small-molecule

BI-1935 is an inhibitor of soluble epoxide hydrolase (sEH). For diseases related to cardiovascular disease.

SPHINX is a new generation inhibitor of SPRK1

A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells.

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

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)

Sacituzumab (hRS7) is an antibody inhibitor and a humanized monoclonal antibody targeting trophoblast cell surface antigen 2 (TROP2), serving as a component of the antibody-drug conjugate sacituzumab govitecan, used for research and treatment of TROP2-high-expressing tumors such as triple-negative breast cancer.

Azelaprag (AMG 986) is an oral apelin receptor agonist (EC50 = 0.32 nM). Azelaprag may be used to treat neurological disorders, cardiovascular diseases, and obesity with metabolic syndrome.

Niclosamide is a classic salicylanilide antiparasitic drug and a multi-target, low-toxicity, broad-spectrum small-molecule modulator with anthelmintic and antitumor activity. Niclosamide disrupts the parasite’s energy metabolism by uncoupling mitochondrial oxidative phosphorylation, leading to reduced ATP production and ultimately killing the parasite. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells.

A2B receptor antagonist 1 is a small molecule antagonist and an A2B adenosine receptor antagonist with potent antagonistic activity, and can be used for research on adenosine receptor-related diseases.

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

Candoxatril (UK 79300) is a small-molecule inhibitor and a neutral endopeptidase (NEP) inhibitor with oral activity and cell permeability, used for the treatment of chronic heart failure and capable of improving exercise capacity in patients receiving angiotensin-converting enzyme inhibitor therapy.

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].

Clozic (ICI 55897) is a small molecule anti-arthritis candidate that exerts anti-inflammatory effects by reversibly inhibiting excessive proliferation of synovial cells, and can be used for mechanistic studies of rheumatoid arthritis and related inflammatory diseases.

CNS-5161 hydrochloride (CNS 5161A) is a small molecule antagonist and an NMDA receptor antagonist that selectively and non-competitively blocks the action of glutamate, and can be used for research on neurological diseases.

LTB4-IN-1 (Anti-inflammatory agent 2, Compound 6) belongs to small molecule inhibitors and is a leukotriene B4 (LTB4) synthesis inhibitor (IC50 = 70 nM) with good anti-inflammatory activity. This compound can be used in experimental research on inflammation-related diseases.

Ecastolol is a small molecule inhibitor, a β-adrenergic receptor antagonist that exerts its pharmacological effect by blocking catecholamine-induced agonism of this receptor, with anti-anginal properties, used for cardiovascular disease research.

Orforglipron (LY3502970) belongs to non-peptide small molecule GLP-1 receptor agonists and is a highly selective, orally effective GLP-1 receptor agonist with good cell permeability and oral bioavailability. This compound is used in research on type 2 diabetes and obesity, demonstrating significant glucose-lowering and weight-reducing activities.

Pentiapine (CGS 10746) is a small-molecule inhibitor and a dopamine release inhibitor with cell permeability, used in neuropharmacological research to modulate dopaminergic signaling, holding significant application value in studies related to nervous system mechanisms.

5-HT2 antagonist 1 is a small molecule antagonist functioning as a 5-HT2B receptor antagonist (IC50 = 33.4 nM), with oral bioactivity and weak inhibition of α1 receptors, employed in research on hepatocellular carcinoma and related diseases.

MIK665 (S-64315) is a small-molecule inhibitor and a myeloid cell leukemia sequence 1 (MCL1) inhibitor (IC50 = 1.81 nM) with high selectivity and cell permeability. Used in experimental research, this compound exhibits antitumor activity in hematologic malignancies such as acute myeloid leukemia.

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.

Ziresovir (RO-0529/AK0529) belongs to small molecule inhibitors and is a respiratory syncytial virus (RSV) fusion protein (F protein) inhibitor (EC50 = 3 nM) with oral activity and selectivity. This compound is used in research on respiratory syncytial virus infection, significantly alleviating bronchitis symptoms and reducing viral load.

ZT 52656A hydrochloride belongs to synthetic small molecule compounds and is a highly selective kappa opioid receptor (KOR) agonist with good receptor selectivity and potential peripheral action characteristics. This compound effectively prevents or significantly alleviates ocular pain through KOR activation, and can be used in pain-related mechanism research.