A novel dual inhibitor of mTOR and DNA-PK with IC50 of 21 nM and 13 nM, respectively.

HZS60 is a NMDAR/TRPM4 inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke.

NSC 31152 is an antimicrobial agent, with MIC values of 18.7-21.0 µg/mL for S. aureus, S. epidermidis, E. coli, P. aeruginosa, A. niger, and A. fumigatus.

TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology.

GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM .

alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.

PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.

PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.

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.

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].