RX-3117 is an orally available and potent DNA synthesis inhibitor with potential antineoplastic activity.

4'-bromo-resveratrol, a brominated analog of resveratrol, shows significant anticancer properties through its unique capacity to inhibit SIRT1 and SIRT3 simultaneously. In melanoma models, it alters cellular metabolism by targeting mitochondrial function, leading to cell cycle arrest and induction of programmed cell death. This multimodal mechanism suggests potential applications in overcoming treatment resistance.

5F-203 (NSC-703786) exhibits its anticancer properties through a multimodal mechanism of action. As a DNA-damaging agent, it creates stable adducts while arresting cell cycle progression. The compound's ability to strongly activate AhR signaling results in marked CYP1A1 induction. Additional effects include ROS generation and concurrent activation of multiple stress-responsive kinase pathways (JNK, ERK, and p38), collectively contributing to its cytotoxic profile.

OS-3-106 represents a blood-brain barrier permeable compound demonstrating exceptional selectivity and potency as a dopamine D3 receptor (D3R) agonist. With an impressive binding affinity of Ki = 0.2 nM for D3R, this compound shows particular promise for investigating potential therapeutic interventions in psychoactive substance addiction disorders. Its unique pharmacological profile makes it a valuable research tool for studying reward system modulation.

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

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.

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.

ML303 is an antagonist of pyrazolopyridine influenza virus nonstructural protein 1 (NS1) (IC90 : 155 nM).

Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 µM.

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.

K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.

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

BRINP2-related peptide (BRP) is a 12-mer peptide, as a potent anorexigenic peptide. BRP demonstrates significant appetite-suppressing effects in mice and pigs, and triggers FOS activation in the hypothalamus.

Disodium (R)-2-Hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.

CA-170, also known as AUPM170 and PD-1-IN-17, is a programmed cell death-1 (PD-1) inhibitor. PD-1-IN-17 was first reported in patent WO2015033301A1, (Compound 4), inhibits 92% splenocyte proliferation at 100 nM.

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.

Ac-LETD-AFC is a caspase-8 fluorogenic substrate. Ac-LETD-AFC can measure caspase-8 fluorogenic activity and can be used for the research of cancer cell apoptosis and oxidative stress metabolism.

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.

Highly potent cytotoxic microtubule inhibitor

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.