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).

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).

(-)-Dexamethasone Acid, also known as (11β,16α,17α)-9-Fluoro-11,17-dihydroxy-16-methyl-3-oxoandrosta-1,4-diene-17-carboxylic acid, is a synthetic glucocorticoid. It is a fluorinated steroid and a key intermediate in the synthesis of dexamethasone, a widely used anti-inflammatory and immunosuppressant medication. 

BC18630 (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.

LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model.

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.

3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels.

BC18813 (BC 18813) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 48 nM in cell-based assays.

Apaziquone (EO-9), an analog of Mitomycin C, is a prodrug that is activated to DNA damaging species by oxidoreductases (particularly NQO1). Apaziquone has the ability to kill aerobic and/or hypoxic cancer cells. Apaziquone, a bioreductive alkylating agent, inhibits cell proliferation and induces apoptosis in oral squamous cell carcinoma (OSCC) cells. Apaziquone significantly reduces oral tumor xenograft volume in immunocompromised NOD/SCID/Crl mice.

SMS121 is a CD36 inhibitor with a KD values of about 5 µM. SMS121 reduces the uptake of lipids and inhibits cell viability in acute myeloid leukemia cells. SMS121 has antitumor activity.

Z57346765 is a PGK1-specific inhibitor that reduces the activity of metabolic enzymes in PGK1 glycolysis and inhibits PGK1-dependent cell proliferation. Z57346765 exerts inhibitory effects against clear cell renal cell carcinoma (KIRC).