CSi12N3 is a bioorthogonally activatable ionizable lipid containing two cleavable silyl-ether-linked C12 tails and a dual-amine headgroup. Formulated as SiLNPs, it remains relatively silent before activation but undergoes Phe-BF3-triggered desilylation, nanoparticle destabilization, and accelerated cytosolic mRNA release. The reported formulation produced up to 44-fold higher mRNA expression than SM-102 LNPs in vitro, with an approximately 10-fold activation-to-silent ratio. In a B16-F10 melanoma model, CSi12N3-based SiLNPs delivering GDNT mRNA induced tumor-localized pyroptosis and inhibited tumor growth without detectable systemic toxicity in the reported study. CSi12N3 is therefore a promising preclinical research lipid for externally controlled, tumor-selective mRNA delivery.

LDN193189 (DM-3189) hydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

C6O2B2 is a cholesterol-conjugated cationic/ionizable lipid developed for ligand-free mRNA delivery to brain endothelial cells following intravenous administration. Its architecture combines a piperazine-containing polyamine core, four degradable ester-linked hydrophobic tails, and a covalently attached cholesterol moiety through a flexible five-carbon spacer. Among 51 newly synthesized cholesterol-based lipids, C6O2B2 produced the strongest brain luciferase expression. An optimized LNP formulation containing C6O2B2, DODAP, DSPC, and DMG-PEG enabled efficient functional mRNA expression throughout the cerebral vascular network, with preferential transfection of CD31-positive brain endothelial cells and minimal detectable neuronal or glial expression. The formulation preserved BBB integrity in Evans blue and contrast-enhanced MRI assessments. Mechanistic studies associated its activity with improved membrane fusion, enhanced endosomal escape, and ApoA-I enrichment in the protein corona. Delivery of IL-10 mRNA also reduced vascular leakage and inflammatory cytokines in a mouse model of acute neuroinflammation. C6O2B2 remains a preclinical research lipid requiring further pharmacokinetic and repeat-dose evaluation.

CY7 is an ionizable lipid engineered for localized pulmonary mRNA delivery. Its structure combines a cyclohexane-based core, a 4-dimethylaminopiperidine ionizable headgroup, two ester linkers, and four extended hydrophobic branches. In LNPs formulated with cholesterol, DSPC, and DMG-PEG, CY7 produced substantially higher local luciferase expression and lung-to-liver selectivity than SM-102 following intratracheal administration. CY7 LNPs also enhanced functional mRNA expression in pulmonary neutrophils, endothelial and epithelial cells, as well as dendritic and B cells in lung-draining lymph nodes. When used to deliver PcrV and OprF-I mRNAs, pulmonary CY7 LNP vaccination generated rapid antigen-independent innate protection followed by durable antigen-specific humoral, mucosal, and cellular immunity. In mouse models, it reduced bacterial burden and improved survival following challenge with laboratory and carbapenem-resistant Pseudomonas aeruginosa. CY7 remains a preclinical research lipid requiring further pharmacokinetic, repeat-dose, and translational safety evaluation.

VLX600 is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

Glimepiride impurity 1 is an impurity of Glimepiride (HY-B0104).

MEDICA16 is a GPR40 agonist. MEDICA 16 is a β,β'-dimethyl hexadecanedioic acid which exhibits hypolipidemic and antidiabetogenic effects in the rat.

ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.

CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.

Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), B

LDN193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

Altiratinib is a MET/TIE2/VEGFR2/TRK (A,B,C) kinase inhibitor in Phase 1 clinical development for the treatment of invasive solid tumors including glioblastoma.

HM-61713 (BI-1482694) is an orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

miR-21 inhibitor 12 (miR-21-IN-12) is a small molecule inhibitor of microRNA-21 expression and inhibit miR-21 transcription.miR-21-IN-12 inhibited transcription of the miR-21 gene resulting in significant reductions in primary and mature miR-21 levels.miR-21-IN-12 demonstrated cytotoxicity in a cervical cancer cell line via induction of apoptosis and was capable of reducing microtumor formation in a long-term clonogenic assay.miR-21-IN-12 shows some level of selectivity for miR-21 and is not a general miRNA pathway inhibitor.

PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.

JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.

NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

KM822 is avselective, noncompetitive modulator of human dopamine transporter (DAT) with IC50 3.7 μM, which shows 30 and 50 folds higher than for human norepinephrine transporter (hNET) and human serotonin transporter (SERT), respectively.