sting-in-2

STING-IN-2 (C-170) is a potent, covalent inhibitor of STING, effectively targeting both mouse (mmSTING) and human STING (hsSTING), and is applicable for autoinflammatory disease research.

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

cGAMP (Cyclic GMP-AMPP) diammonium serves as an intrinsic second messenger in metazoans, initiating the production of interferons upon cytosolic DNA detection. It activates the stimulator of interferon genes (STING), subsequently triggering a signaling cascade that culminates in the synthesis of type I interferons and various immune mediators [1] [2] [3] [4].

Pachypodol, a methoxyflavonoid isolated from Pogostemon cablin Bentham, has antioxidant and cytoprotective properties and inhibits the growth of CaCo 2 colon cancer cell lines in vitro.Pachypodol protects neonatal rats from anesthesia-induced apoptosis in the developing brain through modulation of the JNK ERK pathway.PDGFRα kinase inhibitory activity in macrophages exposed to STING agonists.

Mal-VC-PAB-(N-Me-amide-C3)-ADU-S100 triethylamine, an immune stimulator antibody conjugate (ISAC), comprises an anti-human epidermal growth factor receptor 2 (HER2) antibody, a STING agonist (ADU-S100), and a linker, and is used in cancer research.

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Khan, K.M., Iqbal, S., Lodhi, M.A., et al. Biscoumarin: New class of urease inhibitors; economical synthesis and activity. Bioorg. Med. Chem. 12(8), 1963-1968 (2004).

5'-pApA is a linearized form of cyclic di-AMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3,4It is a metabolite of cyclic di-AMP formedviahydrolysis by various phosphodiesterases (PDEs).55'-pApA is intended for use as a negative control for cyclic di-AMP signaling. 1.Burdette, D.L., Monroe, K.M., Sotelo-Troha, K., et al.STING is a direct innate immune sensor of cyclic-di-GMPNature478(7370)515-518(2011) 2.Parvatiyar, K., Zhang, Z., Teles, R.M., et al.DDX41 recognizes bacterial secondary messengers cyclic di-GMP and cyclic di-AMP to activate a type I interferon immune responseNat. Immunol.13(12)1155-1161(2012) 3.Woodward, J.J., Iavarone, A.T., and Portnoy, D.A.c-di-AMP secreted by intracellular Listeria monocytogenes activates a host type I interferon responseScience328(5986)1703-1705(2010) 4.Witte, C.E., Whiteley, A.T., Burke, T.P., et al.Cyclic di-AMP is critical for Listeria monocytogenes growth, cell wall homeostasis, and establishment of infectionmBio4(3)e00282-00213(2013) 5.Fahmi, T., Port, G.C., and Cho, K.H.c-di-AMP: An essential molecule in the signaling pathways that regulate the viability and virulence of gram-positive bacteriaGenes (Basel)8(8)197(2017)

MSA-2 dimer, a selective and orally active non-nucleotide STING agonist with a dissociation constant (Kd) of 145 μM, demonstrates prolonged antitumor and immunogenic activity. It non-covalently binds to STING as a dimer, showing greater permeability compared to cyclic dinucleotide[1].

2',3'-cGAMP-C2-PPA (45) is a cyclic di-nucleotide that acts as a STING agonist (US20210015941A1). It is a drug-linker conjugate for antibody-drug conjugates (ADC) used in the targeted treatment of cancer.

STING Agonist-22 (CF501) is a potent non-nucleotide STING agonist that functions as an adjuvant by activating STING to induce the type I interferon (IFN-I) response and the production of proinflammatory cytokines. It enhances the efficacy of original protein vaccines by providing potent, broad, and long-term immune protection. Additionally, STING Agonist-22 has applications in research on SARS-CoV-2 variants and sarbecovirus diseases [1].

Cyclic diadenylate (c-di-AMP) sodium functions as a STING agonist by binding to the STING transmembrane protein, thus activating the TBK3-IRF3 signaling pathway. This activation prompts the production of type I IFN and TNF. Additionally, c-di-AMP sodium serves as a bacterial second messenger in Gram-positive bacteria, where it plays crucial roles in regulating cell growth, survival, and virulence, as well as the host immune response. It also acts as a potent mucosal adjuvant by stimulating both humoral and cellular responses [1] [2] [3] [4].

93-O17S is a chalcogen-containing cationic lipidoid. It has been used in the synthesis of lipid nanoparticles (LPNs) for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice. LPNs containing 93-O17S have been utilized for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens and stimulation of interferon genes [STING] activation in a B16 F10 murine melanoma model.

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

Cyclic di-GMP (c-di-GMP) diammonium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species .