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.

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. 

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).

SR-717 is an agonist of stimulator of interferon genes STING for treating cancer. SR-717 demonstrates broad interspecies and interallelic specificity. SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING. SR-717 displayed antitumor activity; promoted the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitated antigen cross-priming. SR-717 also induced the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner.

TDP1 Inhibitor-3 (Compound 4E) is a (TDP1) inhibitor with an IC50 value of 0.63 μM.

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).

H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively; H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.

Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.

MYC degrader 1 TFA (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, exhibiting significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors.

KT-333 diammonium is a molecular glue degrader that selectively targets STAT3 for proteasomal degradation by bridging interactions between STAT3 and the VHL E3 ubiquitin ligase complex. Exhibiting high specificity for STAT3 degradation, this compound demonstrates potent antitumor efficacy. Its therapeutic potential is particularly relevant in hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

Pomalidomide-d4 is a deuterium-labeled analog of pomalidomide, a third-generation immunomodulatory drug functioning as a molecular glue degrader. This compound selectively binds the cereblon E3 ubiquitin ligase complex, triggering targeted proteasomal degradation of Ikaros family transcription factors—a key mechanism underlying its therapeutic activity.