Protein serine/threonine phosphatase
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mTOR inhibitor
FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.
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- Ogawa Y, .et al. Inhibition of astrocytic adenosine receptor A2A attenuates microglial activation in a mouse model of Sandhoff disease, Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035
- Yuko Okamoto, .et al. In vivo drug delivery efficiency of albumin-encapsulated liposomes as hydrophobic drug carriers, J Drug Deliv Sci Technol, 2018, 47: 62-66
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calcineurin inhibitor
Ascomycin is a potent immunosuppressive agent that could be used as a potential therapeutic agent for autoimmune diseases.
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Calcineurin inhibitory peptide is a selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 uM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).
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mGluR1 antagonist
DL-AP3, a racemic preparation of D-AP3 and L-AP3, is an inhibitor of phosphoserine phosphatase and an antagonist of the metabotropic glutamate receptor (mGluR), blocking phosphoinositide turnover mediated by the mGluR.
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Calcineurin-NFAT inhibitor
INCA-6 is a potent and selective inhibitor of calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling.
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Calcineurin/PP2B inhibitor
Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant.
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Calcineurin inhibitor
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
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