BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 81 nM. BAY-8400 shows synergistic activity of DNA-PK inhibition when combined with DNA damage inducing cancer therapy, like targeted alpha radiation.

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.

KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.

Quorum sensing modulator as a PqsR antagonist

SZU101 is a small molecule TLR7 agonist that directly activates, induces reporter activity (23-fold) in a TLR7-NF-kB reporter system expressed in HEK-293 cells TLR7 signalling.

TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.

Flagelin 22 TFA, a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.

3'-Methoxyapiin (Graveobioside B) is a flavone. 3'-Methoxyapiin can be found in Uraria crinite and celery.

SU-10994 is a novel VEGFR inhibitor.

SW-163D-AcLysValCit-PABC-DMAE is a Drug-Linker Conjugates for ADC which consists of a natural bis-intercalator, SW-163D, conjugated via an AcLysValCitPABC-DMAE linker.

Target Protein-binding moiety 6 hydrochloride is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

Adrenomedullin (AM) (1-52), human (TFA) affects cell proliferation and angiogenesis in cancer.

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

E3 Ligase Ligand-Linker Conjugates 23 (TFA) is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

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.

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

MCULE-3408819416|DC Chemicals

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.

Sortin3 is a sorting inhibitor, blocking Vps16 function, one protein in the class C tethering complex, and increasing aflatoxin synthesis and export.

GD20 is a cell-permeable, nucleotide-inactive-state-selective inhibitor of Gαs, with high selectivity over other G protein subfamilies. GD20 inhibits Gαs steady-state GTPase activity with IC50 of 1.15 μM.

(R)-70 is a 5-HT2AR partial agonists with EC50 of 110 nM, and shows 6.4-fold/51-fold selectivity over 5HT2BR/5HT2CR. (R)-70 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

(R)-69 is a 5-HT2AR partial agonists with EC50 of 41 nM, and shows 4.6-fold/29-fold selectivity over 5HT2BR/5HT2CR. (R)-69 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

PL-SNS-032 conjugate 955 can potently degrade CDK9 in a ubiquitin-proteasome-dependent manner and is much more potent than SNS-032 against various tumor cells in vitro.

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.