immunosuppressant

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].

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.

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.

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.

Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).

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

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

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.

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.

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)

Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.

Abetimus (LJP 394 free base), an immunosuppressant composed of four double-stranded DNA (dsDNA) oligonucleotides, can crosslink anti-dsDNA antibodies on B cell surfaces and reduce anti-dsDNA antibody levels, offering research potential for systemic lupus erythematosus [1].

Brodalumab (AMG 827) is a human monoclonal antibody targeting interleukin 17 receptor (IL-17R) IgG2, often used as an immunosuppressant in the treatment of psoriasis and psoriasis.

Isogarcinol is a natural polyisoprenylated benzophenone first isolated from plant species in the genus Garcinia. It has immunosuppressant actions, inhibiting the protein phosphatase calcineurin (IC50 = 36 μM) and suppressing the proliferation of T cells. Oral administration of isogarcinol in mice decreases delayed type hypersensitivity, prolongs graft survival in allogeneic skin transplants, suppresses inflammation in collagen-induced arthritis, and reduces clinical symptoms in experimental autoimmune encephalomyelitis. Isogarcinol inhibits the proliferation of HL-60 and PC-3 cancer cells (IC50s = 4 and 8 μg/ml, respectively) through cell cycle arrest and apoptosis.

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

Microcolin B, an acylpeptide immunosuppressant, is a highly potent and biologically unique compound containing proline. It is derived from the blue-green alga Lyngbya majuscule.

Derivative 2 is A novel Derivative of Cyclosporin A.Cyclosporin A is an immunosuppressant that binds to cyclophilin and inhibits calcineurin.

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

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.

Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. Cyclosporin B displays antiviral properties, inhibiting the entry of hepatitis B into hepatocytes. Cyclosporin B also

Cedelizumab (RWJ 49004), an IgG4 monoclonal antibody, selectively targets CD4 and exhibits immunosuppressant properties [1].

Muromonab, a monoclonal antibody that targets the CD3 receptor, blocks cytotoxic T cell function and serves as an immunosuppressant agent. It is administered to mitigate acute rejection of solid organ transplants [1].

Plipastatin A1, a lipopeptide isolated from B. cereus, demonstrates enzyme inhibitory and immunosuppressant properties. It effectively inhibits enzymes phospholipase A2 (PLA2), phospholipase C (PLC), and phospholipase D (PLD) with half-maximal inhibitory concentrations (IC50s) of 2.9, 1.3, and 1.4 µM, respectively. Additionally, at a concentration of 100 µg/ml, plipastatin A1 inhibits lipopolysaccharide (LPS)-induced B cell blastogenesis and T cell blastogenesis triggered by concanavalin A. In vivo studies reveal that a dose of 0.1 mg/animal effectively suppresses delayed-type hypersensitivity in mice.

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

Cyclosporin D is a metabolite of cyclosporin A, an immunosuppressant drug that binds cyclophilin D, inhibiting the phosphatase activity of calcineurin in T cells.

Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

Methotrexate diethyl ester is an antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofoltae dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.

5-Monobutyl methotrexate is an antineoplastic antimetabolite with immunosuppressant properties. It is a TETRAHYDROFOLATE DEHYDROGENASE inhibitor and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component

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.

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

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

Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor

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

Sydowinin B is a xanthone polyketide that has been found inA. sydowiiand has immunosuppressant activity.1It inhibits LPS- or concanavalin A-induced proliferation of isolated mouse splenic lymphocytes (IC50s = 19.2 and 20.8 μg/ml, respectively).2Sydowinin B inhibits superoxide generation in, and elastase release from, isolated human neutrophils induced by cytochalasin B and N-Formyl-Met-Leu-Phe with IC50values of 21.2 and 12.62 μM, respectively.3

Bactobolamine, an immunosuppressant, suppresses IL-2 production in CTLL cells at a concentration of 200 µg/ml and extends heart allograft survival in both MHC-compatible and MHC-incompatible rat pairings at a dosage of 200 mg/kg. Additionally, it enhances lifespan in rat liver and canine kidney allograft models.

Remisporine B is a polyketide and derivative of remisporine A that has been found inPenicilliumand has immunosuppressant activity.1,2It inhibits LPS- or concanavalin A-induced proliferation of isolated mouse splenic lymphocytes (IC50s = 30.1 and 32.4 μg/ml, respectively).1 1.Liu, H., Chen, S., Liu, W., et al.Polyketides with immunosuppressive activities from mangrove endophytic fungus Penicillium sp. ZJ-SY2Mar. Drugs14(12)217(2016) 2.Kong, F., and Carter, G.T.Remisporine B, a novel dimeric chromenone derived from spontaneous Diels-Alder reaction of remisporine ATetrahedron Lett.44(15)3119-3122(2003)

Tucotuzumab (Anti-EPCAM Recombinant Antibody) is a protein composed of an IgG1 monoclonal antibody specific for the human Epithelial Cell Adhesion Molecule (EpCAM) antigen, linked to two molecules of IL-2 . Tucotuzumab is an immunosuppressant and antineoplastic agent [1] .

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

Azotomycin is an antagonist of L-glutamine and may be used as an immunosuppressant.

Cyclosporin A-d4 (Major) is a deuterated compound of Cyclosporin A. Cyclosporin A has a CAS number of 59865-13-3. Cyclosporine A is a Calcineurin Inhibitor Immunosuppressant. The mechanism of action of cyclosporine is as a Calcineurin Inhibitor, and Cytochrome P450 3A4 Inhibitor, and P-Glycoprotein Inhibitor.

Colletodiol is a fungal metabolite that has been found inD. grovesiiand has immunosuppressant and antiviral activities.1,2It inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes (IC50s = 12 and 5 μg/ml, respectively).1Colletodiol inhibits influenza A viral replication in HeLa-IAV-Luc cells.2 1.Fujimoto, H., Nagano, J., Yamaguchi, K., et al.Immunosuppressive components from an ascomycete, Diplogelasinospora grovesiChem. Pharm. Bull.46(3)423-429(1998) 2.Lai, W., Wang, S., and Ye, X.Colletodiol inhibits the replication of influenza A virus WSN/H1N1 by reducing the activity of viral RNA polymeraseWei Sheng Wu Xue Bao53(12)1334-1339(2013)

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.

Homodestcardin is a cyclic depsipeptide fungal metabolite that has been found in T. roseum and has immunosuppressant activity. It inhibits concanavalin A-induced proliferation of isolated mouse T cells.

CYP3A4-IN-3 is a specific, highly affinity cytochrome P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) inhibitor (IC50: 0.075 μM). CYP3A4-IN-3 is an analogue of ritonavir with a simpler structure and twice as much inhibition as ritonavir. CYP3A4-IN-3 can be used as an antiviral agent and immunosuppressant.

Methotrexate di-n-butyl ester is an antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofoltae dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.

Methotrexate-d3 is a deuterated compound of Methotrexate. Methotrexate has a CAS number of 59-05-2. Methotrexate is a folate analog metabolic inhibitor with immunosuppressant and antineoplastic properties.

Cyclosporin H (CsH), a specific inhibitor of FPR1, inhibited lung inflammation in the ALI models. CsH significantly attenuated MTDs or NFP-induced inflammatory lung injury and activation of MAPK and AKT pathways. Cyclosporin H is a viral transduction enha

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

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

L-732531 is a tacrolimus-related immunosuppressant with lower toxicity.