CRANAD-2 is a difluoroboron-derivatized curcumins as near-infrared probe for in vivo detection of amyloid-beta deposits. Upon interacting with Abeta aggregates, CRANAD-2 undergoes a range of changes, which include a 70-fold fluorescence intensity increase, a 90 nm blue shift (from 805 to 715 nm), and a large increase in quantum yield. Moreover, this probe also shows a high affinity for Abeta aggregates (K(d) = 38.0 nM), a reasonable log P value (log P = 3), considerable stability in serum, and a weak interaction with albumin. After intravenous injection of this probe, 19-month-old Tg2576 mice exhibited significantly higher relative signal than that of the control mice over the same period of time.

A286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

Epiblastin A is a Casein Kinase 1 (CK1) inhibitor. Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

EC23 is a fluorescent, voltage, indicator, action, potentials, mammalian, neurons, perturbations, cardiac, waveform, pluripotent, stem, cell-derived, cardiomyocytes

GNE-140 racemic is a novel potent lactate dehydrogenase (LDHA) inhibitor. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance.

SEMBL is a potent NF-κB inhibitor that inhibits DNA binding of NF-κB component p65.

VU0155094 is a potent, selective pan-Group III mGlu positive allosteric modulator with IC50 of 3.43/1.5/0.93 uM for mGlu8/7/4, respectively.

A specific inhibitor of MDA-9/Syntenin activity that inhibits MDA-9/Syntenin binding to EGFRvIII.

Selective 5-HT1B serotonin receptor antagonist

Novel potent and selective NADPH oxidase inhibitor, targeting Nox4 in TGFβ-induced lens epithelial to mesenchymal transition

PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.

Zidebactam, also known as WCK-5107, is a Beta lactamase inhibitor. Zidebactam is a novel Inhibitor of PBP2 Showing Potent "β-Lactam Enhancer" Activity against Pseudomonas aeruginosa, Including Multidrug-Resistant Metallo-β-Lactamase-Producing High-Risk Clones. Zidebactam demonstrated specific high-affinity binding to PBP2 of A. baumannii (0.01 μg/ml for both of the compounds). The MIC of zidebactam was >1,024 μg/ml for wild-type and multidrug-resistant Acinetobacter strains. Zidebactam is a PBP2 inhibitor that show a potent β-lactam enhancer effect against A. baumannii, including a multidrug-resistant OXA-23-producing ST2 international clone.

PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].

Supinoxin, also known as RX-5902, is orally bioavailable small molecule inhibitor of phosphorylated-p68 RNA helicase (P-p68), with potential anti-proliferative and antineoplastic activity. Upon oral administration, P-p68 inhibitor RX-5902 may both inhibit the activity of the anti-apoptotic B-cell lymphoma 2 (Bcl-2) protein and facilitate the induction of cyclin-dependent kinase inhibitor 1 (p21). This may prevent G2/M cell cycle progression and lead to growth inhibition in tumor cells. P-p68 is overexpressed in various types of solid tumors but absent in normal tissues, and plays a role in tumor progression and metastasis.

MKT-077 (FJ-776) is a highly water-soluble (>200 mg/ml) rhodacyanine dye that exhibits significant antitumor activity, binds to Hsp70 family member, mortalin (mot-2), and abrogates its interactions with p53.

GPR52-IN-43(CAY10786) is a novel GPR52 antagonist, reducing mHTT levels by targeting GPR52 and promoting survival of mouse primary striatal neurons, and also reducing HD-related phenotypes in HdhQ140.

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.

D-Luciferin sodium is heterocyclic light-emitting compound and natural ligand for luciferase used to detect cell activity. It requires ATP for its reaction, emitting a greenish-yellow luminescence at a peak wavelength of approximately 530 nm. The salt form of luciferin dissolves in water or other typical buffers.

M1001 is a novel allosteric agonist of hypoxia-inducible factor-2α subunit (hif-2α), significantly displacing pocket residue y281

ZZW-115 (ZZW115, ZZW 115) is a potent inhibitor of NUPR1 (Kd=2.1 uM), an intrinsically disordered protein (IDP) with an entirely disordered conformation.

Cell-permeable, irreversible inhibitor of caspase-3/CPP32; inhibits tumor cell apoptosis. Neuroprotective in rat hippocampus following seizures in vivo.

Z-IETD-FMK is a specific Caspase-8 inhibitor.

ICG amine, as a near-infrared fluorescent probe, binds to amino acid residues without condensing agents. ICG is a tricarbocyanine dye.

Ganaplacide (KAF156, GNF-156) is a novel antimalarial clinical candidate that shows blood schizonticidal activity with IC50 of 6-17.4 nM against P falciparum drug-sensitive and drug-resistant strains.

SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) is a potent activator of potassium channel with EC50 of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively.

Alexamorelin is a synthetic growth hormone (GH) secretagogue.

GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively).

BI 671800 is a potent, oral prostaglandin D2 receptor (CRTH2) antagonist for treatment of asthma..

HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively.