Mps1-IN-3 is a selective and highly potent Mps1 kinase inhibitor with IC50 of 50 nM.

Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.

VK-II-36, a structural analog of carvedilol, selectively suppresses sarcoplasmic reticulum Ca²⁺ release without exhibiting β-receptor blocking activity. It effectively inhibits both early and delayed afterdepolarizations, thereby preventing triggered arrhythmias. This unique pharmacological profile makes VK-II-36 a promising candidate for antiarrhythmic therapy.

Galloflavin is a strong inhibitor of lactate dehydrogenase (LDH), effectively targeting both LDH-A and LDH-B isoforms with calculated inhibitory constants (Ki) of 5.46 μM and 15.06 μM, respectively, for pyruvate. By disrupting LDH activity, galloflavin suppresses glycolysis and reduces ATP generation, leading to the inhibition of cancer cell proliferation. This mechanism highlights its potential as an anticancer agent targeting metabolic pathways.

A small molecule that promotes differentiation of iPS-derived hepatocytes.

Fluxapyroxad is a broad-spectrum fungicide which inhibits the succinate dehydrogenase (SQR) enzyme.

ALLM (Calpain Inhibitor) is cell-permeable, peptide aldehyde inhibitor of calpains and cathepsins.

Pal-GHK is a form of the extracellular matrix-derived peptide GHK containing palmitic acid, which allows it to penetrate the stratum corneum to the epidermal and dermal skin layers. Pal-GHK increases collagen synthesis in skin fibroblasts. It has been used with the zwitterionic surfactant C12 dodecyldimethylamine oxide (C12DMAO) to study self-assembly of the mixture into aggregates, ribbons, and nanobelts. Pal-GHK has also been used as an internal standard for the quantification of pal-KTTKS in anti-wrinkle creams by LC-MS/MS

TAE-1 is a AChE inhibitor. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme).

AV-412, also known as MP-412, is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization.

ATF3W-aeg peptide is a selective, peptide inhibitor of activating transcription factor 3 (ATF3) with high affinity (Kd=151 nM), increases CCL4 expression levels in human macrophages.

SM1-71 (Compound 5) is a highly effective TAK1 inhibitor, exhibiting a Ki value of 160 nM. Beyond its primary target, this compound demonstrates covalent inhibitory activity against a broad spectrum of kinases, including MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1, and RSK2. Due to its multi-kinase inhibitory profile, SM1-71 effectively suppresses the proliferation of various cancer cell lines, highlighting its potential as a promising therapeutic agent.

​​COE2-2hexyl​​ represents an innovative class of antimicrobial agents, demonstrating broad-spectrum antibacterial activity through its unique conjugated oligoelectrolyte (COE) structure.

XL177A is a potent USP7 inhibitor. XL177A irreversibly inhibits USP7 with sub-nM potency and selectivity across the human proteome. Evaluation of the cellular effects of XL177A reveals that selective USP7 inhibition suppresses cancer cell growth predominantly through a p53-dependent mechanism: XL177A specifically upregulates p53 transcriptional targets transcriptome-wide, hotspot mutations in TP53 but not any other genes predict response to XL177A across a panel of ~500 cancer cell lines, and TP53 knockout rescues XL177A-mediated growth suppression of TP53 wild-type (WT) cells.

SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively.

Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload.

LDC203974(IMT1B) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT) with improved pharmacokinetic profiles than LDC195943(IMT1).

​​RBC1HI​​ represents a breakthrough in epigenetic modulation for opioid withdrawal management, demonstrating dual pharmacological activity as a selective HDAC1/HDAC2 inhibitor with neuroprotective properties.

AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.

AZD4604 (AZD-4604) is a potent, selective Janus-associated kinase 1 (JAK1) inhibitor with anti-inflammatory effect.

​​BRD4884​​ is a novel histone deacetylase (HDAC) inhibitor demonstrating selective class I HDAC inhibition with nanomolar potency.

​​BGC-20-1531 (PGN 1531)​​ is a novel benzenesulfonamide-based compound that functions as a selective prostaglandin E2 receptor EP4 subtype antagonist.

​​Jarin-1​​ represents a breakthrough in plant hormone modulation as the pioneering small-molecule inhibitor of jasmonoyl-L-isoleucine synthetase (JAR1).

​​MEK-IN-4​​ is a novel small-molecule inhibitor targeting the MAPK/ERK kinase (MEK) pathway with therapeutic potential across multiple disease areas.

​​Dafadine-A​​ represents a novel class of cytochrome P450 inhibitors with unique species-specific activity.

​​JNJ-5207787​​ represents a breakthrough in neuropeptide Y receptor modulation as a brain-penetrant, selective Y2 receptor antagonist.

​​TI17​​ represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.

​​B355252​​ is a novel neuroprotective compound that demonstrates dual mechanisms of action to support neuronal survival and regeneration.

​​MK-0343 (MRK-409)​​ represents a novel class of benzodiazepine-site ligands with unique GABAA receptor subtype selectivity.

​​NIAD-4​​ is an advanced fluorescent probe specifically engineered for high-contrast imaging of amyloid-β (Aβ) aggregates in Alzheimer's disease research.