HHS-475 is a novel sulfur-triazole exchange (SuTEx) covalent probe with ~5-fold enhanced chemoselectivity for tyrosines over other nucleophilic amino acids.

GalNac-L96, the G-rich oligonucleotides carrying the longer GalNAc linker that can be used for delivery of nucleic acid drugs[1].

LS-170 is a potent, selective and cell-active chemical inhibitor that targets the ATAC-specific YEATS2 YEATS domain with IC50 of 0.14 μM. LS-170 specifically reduces the chromatin occupancy of the ATAC complex, decreases the ATAC-dependent histone acetylation level and downregulates the expression of ATAC-governed genes, leading to significantly suppressed tumor growth in a lung cancer mouse model.

Compound 78 is a molecular glue for the unique composite surface of the 14-3-3/C-RAF259 complex. Compound 78 results in 210-fold stabilization of the 14-3-3σ/C-RAF259 complex in fluorescence anisotropy assays and has an EC50 of 1.2 μM in a cellular 14-3-3/C-RAF NanoBRET assay. Compound 78 shows greater selectivity for C-RAF in the NanoBRET assay and the protection of phosphorylation.

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

AMG1556 is a biodegradable, cyclic amino alcohol-based ionizable lipid from the AMG series, designed specifically for mRNA delivery via lipid nanoparticles (LNPs).

ATN-224 is a choline salt of tetrathiomolybdate and an inhibitor of superoxide dismutase 1 (SOD1; IC50s = 2.91 and 3.51 µM in human and mouse blood cells, respectively, in vitro).

The trivalent β-GalNAc ligand is specific for Asialo Glycoprotein Receptors (ASGPR) on hepatocyte cells. β-Ala-PEG3 acts as linker/spacer between triantennary GalNAc and Fluorescein isothiocyanate (FITC).

Tris-GalNAc-GABA-NH2 linked via PEG2k to phospholipid (DSPE or 1,2-distearoyl-sn-glycero-3-phosphoethanolamine) where GABA = gamma-Aminobutyric acid, or γ-aminobutyric acid.

Trivalent β-GalNAc Ligand with discrete, monodisperse, azido-functionalized PEG3 linker/spacer

Tris-GalNAc ligands bind to Ashwell-Morell (also Asialoglycoprotein receptor or ASGPR) receptors and are validated ligands in medicinal chemistry for liver-specific drug delivery.

The trivalent β-GalNAc Ligand is specific for Asialo Glycoprotein Receptors on hepatocyte cells. β-Alanine-PEG3 acts as linker/spacer between multivalent GalNAc and biotin.

HY-501​​ is a next-generation cationically ionizable lipid engineered for high-efficiency RNA delivery developed by Biontech. Formulated at ​​40–50 mol%​​ in lipid nanoparticles (LNPs) alongside DSPC, cholesterol, and polysarcosine-conjugated lipid ​​C14pSar23​​, HY-501 yields uniform, stable particles (80–100 nm) with >90% RNA encapsulation. It demonstrates ​​superior in vivo performance​​: driving 2-fold higher protein expression than benchmark lipids (EA-405/HY-405) in muscle tissue, minimizing off-target liver accumulation, and reducing immunogenic risks (near-zero complement activation and <5% hemolysis). Preclinically, HY-501-based LNPs encoding SARS-CoV-2 spike protein elicit potent neutralizing antibodies and T-cell responses, underscoring its utility in precision vaccines. Its combination of scalable synthesis, exceptional transfection efficiency, and biosafety establishes HY-501 as a transformative vector for therapeutic RNA delivery.

LIPID 14 is a novel ionizable lipid used for mRNA delivery.In 2021, Elia et al. used lipid 2 LNPs and lipid 14 LNPs to deliver mRNA encoding SARSCoV-2 human Fc-conjugated receptor binding domain (RBDhFc mRNA). While both lipid 274 LNP RBD-hFc mRNA and lipid 14 LNP RBD-hFc mRNA induced equal cellular and humoral responses in mice at an mRNA dose of 5 μg, only lipid 14 LNP RBD-hFc mRNA exhibited strong immunogenicity following intradermal administration. Both intradermal administration and intramuscular administration of lipid 14 LNPs could activate antigen presenting cells (APCs), thus inducing cellular responses.

(±)-H3RESCA-TFP ((±)-H3L28) is a tetrafluorophenyl ester derivative of restrained complexing agent (RESCA). (±)-H3RESCA-TFP can be used to conjugate the chelator with a biomolecule via amine coupling (e.g., N terminus and/or the ε-amino groups of lysine).

FAS-IN-1 is a potent inhibitor of fatty acid synthase (FAS) wtih IC50 of 10 nM..

GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.

LX-1031 is a potent, orally active tryptophan 5-hydroxylase (TPH) inhibitor with potency of 10-100 nM, reduces 5-HT synthesis peripherally.

IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk with an IC50 of 0.5 nM.

NV914 is a small molecule inhibitor of tRNA-specific 2′-O-methyltransferase (FTSJ1), exerts readthrough activity in vitro and in vivo.

NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.

S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.

ALC-0159 (di-C18) is an analog of ALC-0159, in which the original C14 chain is replaced with C18 chain. C18-ALC-0159 demonstrates high stability in vivo, effectively prevents binding with proteins such as ApoE, and achieves a prolonged blood circulation time. It also reduces liver targeting and accumulation.

CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.AK-42 binds to an extracellular vestibule above the channel pore. AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.AK-42 is a powerful tool for investigating CLC-2 neurophysiology.

​​BMS-986463​​ is a novel, first-in-class targeted protein degrader designed to specifically eliminate WEE1 kinase, a master regulator of cell cycle progression.

Aminoxyrone is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM; destabilizes BCR-ABL1 without inducing HSR in vitro and in vivo, additionally reduces pAKT-S473, pS6 expression and expression of client proteins associated with HSP90 chaperone activity, involving t-AKT, t-STAT5a, t-CRKL, cMYC, and BCL2; triggers the degradation of HSP90 client proteins without elevating the expression of HSPs (HSP70, HSP40 & HSP27); significantly inhibits cell growth and induces apoptosis of human leukemic stem cells (LSCs) with average EC50 of 20.94 uM, Aminoxyrone is effective in imatinib resistant CML and lacks heat shock response.

LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM,. Phase 3.

GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.