small molecule

GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration

Azelaprag (Example 263.0) is a candidate active molecule (EC50= 0.32 nM) for an apelin receptor agonist. Azelaprag can be used to treat nervous system diseases, cardiovascular diseases.

CB-6644 is a small molecule inhibitor of the ATPase activity of the RUVBL1 2 complex. It specifically interacts with RUVBL1 2 in cancer cells and blocks the ATPase activity of RUVBL1 2 with a half-maximal inhibitory concentration (IC50) of 15 nM[1].

VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.

Petesicatib (RG 7625) is a small molecule histone-S (Cat-S) inhibitor for the study of primary dry syndrome and autoimmune diseases.

Risdiplam (RG7916) is a centrally and peripherally distributed and orally administrable small molecule SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

Sacituzumab is a humanized IgG1 monoclonal antibody utilized in the synthesis of antibody-active small-molecule couplings (naked antibody to Sacituzumab govitecan). It exhibits potential antitumor activity and is employed in tumor research.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

AZD0780 (EX-A6975) is an oral small molecule PCSK9 inhibitor being developed by AstraZeneca as a first-in-class treatment for patients with dyslipidemia that is uncontrolled with statins alone.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation.

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R/T790M mutant non-small cell lung cancer.

Alpertine HCl is a small molecule compound with anti-neuropathic properties.

AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

Complement C5-IN-1 is a small-molecule inhibitor of complement component 5 protein (C5).

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.