GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.

HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM.

Irreversible inhibitor of amiloride-sensitive Na channels; derivative of amiloride

T62 is an allosteric enhancer of A1 adenosine receptor.

Nrf2 acticatior AI-2 is a small-molecule inducer of the antioxidant response element (ARE) that activates and stabilizes Nrf2 by covalently modifying Keap1.

Defibrotide sodium is a complex mixture of single stranded polydeoxyribonucleotides. Defibrotide sodium has liver protection, anti-inflammatory, antithrombotic, profibrinolytic, and anti-ischemic properties. Defibrotide sodium can be used for sinusoidal obstruction syndrome (SOS)/veno-occlusive disease (VOD) research.

K161 is a potent, pan-SHIP1/2 inhibitor with IC50 of 1.5- 6 uM and 6.5-13 uM, respectively.

CK147 (CK-147) is a potent CD4 down-modulator with IC50 of 63 nM, inhibits Sec61-dependent cotranslational translocation of huCD4 in vitro.

2-Deoxy-2-fluoro-L-fucose, an L-fucose analog, is a fucosylation inhibitor. 2-Deoxy-2-fluoro-L-fucose inhibits de novo synthesis of GDP-fucose in mammalian cells. Fucosylation is a relatively well-defined biomarker for progression in many human cancers; for example, pancreatic and hepatocellular carcinoma.

Tiafenacil is a new protoporphyrinogen IX oxidase (PPO)-inhibiting herbicide, with IC50 values of 22 to 28 nM for various plant species, including amaranth (Amaranthus tuberculatus), soybean (Glycine max), arabidopsis (Arabidopsis thaliana), and rapeseed (Brassica napus).

LY3202626 is a small molecule non-selective BACE1 inhibitor, causes dose-dependent reductions in CSF and plasma Aβ concentrations, shows potential for the treatment of Alzheimer's disease..

Nalfurafine (TRK-820, TRK820) is potent, selective agonist of kappa-opioid receptor with Ki of 3.5 nM, 15-fold less potent for μOR and little affinity for δOR (Ki=53 and 1,200 nM, respectively).It is for research use only, and the end user must be the universities.

Fraisinib is a specific and effective inhibitor of glycyl-tRNA synthetase 1 (GARS1), suppresses the synthesis of Ap4A by GARS1 and displays strong anti-tumoral potential.

SPI-21 (Spt5-Pol II inhibitor 21) is a small-molecule inhibitor of Spt5-Pol II with IC50 of 25.2 uM.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is an oral Polo-like kinase 1 (PLK1) inhibitor, a key regulator of cell cycle progression and mitosis. It selectively inhibits PLK1 with a reported half-maximal inhibitory concentration (IC₅₀) of approximately 2 nM, while demonstrating significantly lower activity against other Polo-like kinases (PLK2 and PLK3). Onvansertib has shown potent anti-proliferative effects in various cancer cell lines, particularly in colorectal cancer, acute myeloid leukemia (AML), and prostate cancer models. It induces mitotic arrest, leading to apoptosis in tumor cells. Onvansertib has demonstrated synergistic effects when combined with chemotherapeutics such as irinotecan, 5-fluorouracil (5-FU), and decitabine, enhancing their efficacy in resistant cancers.

Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).

S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively.

F1957-0088 is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (TTD vs. H3K9me3) EC50 of 45.1 uM.

ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A.

Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.

Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].

LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.

KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.

NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.NADI-351 inhibited OE33 cell growth in single dose MTT assays (EC50= 10 uM) and, more potently, in multi-dose colony formation assays (EC50=1.3 uM)NADI-351 is 15 times more potent than IMR-1 in an NTC AlphaScreen assay.NADI-351 selectively disrupted Notch1 transcription complexes, inhibited recruitment of Notch1 to the NTC (Notch Ternary Complex) and to the HES1 promoter, and reduced Notch1 recruitment to target genes.NADI-351 inhibits tumor growth in Notch-dependent cancers and does not exert gastrointestinal toxicity associated with goblet cell metaplasia.NADI-351 selectively inhibits stem-like esophageal adenocarcinoma (EAC) cell populations.

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

Pyrcoumin is a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1, IC50=3.3 uM), inhibits Wnt signaling with IC50 of 8.4 uM in SuperTOPFlash reporter gene assays.

A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3).