AK-968-11563024 is an inhibitor of marine V. vulnificus NAT [ (VIBVN)NAT] with an IC50 of 18.86 µM. NATs (Arylamine N-acetyltransferases) in marine V. vulnificus plays a role in drug metabolism, contributing to the development of drug resistance. Therefore, AK-968-11563024 can be utilized in research related to drug resistance.

9-tert-Butyldoxycycline exhibits immunomodulatory activity, alters the polarization states polymorphonuclear neutrophils, and ameliorates the inflammatory response in ischemia-reperfusion injury model. 9-tert-Butyldoxycycline is the ligand for ‘Tet-On’ switch system.

8-Nonynoic acid (non-8-ynoic acid) is a fatty acid that belongs to the group of octynoic acids. It exhibits antibacterial activity against gram-positive bacteria by binding to bacterial fatty acids. 8-Nonynoicacid also inhibits growth of gram-negative bacteria by inhibiting the synthesis of fatty acids. It is also capable of inhibiting growth of both aerobic and anaerobic bacteria in biochemical assays.

8-Hydroxyerythromycin is a semi-synthetic antibiotic with an antibacterial activity.

2,2',4'-Trichloroacetophenone (Compound 3) is an α-haloacetophenone analogue. 2,2',4'-Trichloroacetophenone exhibits good antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) with EC50 values of 0.54 and 2.02 mg/L, respectively. 2,2',4'-Trichloroacetophenone can be used for antibacteria study.

1-Aminoacridine (1-Acridinamine) is a bright fluorescent dye. 1-Aminoacridine acts as an anti-infective agent and mutagen due to its ability to interact with DNA.

11-Hydroxynovobiocin has anti-Gram-negative bacteria effect.

10-Deoxymethymycin (Antibiotic YC 17) displays antibiotic activity against Gram positive bacteria.

(R)-DS86760016 is the R-enantiomer of DS86760016 and a linker. Mc-Pro-PAB-MMAE can be used for synthesis of ADCs.

(E/Z)-MC4 is an enantiomer of the antibacterial agent MC4, which has antibacterial activity against a group of Staphylococcus aureus strains including MRSA, and has no significant toxicity to mammalian cells.

A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.

IODVA1 is a small molecule with cellular inhibitory activity against several transformed cell lines including Ras-driven cells, targets Rac activation and signaling instead of Ras; IODVA1 inhibits ST8814 cell proliferation with GI50 of 1 uM, similar results were observed with MCF7, MDA-MB-231, and T47D cells with estimated GI50s <1 uM. IODVA1 significantly decreases number of colonies of the breast cancer cells in soft agar at 1 and 3 uM. IODVA1 probably does not bind Ras and that its mechanism of action is likely Ras-independent, inhibits lamellipodia and circular dorsal ruffle (CDR) formation in MDA-MB-231 cells and decreases Rac activation. IODVA1 inhibits Rac activation and downstream signaling leading to inhibition of lamellipodia and CDR formation; IODVA1 inhibits cell-substratum and cell-cell interactions, does not target kinases, and reduces tumor burden of solid tumors in vivo.

Δ9-THCH is structurally similar to known phytocannabinoids.

Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.

AM 432 is potent, selective, orally active prostaglandin D2 receptor (DP2/CRTH2) antagonist with binding IC50 of 6 nM for hDP2.AM-432 shows no cross-reactivity against the TP or IP receptors, COX-1 or COX-2 and minimal activity at DP1 receptor. AM432 shows excellent potency in a human whole blood eosinophil shape change assay.AM432 exhibits efficacy in both a murine model of allergic rhinitis and a cigarette smoke induced inflammatory model of COPD.

Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.

Thioparib is a next-generation potent, orally bioavailable pan-PARP inhibitor with IC50 of 0.13/0.006 nM (PARP1/2), overcomes multiple PARPi resistance both in vitro and in vivo.

Novel Inhibitor of TonB Function

A potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2, ACAT2) with IC50 of 11.8 nM, >6,000-fold selectivity over ACAT1.

A derivative of the antifungal drug itraconazole (ITA) as an inhibitor of MFB cell fate in resident fibroblasts derived from multiple murine and human tissues.

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

RS-0406 is a novel beta-sheet breaker, RS-0406 reverses amyloid beta-induced cytotoxicity and impairment of long-term potentiation in vitro. RS-0406 arrests amyloid-beta oligomer-induced behavioural deterioration in vivo.

HTS13286 is a selective AQP9 inhibitor with IC50 of 1.5 uM (inhibition of CHO-AQP9 cell water permeability).

SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic.

GLPG-1690 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc.

H-151(H151) is a novel STING (stimulator of interferon genes) antagonist.

NAMPT activator (NAT-5r) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 180 nM, 3-fold improved activity over NAT.NAMPT activator (NAT-5r) had no effect on NMNAT1 enzyme activity, both NAMPT mutants of K189R and K189A reduced the binding affinity of NAT-5r.NAMPT activator (NAT-5r) treatment significantly enhanced NAD content in NAMPT-WT cells, but not in NAMPT-CRISPR cells.Treatment of NAT-5r at 3 μM concentrations for 4 h induced significant elevation of cellular NAD.NAMPT activator (NAT-5r) induced subsequent metabolic and transcriptional reprogramming, promoted proliferation and maintain the self-renewal of NSCs and protects peripheral sensory neurons from paclitaxel-(PTX) induced damage in mouse model.

A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM).