small-molecule

Azelaprag (AMG 986) is an effective small-molecule apelin receptor agonist. Azelaprag can be used to treat neurological diseases and cardiovascular diseases.

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.

C16 Ceramide (Palmitoyl Ceramide) is a naturally occurring small molecule that activates p53 by directly and selectively binding to it.

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.

C004019 is a small molecule PROTAC capable of targeting tau for selective protein degradation from the cell, while recruiting tau and E3 ligase (Vhl) for selective enhancement of tau ubiquitination and proteollyzation. C004019 is a candidate for AD and related tau protein diseases.

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.

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].

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.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular system.

RH01386 is a small molecule that prevents ER stress-induced β cell dysfunction and death, inhibits proapoptotic gene expression, and restores ER stress-impaired glucose-stimulated insulin secretion responses, showing potential for type 2 diabetes treatment.

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.