Novel, potent, mutant-selective BET bromodomain inhibitor, showing >100-fold selectivity for the L/V mutant over wild-type and excellent DMPK properties

Inhibitor of cyclin-dependent kinases

Novel ATP-competitive GSK-3ß inhibitor, exhibiting potent antiproliferative activity

Endogenous peripheral TRPV1 ligand

Dual human A2a antagonist/MAO-B inhibitor

Potent and selective activator of protein kinase A (PKA) type I and II

Potent activator of cGMP-dependent protein kinase Ia, Ib and type II as well as of cGMP- gated ion channels

Unique cytoprotective mediator, inhibiting oxidative stress; Novel probe of the protein S-guanylation

Antitumor agent, displaying cytotoxicity against the human cancer cell lines, including MDA231, T-47D, Hs578t, SaoS2, K562, SKHep1,and Hep3B

Novel inhibitor of nitric oxide formation in macrophages independent of effects on TNF

Specific non-nucleoside RT inhibitor (NNRTI) of HIV-1 RT

Inhibitor of RNA synthesis

Building Block

Potent and selective inhibitor of NTPDase1

Potent and selective inhibitor of NTPDase1

Potent and selective inhibitor of NTPDase1

Building block for syntheses of 8-BuS-AMP, ADP, ATP, and c-AMP

Novel activator of cAMP-dependent protein kinase (PKA) with high selectivity for site B-I of PKA

Carcinogenic adduct, covalently binding DNA bases and promoting mutagenesis near the adduct site

Novel tumor-targeting NIR fluorophore-conjugated hypoxic tumor inhibitor, preferentially accumulating in hypoxic tumor cells, sensitively outlining the tumor contour, and effectively inhibiting tumor growth synergistically by chemotherapy and radiotherapy

Precursor of paclitaxel, a anti-tumor agent

Potent dual PKCθ/δ inhibitor, efficiently inhibiting tumor growth in pancreatic cancer (PC) by inducing cellular apoptosis and suppressing the NF-κB/p-P65 pathway

Potent and selective calcium sensing receptor agonist

Non-selective NOS inhibitor

Potent inhibitor of AChE in treatment of cognitive manifestation of AD

Natural hypoxia-inducible factor-1α (HIF-1α) inhibitor, targeting the protein activity which could stabilize HIF-1α

Fluorescent amino acid for protein labeling

Novel Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist, Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

Useful pharmaceutical building block

Ligand binding to the orthosteric site of D2 receptor