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.

CID 3117694 is a selective, non-competitive inhibitor of ADAM10 with IC50 of 1.1 uM, does not inhibit ADAM17.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.

Cagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake. Cagrilintide has the potential for the research of obesity.

Modified phospholipid products: it is to modify the amino group (primary amino group) -NH3 at the end of DSPE into NHS, COOH, N3, MAL, Thiol (SH), OPSS, FITC, FA, Biotin and other different active groups. Phospholipids DSPE belong to the lipid family of biopolymers. Phospholipids consist of two fatty acids, a glycerol unit, a phosphate group, and a polar molecule. The phosphate groups and polar head regions of the molecule are hydrophilic (attracted to water), while the fatty acid tail is hydrophobic (repelled by water). When placed in water, the phospholipids Orient themselves into a double layer, where the non-polar tail region faces the inner region of the double layer. The polar head region faces outward and interacts with the water.

Novel peptidomimetic antagonist of the PHF1 Tudor domain, binding both PHF1 Tudor domain and the related protein PHF19

MRT-6160 represents a groundbreaking molecular glue degrader designed to selectively target VAV1, achieving its proteasomal degradation with a DC50 value of 7 nM. This innovative compound showcases its unique mechanism and therapeutic potential.

CCI-38 is an effective YTHDF2 inhibitor with Kd of 10.1 μM. CCI-38 can suppress YTHDF2-mediated post-transcriptional regulation of target gene expression. CCI-38 also exhibits potent therapeutic efficacy and synergies with T cell-based immunotherapy in treating B cell malignancies.

DD-CIP2 is a DNA damage chemical inducer of proximity. DD-CIP2 demonstrates dramatically increased potency in SU-DHL-5 and MOLT-4 cells with EC50 of 0.78 nM and 4.6 nM, respectively. DD-CIP2 induces robust DNA damage and apoptosis in vitro and exhibits antitumor efficacy in vivo.

UDSP-Hep is a bacterial ADP-heptose analogue. UDSP-Hep is a potent ALPK1 agonist with EC50 of 0.0423 μM. UDSP-Hep distinguishs Alpk1 polymorphism and exhibits a stronger Alpk1-mediated antitumour effect and synergized with checkpoint inhibitors.

D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.