ZINC 39395747 is a novel potent derivative of propylthiouracil that functions as a cell-active inhibitor of cytochrome b5 reductase 3 (CYB5R3) with IC50 of 9.14 uM.

Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand, demonstrates the neuroprotective effects against 10 0M Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture.

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

NC-001 (NC 001, NC001, az-NC-001) is a potent, specific, cell-permeable inhibitor of immunoproteasome caspase-like sites (β1i and β1), does not correlate with inhibition of chymotrypsin-like sites..

GCPII-IN-1 TFA is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM.

VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation.

USP10-IN-3 is a HBX19818 analog, potent and selective USP10 inhibitor, but does not inhibit USP7 (IC50>100 uM).

GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media.

Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM.

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]

DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.

TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.

Specific inhibitor of vaccinia-related kinase 1 (VRK1)-mediated phosphorylation of barrier-to-autointegration factor (BAF)

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro.

BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.

A novel, second-generation C-terminal Hsp90 inhibitor with Kd of 191 and 726 uM for Hsp90α and Hsp90β, respectively.

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).

SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.

TP-1454 is an activator of PKM2 with AC50 of 10 Nm in biochemical assays.TP-1454 modulates tumor-immune responses by destabilizing T-regulatory cells.

Novel Enrichable and MS-Cleavable Cross-linker to Define Protein-Protein Interactions by Mass Spectrometry

Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis.

YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).

FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.

Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.

Blue fluorescent amino acid, exhibiting blue fluorescence (λ max ~ 405 nm) with a high quantum yield and long lifetime

RO6806051 (compound12) is a potent dual fatty acid binding protein 4 and 5 (FABP4 and FABP5) inhibitor with good selectivity and absorption, distribution, metabolism and excretion (eADME) properties.

Aurachin D is an antibiotic. Aurachin D inhibits Gram-positive bacteria and a few funguses. Aurachin D blocks NADH oxidation in beef heart submitochondrial particles.