Activators & Inhibitors

(Z)-MDL 105519 is an inactive isomer of MDL105519.

Myriocin (Thermozymocidin), a metabolite derived from Myriococcum albomyces, is a serine-palmitoyltransferase (SPT) inhibitor with potential antitumour, anticancer, and antiparasitic activities.Myriocin inhibits tumour growth by regulating macrophage polarisation and function through the PI3K/Akt/mTOR pathway.Myriocin inhibits HCV infection and can be used in the study of neurological diseases. Myriocin inhibits HCV infection and can be used to study neuropathy and fungal infections.

PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).

Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor used in the treatment of HIV and chronic Hepatitis B.

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

Rolofylline is an effective and selective adenosine A1 receptor antagonist. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450.

TA 0910 acid-type is a metabolite of TA 0910. TA-0910 is a metabolically stable analog of thyrotropin-releasing hormone.

Tetrazine-Ph-acid is an alkyl chain-derived PROTAC linker employed in PROTAC synthesis[1].

VU0453379 is a highly selective and central nervous system penetrant positive allosteric modulator of glucagon-like peptide-1R (EC50: 1.3 μM).