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.

(-)-Luteoskyrin has a wide range of antibacterial activity, such as against malaria (with an IC50 of 0.51 μg/mL), tuberculosis (MIC of 6.25 μg/mL), and it also shows antibacterial effects (with MIC for Gram-positive bacteria ranging from 0.39 to 1.56 μg/mL, and for Gram-negative bacteria from 3.13 to 12.50 μg/mL), as well as antifungal activity (with MIC against plant pathogens ranging from 3.13 to 50μg/mL). (-)-Luteoskyrin exhibits cytotoxicity against NCI-H187 cells, with an IC50 range of 0.16–17.99 μg/mL.

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.

FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor. FAP-IN-2 can be used for tumor imaging. FAP-IN-2 has good stability, high uptake and good retention in the tumor site of mouse model.

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.

Methoxy-X04 is a fluorescent dye that crosses the blood-brain barrier and selectively binds to beta-pleated sheets found in dense core amyloid Aβ plaques.

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.

MC-VC-PABC-amide-PEG1-CH2-CC-885 is an Antibody-Drug Conjugates (ADC) based on protein degrading agent (protac molecular glue, etc.).

DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.

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.

D223 is a molecular glue and promotes glucose uptake in the absence of insulin. D223 also increases the affinity of RAS binding to PI3Kα by ~500-fold.

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

MT125​​ is a brain-penetrant small-molecule inhibitor selectively targeting non-muscle myosin IIA/B (NMIIA/B) with >20-fold specificity over cardiac myosin. It demonstrates potent anti-glioblastoma activity by: (1) blocking tumor invasion and cytokinesis (inducing polyploidy), (2) disrupting mitochondrial dynamics to elevate ROS and trigger ferroptosis, and (3) sensitizing tumors to radiotherapy/kinase inhibitors via ROS-driven PDGFR/mTOR pathway activation. Subcutaneous administration achieves brain concentrations twice plasma levels (t_1/2~10.5 hr) with no toxicity observed at 15× the therapeutic dose in rats. MT-125 monotherapy extends survival in GBM models, while combinations with PDGFR/PI3K inhibitors induce long-term remission (>40% mice). Its first-in-class mechanism, safety profile, and CNS bioavailability support clinical development for glioblastoma.

Alirocumab is a human monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9) and it can reduce cholesterol levels in the blood.

Nivolumab anti-PD-1) is a genetically engineered fully human immunoglobulin Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1PD-1PCD-1) with immune checkpoint inhibitory and antineoplastic activities.

BC18630 free base (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.

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).