synergy

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 inhibits the release of IL-8, IL-6, TNFα, and IL-1β in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.GATA4-NKX2-5-IN-1  dose-dependently inhibits the GATA4–NKX2-5 tran

SAR-405 is a potent and selective PIK3C3/Vps34 inhibitor (IC50:1.2 nM; Kd:1.5 nM) that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.

KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.

BSI-401 is an oral inhibitor of PARP-1. It can inhibit pancreatic cancer either when used alone or in synergy with Oxaliplatin.

TBK1-IN-2 (Compound A1) is a potent inhibitor of TBK1 with an IC50 of 775 pM. It binds to TBK1 through stable hydrogen bonding and π-π stacking interactions, thereby inhibiting the phosphorylation of IRF3. TBK1-IN-2 works in synergy with TNF/IFNγ to enhance immune-mediated tumor cell death and is applicable in cancer immunotherapy research.

CAY10766 is an antiviral compound.1It inhibits entry of influenza virus-like particles pseudotyped with hemagglutinin A (HA) from H5N1 influenza A virus into A549 cells (EC50= 0.24 μM). CAY10766 (1 μM) reduces H1N1 and H5N1 influenza A viral titers in infected MDCK cells. It also exhibits synergy with oseltamivir carboxylate in MDCK cells infected with the influenza A reporter PR8-NS1-Gluc virus.

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively.References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984). Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively. References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984).

DHFR-IN-1 is a selective and potent inhibitor of DHFR (dihydrofolate reductase) (IC50: 40.71 nM). DHFR-IN-1 exhibited some antifungal activity and good antibacterial activity against Gram-positive and Gram-negative bacteria.DHFR-IN-1 showed good synergy with Levofloxacin with FIC (partial inhibitory concentration index) = 0.249.

EAPB 02303 is a microtubule-disrupting agent and inhibitor that induces mitosis arrest and spindle assembly impairment, leading to apoptosis (programed cell death) and demonstrating antitumor activity. Furthermore, it exhibits potent synergy with Paclitaxel at lower concentrations [1].

(R)-IDO/TDO-IN-1 (compound 25), an indoleamine-2,3-dioxygenase (IDO) inhibitor, demonstrates good pharmacokinetic properties and exerts anti-tumor effects in the MC38 xenograft model. This compound exhibits synergy when combined with the anti-PD-1 monoclonal antibody (SHR-1210) [1].

Vinzolidine is a semi-synthetic vinca alkaloid. It exerts cytotoxic effects on tumor cells by inhibiting cell division through disruption of tubulin polymerization. Vinzolidine can be utilized in research to investigate synergy with other chemotherapy or biotherapy drugs, as well as cancer cell tolerance or resistance, and to explore strategies to overcome these challenges.

Adenosine receptor modulator 1 acts as an inducer of collagen VII (C7). It enhances the expression of COL7A1 mRNA in donor-derived keratinocytes and, in synergy with Gentamicin, increases the overall levels of C7.

D-Glucan is an orally active immune activator of the Dectin-1 receptor and possesses antioxidant properties (reduces TNF-α). It activates macrophages and neutrophils, eliminates free radicals, inhibits oxidative stress and inflammatory responses, and enhances insulin sensitivity. Additionally, D-Glucan enhances the activity of the antioxidant enzyme glutathione, inhibits gluconeogenesis, and activates GK, promoting glycolysis. It is applicable in research on liver injury protection (antagonizing Acetaminophen toxicity), radiation protection (in synergy with vitamin E), and diabetes (improving glucose metabolism).