CPI-455 analogue is a selective inhibitor of KDM5 demethylases.

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

Elacestrant S enantiomer is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

FAS-IN-1 tosylate is a potent inhibitor of fatty acid synthase (FAS) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.

HS-10 is a novel Hsp90 inhibitor increases the Tm of Hsp90 by 10.5°C.

Novel potent inhibitor of Proprotein convertase subtilisin/kexin 9 (PCSK9), targeting the PCSK9/LDLR protein-protein interaction

Jun8-76-3A is a potent and selective noncovalent SARS-CoV-2 Mpro inhibitor with Ki of 0.07 μM. Jun8-76-3A only selectively inhibits SARS-CoV-2 and SARS-CoV Mpro, but not other viral proteases and host proteases including calpain 1, cathepsins L and K, and trypsin.

5,3-AB-CHMFUPPYCA is an analytical reference standard that is structurally classified as a synthetic cannabinoid.

Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.

CPI-169 R is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2.

SRX 3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.SRX3305 showed enhanced binding to the drug-resistant C481S mutant of BTK compared to SRX-3262 (IC50=9 uM and 25 uM, respectively).SRX3305 displayed cytotoxicity aginst MCL cell lines JeKo-1, Mino, Granta with IC50 of 58 nM, 1 nM, 1.1 uM, respectively.SRX3305 inhibited cell vbiability of JeKo-1 BTK C481S and Mino BTK C481S mutant cell lines with IC50 of 1 uM and 47 nM, respectively, with minimally toxic to healthy donor PBMCs.SRX3305 showed improved efficacy in MCL and Ibrutinib-resistant MCL cells, SRX3305 impacted gene expression, perturbs the cell cycle and promotes apoptosis in MCL.

PRL295 is a small molecule Keap1-Nrf2 protein–protein interaction inhibitor.PRL295 binds to Keap1 in the cellular environment, disrupting its interaction with Nrf2, which leads to enhanced gene expression of the classical Nrf2 target NQO1 in cells and in vivo in the mouse liver.PRL-295 increases the thermostability of Keap1 in cell lysates and in live cells.PRL 295 decreased the levels of plasma alanine aminotransferase and aspartate aminotransferase upon acetaminophen-induced hepatic injury.

UHRF1 PHD inhibitor MLD4 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=12.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD4 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells.

NJH-2-075 is an alkyne-functionalized probe of EN523, retains binding to OTUB1 in vitro.

UHRF1 PHD inhibitor MLD5 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=7.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD5 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells.

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.

KMN-159 is a potent prostaglandin E2 type 4 (EP4) receptor agonist with Ki of 0.38 nM and shows five fold increase in potency versus KMN-80.

VU6003586 is a novel allosteric modulators of mGlu5 with EC50 of 174 nM.

DS54360155 is an orally potent analgesic without μ-opioid receptor agonist activity.

N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible allosteric activity, which could be competitively inhibited by GHSR1a antagonists YIL781 and JMV2959.N8279 is a weak activator of GHSR1a-mediated, βarr2-dependent cellular responses relative to ghrelin.N8279 requires receptor sites and/or conformational states driven by the GHSR1a ECD that are distinct from ghrelin.N8279 is brain-penetrant and attenuates aberrant DAergic behavior in mice.

SMN2 splicing modulator TEC-1 is a novel specific, CNS penetrant small molecule SMN2 splicing modulator, increases the expression level of FL-SMN2 mRNA and decreases the expression level of Δ7 mRNA.TEC-1 showed higher selectively (>60-fold) on galactosylceramidase and huntingtin gene expression compared to previously reported compounds (e.g., SMN-C3) due to off-target effects on cryptic exon inclusion and nonsense-mediated mRNA decay.TEC-1 modulates SMN2 splicing and displays disease-modifying effects in motor neurons derived from SMA patient iPSCs (GM24468).|TEC-1 rescues the phenotype in a murine model of spinal muscular atrophy (SMA).

DX314 is a potent, specific CYP26B1 inhibitor with IC50 of 108 nM, >15-fold selectivity over CYP26A1.DX314 potentiates all-trans-RA (atRA) gene expression effects in healthy and diseased reconstructed human epidermis (RHE).DX314 potentiates the effects of atRA on the expression and localization of keratin 10 (KRT10), protects barrier function in RHE.DX314 reduces comedonal number, induces epidermal thickening, and increases comedonal profile, while having no effect on transepidermal water loss (TEWL) in treated rhino mice.

DX-308 is a potent, selective dual CYP26A1/B1 inhibitor and retinoic acid metabolism blocking agent.DX308 does not interact with off‐target nuclear receptors or CYP450s, is not genotoxic, and is stable in skin, despite vigorous hepatic metabolism.Topical DX308 induces comedolysis and epidermal thickening without apparent adverse effects in vivo.DX308 shows potent modulation of retinoid‐responsive genes by DX308 in both healthy and keratinization disorder keratinocytes (KCs).DX 308 may present an improved therapeutic alternative for the treatment of keratinization disorders and other retinoid‐responsive skin ailments.

BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.

AEP07 (AEP 07) is a selective small molecule inhibitor of PARP4 (vPARP) inhibitor with IC50 of 0.8 uM, >12-fold selective over other PARP family members.

Rv1625c agonist V-59 (V-59) is a specific small molecule agonist of the Mtb adenylyl cyclase Rv1625c, inhibits Mtb growth in macrophages (EC50=0.3 uM) in an Rv1625c-dependent mechanism.V-59 inhibits Mtb growth in cholesterol media (EC50 0.70 uM), but not in media containing the two-carbon fatty acid acetate, or in standard rich growth media.V-59 stimulates Rv1625c to produce cAMP, which is necessary for V-59 to inhibit Mtb growth.Chemically activating Rv1625c via V-59 preferentially inhibits cholesterol utilization in WT Mtb, rather than equally inhibiting all lipid utilization by the bacterium.

Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer.

SLLK, Control Peptide for TSP1 Inhibitor (TFA) is a control peptide for LSKL, which is a Thrombospondin (TSP-1) inhibitor.

(-)-CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 13.5 uM.

A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae.