[ADIPOGEN]: LATEST ADDITIONS SMALL MOLECULES FOR IMMUNE RESPONSE RESEARCH

02 Jul [ADIPOGEN]: LATEST ADDITIONS SMALL MOLECULES FOR IMMUNE RESPONSE RESEARCH

Latest Additions   
Autophagy – NLRP3 & CARD8 Inflammasomes – STING – GLP-1R – SARS-CoV-2 – Extremolytes

NEW Chaperone-mediated Autophagy Activator
CA77.1 

CA77.1 (Prod. No. AG-CR1-0165) is a novel selective chaperone-mediated autophagy (CMA) activator by increasing the expression of the lysosomal receptor LAMP2A. CA77.1 is able to activate CMA in vitro and in vivo. It has been shown in animal studies that administration of CA77.1 may help to degrade toxic pathogenic protein products, such as tau proteins, and has potential applications in the treatment of Alzheimer’s disease.

LIT: Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome: M. Bourdenx, et al.; Cell 184, (2021)

Potent NLRP3 Inflammasome Inhibitors!
Dapansutrile 

Dapansutrile (Prod. No. AG-CR1-3535) is a potent, selective and orally active inhibitor of the NLRP3 inflammasome. It directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 adenosine triphosphatase (ATPase) activity, suppressing NLRP3 inflammasome assembly and activation. Compared to MCC950 it has a favorable toxicological safety profile for in vivo studies.

LIT: Dapansutrile, an oral selective NLRP3 inflammasome inhibitor, for treatment of gout flares: an open-label, dose-adaptive, proof-of-concept, phase 2a trial: V. Kluck, et al.; Lancet Rheumatol. 2, e270 (2020)

MCC950 . Na
MCC950 . Na (Prod. No. AG-CR1-3615) is a potent, selective and orally available NLRP3 inflammasome inhibitor that prevents oligomerization of Asc in cells stimulated with LPS and Nigericin. MCC950 is the standard inhibitor for in vitro research.

LIT: A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases: R.C. Coll, et al.; Nat. Med. 21, 248 (2015)

CARD8 – Inflammasome Sensor of HIV! NEW Insights
Efavirenz  

Efavirenz (Prod. No. AG-CR1-3751)  is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits antiviral and anticancer activities. Recently, NNRTIs such as Efavirenz and Rilpivirine (AG-CR1-3750) have been described to bind and dimerize the HIV-1-Gag-Pol polyprotein containing the protease, causing premature viral protease activation and leading to CARD8 activation in HIV-1 infected cells. Treating HIV-1-infected macrophages and CD4+ T cells with NNRTIs leads to CARD8-mediated caspase-1 activation and pyroptotic cell death.

LIT: CARD8 is an inflammasome sensor for HIV-1 protease activity: Q. Wang, et al.; Science 371, 6535 (2021)

NEW STING Agonist!
MSA-2  

MSA-2 (Prod. No. AG-CR1-0164) is a new orally available cell-permeable STING (STimulator of INterferon Genes) agonist with anti-tumoral effect. Like the natural ligand of STING, cyclic guanosine monophosphate-adenosine monophosphate (cGAMP, a cytosolic double-stranded DNA sensor), MSA-2 induces the release of type I interferons and other proinflammatory cytokines. STING-controlled interferon production is involved in antiviral defense as well as antitumor immunity.

LIT: An orally available non-nucleotide STING agonist with antitumor activity: B.S. Pan, et al.; Science 369, 6506 (2020)

Long-Acting GLP-1 Receptor Agonists BULK Available!
AdipoGen Life Sciences offers antidiabetic and antiobesity long-acting glucagon-like peptide-1 (GLP-1) receptor agonists as research reagents. GLP-1 receptor agonists stimulate insulin and suppress glucagon secretion in a glucose-dependent manner and they reduce energy intake.

SARS-CoV-2 Related Compounds BULK Available!
AdipoGen Life Sciences offers a selection of antiviral small molecules as potential tools for in vitro studies of COVID-19. There are an increasing numbers of compounds with high therapeutic potential.

High Purity Extremolytes! BULK Available!