GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits premature atrial contractions.GS-680 significantly reduced CaMKII autophosphorylation.GS-680 inhibits pro-arrhythmic activity in human atrium and improves contractility in failing human ventricle.

FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively). FHP01 does not inhibit the ATPase activity of DDX3X and the helicase activity of DDX1 (IC50>100 uM). FHP01 also inhibited WNT signaling, a key tumorigenic pathway already correlated to DDX3X functions in breast cancer model cell lines. FHP01 inhibits ER+/PR+ (IC50 = 12.43 and 10.62 μM in MCF7 and T47D cells, respectively) and HER2+ (IC50 = 13.46 μM in SKBR3) cells, but lower in control MCF10A cells (IC50 = 28.71 μM). FHP01 (45 mg/kg, i.p. injection) suppresses rowth of MDA MB 231 tumor xenografts in nude mice.

TH6342 is a SAMHD1 inhibitor with IC50 of 9.1 μM/11.0 μM/5.8 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively. TH6342 engages pre-tetrameric SAMHD1 and deter oligomerization and allosteric activation without occupying nucleotide-binding pockets.

TH7127 is a SAMHD1 inhibitor with IC50 of 4.9 μM/4.5 μM/4.0 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively.

EP055 (EP-055) is a small molecule that targets EPPIN on the surface of sperm and inhibits motility (IC50=199.5 uM, CASA assay using human sperm), binds to the C-terminal domain of EPPIN.

AM-5308 is a potent and selective KIF18A inhibitor with demonstrated antitumor activity in cell-based and animal models. Its ability to disrupt mitosis and induce cancer cell death makes it a promising candidate for further development as a cancer therapeutic.

Novel potent broad-spectrum metallo-β-lactamase (MβL) inhibitor, inhibiting the MβLs NDM-1, VIM-2, ImiS, and L1

NCGC00161856 is identified as the first small-molecule ligand and inverse agonist of the thyroid-stimulating hormone receptor (TSHR). It inhibits basal cAMP production in HEK-EM 293 cells that stably express TSHRs, with a half-maximal inhibitory concentration (IC50) of 3.0 µM. This means that NCGC00161856 effectively reduces the constitutive activity of TSHR, which is the receptor's activity in the absence of its natural ligand (thyroid-stimulating hormone, TSH).

TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB.

ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice. ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs). ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β.

Precursor of Cholestify,18F-Cholestify, which binds cytochrome P450 46A1, detected cholesterol breakdown in the mammalian brain. CYP46A1 converts cholesterol to 24-hydroxycholesterol, a form easily eliminated from the brain.

PS-13 Precursor 19 is a critical intermediate in the synthesis of PS-13, a highly potent and selective COX-1 inhibitor. PS-13's exceptional selectivity for COX-1 over COX-2 makes it a promising compound for both therapeutic development and research applications focused on understanding COX-1-mediated processes.

SL25.1188 Precursor is a key intermediate in the synthesis of SL25.1188, a reversible and selective MAO-B radioligand. The radiolabeled form, [¹¹C]SL25.1188, is a promising PET imaging agent for studying MAO-B in the brain, with applications in neurodegenerative disease research and drug development. Its reversible binding and high selectivity make it a valuable tool for understanding MAO-B's role in health and disease.

3BP-3940 is a highly potent FAP-targeting peptide with significant potential in theranostics. Its ability to be coupled with diagnostic and therapeutic radionuclides makes it a versatile tool for tumor imaging, targeted therapy, and treatment monitoring. By focusing on the tumor stroma, 3BP-3940 offers a promising approach to improving cancer diagnosis and treatment, particularly for cancers with prominent stromal involvement. As research progresses, 3BP-3940 could play a key role in advancing precision oncology.

FAP-2286 is a highly promising FAP-targeting theranostic agent with potent affinity for FAP, versatile radionuclide coupling capabilities, and demonstrated antitumor activity. Its ability to serve as both a diagnostic imaging agent and a therapeutic tool makes it a valuable asset in oncology, particularly for cancers with prominent stromal involvement. As research progresses, FAP-2286 has the potential to significantly advance cancer diagnosis, treatment, and research, offering new hope for patients with FAP-expressing tumors.

SH-FAPI-4 is a specific fibroblast activation protein inhibitor (FAPI) compound that belongs to the FAPI family of molecules. SH-FAPI-4 is expected to selectively accumulate in FAP-positive tumors and disrupt the functions of cancer-associated fibroblasts (CAFs) within the tumor microenvironment. By inhibiting FAP activity, this compound aims to potentially slow tumor growth, enhance the efficacy of other cancer treatments, and modulate the tumor microenvironment.

NOTA-FAPI-46 is an analogue of FAPI-46 (MedKoo Cat#207189). NOTA-FAPI-46 is useful in the diagnosis or treatment of a disease characterized by overexpression of fibroblast activation protein (FAP). NOTA-FAPI-46 can be used as a PET tracer for detection of diseases or disorders related to fibroblast activation protein.

LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. LY3437943 can be used for the research of obesity.

Savirin (S. aureus virulence inhibitor) is a small molecule that targets the agr (accessory gene regulator) quorum sensing system in Staphylococcus aureus (S. aureus). The agr system is a key regulatory pathway that controls the expression of virulence factors in S. aureus, which are critical for its pathogenicity. The system involves a two-component signal transduction pathway consisting of AgrC (a histidine kinase) and AgrA (a response regulator).

UT-59 is a specific inhibitor that targets the cholesterol-sensing membrane protein Scap (SREBP cleavage-activating protein). It functions by binding to Scap's cholesterol-binding site, which prevents Scap from interacting with SREBPs (sterol regulatory element-binding proteins). This inhibition blocks the activation of SREBPs, which are key transcription factors involved in lipid and cholesterol biosynthesis. As a result, UT-59 effectively suppresses lipid synthesis, making it a potential therapeutic candidate for conditions associated with dysregulated lipid metabolism, such as hyperlipidemia, atherosclerosis, or metabolic disorders.

GLS-15 is a novel GalNAc-derived small molecule structure designed for siRNA delivery.

FL-1607, a novel Fam20C inhibitor, has shown remarkable anti-proliferative effects in triple-negative breast cancer (TNBC) cells. This compound induces apoptosis and significantly reduces the migration ability of MDA-MB-468 cells, underscoring its potential as a promising therapeutic agent for TNBC treatment.

Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.

E7090 (E 7090) is a highly potent and selective orally bioavailable inhibitor targeting FGFR1, FGFR2, and FGFR3, with IC50 values of 0.71 nM, 0.50 nM, and 1.2 nM, respectively. It exhibits significantly weaker inhibition of FGFR4, with an IC50 of 120 nM. This distinct selectivity profile positions E7090 as a promising therapeutic candidate for diseases driven by aberrant FGFR1-3 signaling, offering a targeted approach to inhibit these receptors while minimizing off-target effects on FGFR4. Its oral availability further enhances its potential as a convenient and effective treatment option for patients with FGFR-dependent conditions.

Azido-acetal linker is stable at physiological pH (7.4) but rapidly hydrolyzes in the acidic environment of endosomes useful as a fragment of lipid synthesis.

DPPE-MPEG(2000) is a PEGylated form of 1,2-dipalmitoyl-rac-glycero-3-PE (DPPE). It has been used in the synthesis of anionic liposomes for drug redistribution and toxicity prevention.