Diprotin A is a tripeptide inhibitor of dipeptidyl peptidase 4

Teglicar, in vitro and in animal models, reduces gluconeogenesis and improves glucose homeostasis, refreshing the interest in selective and reversible L-CPT1 inhibition as a potential antihyperglycemic approach.

Daporinad, also known as APO-866 and FK866, is a small molecule with potential antineoplastic and antiangiogenic activities. NMPRTase inhibitor APO866 binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis.

CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.

Tamibarotene(Am-80) is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.

Mirk-IN-1 is a potent, specific inhibitor of Dyrk1B (Mirk kianse) and Dyrk1A with IC50 of 68 nM and 22 nM respectively, shows SW620 cell IC50 of 1.9 uM.

INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.

EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

EN460 is a specific mall molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1), interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation (IC50=1.9 uM).

SCH 529074 is a small molecule mutant p53 reactivator that binds p53 DNA binding domain with Kd of 1-2 uM.

Merck60 (BRD 6929, Compound-60) is a potent, selective and brain-penetrant inhibitor of HDAC1 and HDAC2 with IC50 of 1 nM and 8 nM respectively.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

Aspalatone is an anti-platelet aggregator (antithrombotic) that has been shown to prolong bleeding time in the mouse model. Aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy.

Ameltolide, a 4-aminobenzamide derivative, is an anticonvulsant agent which has been shown to be effective at inhibiting seizures in animal models.

LUF7346 is a novel hERG allosteric modulator that slows IKr deactivation and positively shifting IKr inactivation.

Cl-amidine (hydrochloride) is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

CCCI-01 is an inhibitor of centrosome clustering in cancer cells.

Chlorfenson is used to treat onychomycosis (nail fungus) as the primary indication.

A small molecule tumor translocation inhibitor that inhibits the prostate cancer cell transcriptional program, in part by inhibition of the demethylase KDM4C (IC50=30 uM).

BRD2492 is a highly potent, selective HDAC1/2 inhibitor (IC50=2/19 nM, respectively) that displays excellent selectivity versus HDAC3 (IC50=2.08 uM, ≥110-fold selectivity) and all other HDAC isoforms, increases caspase-3 activation..

CTX-012414 is a KAT6A inhibitor with IC50 value of 0.49 μM and KD value of 0.38 -M.

Sulphenone is a chemical that can be used for the control of mite. .

PAQ (Compound 4c) is a quinoxaline derivative. PAQ is an orally active neuroprotective agent, which targets dopamine (DA) neurons and activates reticulum endoplasmic ryanodine receptor (RyR) channels, without effects on glia cells.

C902 is a small-molecule inhibitor targeting LIN28-let-7 interaction, shows dose-dependent inhibition in an EMSA validation assay with IC50 of 5 uM.

Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.

Robenacoxib is a nonsteroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the relief of pain and inflammation in cats and dogs, a Cyclooxygenase(COX)-1 and COX-2 inhibitor..

SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ.

6-Maleimidocaproic acid contains a maleimide group and a terminal carboxylic acid. The terminal carboxylic acid can be reacted with primary amine groups in the presence of activators (e.g. EDC, or DCC) to form a stable amide bond. The maleimide group will react with a thiol group to form a covalent bond, enabling the connection of biomolecule with a thiol.