calcineurin

Mycophenolic Acid Impurity (5,7-dihydroxy-4-methylphthalide) is an an immunosuppresant drug and potent anti-proliferative, and can be used in place of the older anti-proliferative azathioprine. It is usually used as part of triple therapy including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone. It is also useful in research for the selection of animal cells that express the E. coli gene coding for XGPRT (xanthine guanine phosphoribosyltransferase).

Magnoloside A (Magloside A) is a phenylethanol glycoside from M. obovata Thunb, a calmodulin phosphatase inhibitor.

Calcineurin substrate acetate is from the regulatory RII subunit of cAMP-dependent protein kinase.

Calcineurin Autoinhibitory Peptide acetate is a selectivecalcineurin phosphatase inhibitor(IC50 ~ 10 μM). Calcineurin Autoinhibitory Peptide acetate can be used in the protection of neurons from excitatory neuronal death.

Calcineurin substrate (TFA), a peptide derived from the regulatory RII subunit of cAMP-dependent protein kinase, is utilized in the calcineurin activity assay [1].

Calcineurin Autoinhibitory Peptide TFA is a selective inhibitor of Ca2+ calmodulin-dependent protein phosphatase (calcineurin), exhibiting an inhibitory concentration (IC50) of approximately 10 μM. This compound has been shown to protect neurons from excitatory neuronal death [1] [2].

Calcineurin substrate (TFA) is a polypeptide derived from the regulatory RII subunit of camp-dependent protein kinase.Calcineurin substrate (TFA) can be used to determine the activity of Calcineurin.

Calcineurin Substrate is a Peptide from the regulatory RII subunit of cAMP-dependent protein kinase.

Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor that disrupts CN-NFAT signaling by targeting the NFAT(P) substrate at the calcineurin (CN) phosphatase site.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein serine/threonine calmodulin phosphatases (IC50=21 μM), enhances transferrin receptor-mediated transcytosis in Caco-2 cells, and increases the hypoglycemic effect of oral insulin-transferrin. hypoglycemic effect.

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

NFAT Inhibitor (VIVIT peptide) is a cell-permeable compound that selectively inhibits the calcineurin-mediated dephosphorylation of NFAT.

Voclosporin (ISAtx-247) is a novel, orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant used for treating lupus nephritis.

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

Ruclosporin is a compound that inhibits calcineurin, originally developed as an immunosuppressant.

Mevalonolactone is a sesquiterpene lactone known to inhibit calcineurin activity against p-Nitrophenyl phosphate, with an IC50 of 134.29 μM.

JH-FK-08 is an inhibitor of the serine threonine-specific phosphatase enzyme calcineurin (calcium-dependent phosphatase). It demonstrates antifungal activity, effectively inhibiting C. neoformans with a MIC80 of 0.8 µg mL. Additionally, JH-FK-08 exhibits immunosuppressive properties by inhibiting IL-2 expression with an IC50 of 42.6 nM, and shows anti-infective activity in mouse models.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

Fenvalerate (Evercide 2362) is a inhibitor of protein phosphatase 2B (calcineurin), a synthetic pyrethroid insecticide, and inhibits PP2B-Aα.High doses of Fenvalerate impair cognitive and behavioral development.Fenvalerate induces, through the Fas/FasL signaling pathway, the induction of Fenvalerate induces germ cell apoptosis in mouse testis through the Fas/FasL signaling pathway.

Pimecrolimus (SDZ-ASM 981), a calcineurin inhibitor immunosuppressant, binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin.