immunosuppressant

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Cortisone (17-Hydroxy-11-dehydrocorticosterone) is a corticosteroid with potent glucocorticoid activity.

Chlorphenesin (Chlorophenesin) is an antigen-associated immunosuppressant that inhibits IgE-mediated histamine release. It is also used as an antimycotic agent.

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

trans-Benzylideneacetone (Acetocinnamone) is used in various synthetic preparations.

Frentizole, an immunosuppressive agent, is an inhibitor of the Aβ-ABAD interaction

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

Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).

CPYPP is an inhibitor of DOCK2-Rac1 interaction. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner(IC50 : 22.8 µM). CPYPP also inhibits DOCK180, DOCK5 and

BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM in mouse and human T cells, respectively)

Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects, including the induction of apoptosis in activated lymph node cells through caspase-3 and PARP activation [1].

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.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

6-Mercaptopurine (6-MP) is an antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.

RS 61443 (Mycophenolate mofetil) is an immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH)

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.

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

Dexamethasone Sodium Phosphate (Dexadreson) , an interleukin receptor modulator, has anti-inflammatory and immunosuppressant effects. It belongs to a potent glucocorticoid class of steroid synthetic drugs.

Deflazacort (MDL 458) is a glucocorticoid served as an immunosuppressant and anti-inflammatory. It can be used to treat autoimmune diseases due to inhibiting the immune system. It can also be acted in the therapy of some types of Ys. Deflazacort can help to prevent and to treat the rejection of transplanted organs.

Gusperimus trihydrochloride is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.