N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue to promote glucose uptake with an EC50 value of 7.00 μM.

PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.

MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.

MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

PLK1-IN-2 is a PLK1 kinase inhibitor with an IC50 value of 0.384 μM.

Propargyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool for exploring the PRMT5 functions in health and disease.

SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.

PKM2-IN-3 is a inhibitor of PKM2 kinase with IC50 value of 4.1μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.

RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C.

RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively.

KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities.

KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.

N-Acetyl-L-cysteine ethyl ester is an esterified form of N-acetyl-L-cysteine (NAC). N-Acetyl-L-cysteine ethyl ester exhibits enhanced cell permeability, and produce NAC and cysteine. N-Acetyl-L-cysteine ethyl ester increases circulating hydrogen sulfide (H2S) and can be used as an H2S producer. N-Acetyl-L-cysteine ethyl ester has the potential to substitute NAC as a mucolytic agent, and as a GSH-related antioxidant.

RSK4-IN-1 is identified with potent RSK4 inhibitory activity with an IC50 value of 9.5 nM.

RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.

RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.

SARS-CoV-2-IN-8 is a SARS-CoV-2 main protease inhibitor with an IC50 value of 0.75 μM.

SARS-CoV-2-IN-6 is a SARS-CoV-2 3CLpro inhibitor that shows the most potent enzyme inhibitory IC50 value of 73 nM.

SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.

NK007 is a novel anti-SARS-CoV-2 agent with an EC50 value of 30 nM.

SARS-CoV-2-IN-9 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease.

PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC50 value of 7.57 μM.

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).

TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.