AdipoGen eTOPIX: Small Molecules & Natural Products - Highlights - September 2016


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NLRP3 Inflammasome Modulators
BAT Inducers - Antidiabetic, Antibacterial & Anticancer Agents
Fluorescent Dyes


NLRP3 Inflammasome Modulators  Newly Introduced!
Prostaglandin E2 AG-CL1-0001

Inhibits NLRP3 by acting through receptor EP4 activation that increases cAMP and phosphorylates NLRP3 at serine 295 through PKA. PKA phosphorylation of NLRP3 inhibits the NLRP3 ATPase activity, which is required for assembly of NLRP3-ASC complexes.

LIT: M. Sokolowska, et al.; J. Immunol. 194, 5472 (2015) | L. Mortimer, et al.; Nat. Immunol. (Epub ahead of print) (2016)

Prostaglandin E2
N-Acetyl-D-glucosamine AG-CN2-0489

Atypical microbial danger signal that acts as a new activator of NLRP3 inflammasome by dissociating the enzyme hexokinase from the mitochondria.

LIT: A.J. Wolf, et al.; Cell 166, 624 (2016) | H. Hampton, et al.; Cell Host Microbe 20, 130 (2016)



Brown Adipose Tissue (BAT) Inducers   Newly Introduced!
PF-2545920 AG-CR1-3636

Potent and selective phosphodiesterase 10A (PDE10A) inhibitor in vitro and in vivo. Induces browning in white adipose tissue (WAT). Antiobesity and antidiabetic agent.

LIT: M.K. Hankir, et al.; EMBO Mol. Med. 8, 796 (2016)


Also Available:   Miglitol AG-CR1-3635

LIT: T. Sasaki, et al.; Endocr. J. 60, 1117 (2013) | S. Sugimoto, et al.; Nutr. Metab. (Lond) 11, 14 (2014)


Antiobesity Agents    Newly Introduced!
Indole-3-carbinol AG-CR1-3637

Widely used multifunctional aryl hydrocarbon receptor (AhR) agonist. SIRT1 activator. Antiobesity agent through inhibition of adipogenesis in adipocytes. Recently used to increase the population of innate lymphoid cells 3 (ILC3) in gut microbiota.

LIT: Y. Choi, et al.; Int. J. Obes. (Lond) 37, 881 (2013) | B.W. Megna, et al.; World J. Gastrointest. Surg. 8, 115 (2016) | M. Gomez de Aguero, et al.; Science 351, 1296 (2016)

Also Available:   
(Increases Energy Expenditure) - GW501516 (PPARδ Agonist)
BMS-309403 (FABP4 Inhibitor) - Procyanidin A2 (Antidiabetic Antioxidant)


Potent Na+/K+-ATPase Inhibitor
Gitoxin AG-CN2-0485

A cardiac glycoside and natural metabolite of digitoxin. Uncompetitive inhibitor of the Na+/K+-ATPase activity. Inhibits growth of selected human cancer cells.

LIT: M. Colovic, et al.; Russ. J. Phys. Chem. A. 83, 1602 (2009) | L. Moreno Y. Banuls, et al.; Mol. Cancer 12, 33 (2013)

Also Available:   Hellebrin AG-CN2-0475


Ionophore Antibiotic
Lasalocid A sodium salt CDX-L0015

Ionophore. Potent antibacterial agent. Coccidiostat. Forms neutral complexes with monovalent and divalent cations and transports them through apolar phase (including lipid bilayer membranes). Can also transport larger organic cations, like protonated dopamine. Identified as a 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2) inhibitor.

LIT: L.G. Nashev, et al.; PLoS One 7, e46958 (2012)

Lasalocid A sodium salt
Also Available:   Enniatin A & A1 / Enniatin B & B1


Potent & Selective GAPDH Inhibitor   Original Manufacturer!
Heptelidic acid AG-CN2-0118

Antibiotic. Potent selective glyceraldehyde 3-phosphate dehydrogenase (GAPDH) inhibitor. Selectively kills high-glycolytic cancer cells through glucose-dependent active ATP deprivation.

LIT: S. Kumagai, et al.; BBRC 365, 362 (2008)

Heptelidic acid

Strong Luminescent Dye
3,8-Diamino-6-phenylphenanthridine CDX-D0436

DNA intercalator. Used as a chromatographic affinity ligand for the specific separation and purification of supercoiled plasmid DNA (pDNA). It has been investigated for its anti-tumor and anti-viral properties.

LIT: C. Caramelo-Nunes, et al.; J.Chromatogr. A 1307, 91 (2013) | C. Caramelo-Nunes, et al.; Meth. Mol. Biol. 1286, 47 (2015)


Fluorescent pH Probes     Original Bulk Manufacturer!
BCECF-AM Solution CDX-C0603

Widely-used fluorescent intracellular pH indicator. This membrane-permeant compound is modified by intracellular esterases to produce BCECF, a polar fluorescein derivative that is retained by cells.

LIT: N. O'Connor & R.B. Silver; Meth. Cell Biol. 81, 415 (2007)

Also Available: BCECF-AM & BCECF acid

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