PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.

The major circulating metabolite of vitamin D3.

NecroX-5 is a novel necroptosis inhibitor that reduces mitochondrial oxidative stress, prevents hypoxia/reoxygenation injury by inhibiting the mitochondrial calcium uniporter.

Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.

Novel slow H2S-NO-releasing hybrid, attenuating cardiac dysfunction after heart failure

Oral active histone deacetylase inhibitor with potent antitumor activity

Novel histone deacetylase inhibitor (HDACi) with potent oral antitumor activities

Novel histone deacetylase inhibitor (HDACi) with potent oral antitumor activities

Novel next generation orally active DPP-4 inhibitor to treat Type 2 Diabetes

Cyclooxygenase-1 inhibitor

Novel inhibitor of Cyclophilin J (CyPJ) PPIase, demonstrating remarkable inhibition of tumor cell growth, comparable to CsA but much stronger than 5-fluorouracil

Novel inhibitor of Cyclophilin J (CyPJ) PPIase, demonstrating remarkable inhibition of tumor cell growth, comparable to CsA but much stronger than 5-fluorouracil

Novel multi-target inhibitor, harboring selectivity of inhibiting EGFR T790M sparing wild-type EGFR

Natural antibiotic, having diverse biological activities including broad-spectrum antibiosis against Bacteria and lower Eukarya, plant disease suppression, and enhancement of the insecticidal activity of Bacillus thuringiensis toxin against lepidopteran l

Potent, cell-permeable and irreversible caspase-1/5 inhibitor

Antagonist of D1 and D2 dopamine receptors.

Novel COX-2 inhibitor

Novel potentiator of KCNQ2 potassium channels

The first potent and selective Mycobacterium tuberculosis Zmp1 inhibitor

Novel zinc sensor with a chloroalkane linker, reacting specifically with the engineered protein HaloTag, binding zinc ions with a threefold fluorescence enhancement

Gastroprotective agent for the treatment of peptic ulcer

Inhibitor of osteoclastogenesis and macrophage recruitment, decreasing bone turnover and stabilizing the bone matrix, exhibiting diverse anti-tumor effects in osteosarcoma

Potent, selective, and brain penetrating H2 receptor antagonist

Inducer of functional angiogenesis through increased H 2 S availability

Novel antidiabetic agent for the treatment of type 2 diabetes mellitus (DM)

Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3)

Potassium channel opener