esterases are involved, therefore no toxic by-products occur. Long-term stable; is barely metabolized. Fluorescence co-localizes with LysoTracker® Red DND-99. (LysoTracker® is a registered trademark of Molecular Probes, Inc.)
Skyrin Reference: AG-CN2-0001 Non-peptidic anti-diabetic agent [1]. Receptor-selective glucagon antagonist [1]. Free radical species (·OH, R·) and singlet oxygen (1O2) scavenger [2]. Mycotoxin [3, 4]. Cytotoxic [3, 4]. Antioxidant [2]. Inhibitor of botulinum neurotoxin serotype A (BoNTA) [5]. Anti-MRSA compound [6]. Antibiotic [7].
Thapsigargin (high purity) Reference: AG-CN2-0003 Intracellular Ca2+ signaling probe [1]. Specific and sensitive inhibitor of SERCA [2]. Non-TPA/PMA tumor promoter [3]. Histamine release inducer [4]. Apoptosis inducer [5, 6, 7, 8]. Mitochondrial dysfunction inducer [6, 8]. NOS modulator [9]. Angiogenesis inhibitor [10]. Stimulator of arachidonic acid metabolism in macrophages [11]. Autophagy inducer [12, 13]. TRAIL sensitizer [14]. Inducer of ER-stress in the brain.
Zerumbone Reference: AG-CN2-0004 Chemopreventive probe. Apoptosis inducer. Potent anti-tumor compound. Sonic hedgehog signaling pathway inhibitor. Anti-inflammatory activity by downregulating COX-2 and iNOS expression via modulation of NF-kappaB activation. Antinociceptive. Potential therapeutic agent for osteoporosis and cancer-associated bone loss. Stimulator of the ATPase activity of Hsp90.
Anomalin A Reference: AG-CN2-0006 Antiproliferative agent against selected cancer cell lines. Inhibits protein kinases ALK, ARK5, Aurora-B, AXL, FAK, IGF1-R, MET, PIM1, PLK1, PRK1, SRC, and VEGF-R2 with IC50 values between 0.3 and 75.7µM, most probably contributing to the antiproliferative activity. Shown to inhibit VEGF-A dependent endothelial cells sprouting with IC50 value of 1.8µM corresponding to its in vitro inhibitory activity against VEGF-R2 protein kinase (IC50=0.8µM). Lck (p56lck; lymphocyte specific tyrosine kinase) inhibitor. Antioxidant. DPPH radical scavenger.
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).