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BMS-566419 is an acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase (IMPDH). Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme in the de novo synthesis of guanosine nucleotides. BMS-566419 has clinical utility for the research of transplant rejection .
Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasma proteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases .
Muromonab is a monoclonal antibody targeting the CD3 receptor. Muromonab can block all cytotoxic T cell function. Muromonab also as an immunosuppressant agent given to reduce acute solid organ transplant rejection .
Clazakizumab is a monoclonal antibody with high affinity and specificity for the IL-6 (interleukin-6) cytokine. Clazakizumab may be helpful in inhibiting the cytokine response to SARS-CoV-2 in COVID-19. Clazakizumab can be used for the research of psoriatic arthritis (PsA) and renal antibody-mediated rejection .
Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals .
Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals .
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection .
Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals .
Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC50 of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals .
Letolizumab (BMS-986004) is a monoclonal antibody targeting CD40L, which is produced to express mutant IgG1 lacking effector function, including Fc binding and complement fixation. Letolizumab reduces rejection, thromboembolism and prolongs the survival time .
Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease .
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. BI 7446 can activate all five STING variants in cells and induce tumor-specific immune-mediated tumor rejection. BI 7446 can be used for immuno-oncology research .
Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research .
CTPS1-IN-1 (compound R80) is a CTPS1 inhibitor. CTPS1-IN-1 has the potential to research cancer (such as promoting vascular injury or surgical recovery) and immune system diseases (such as rejection of transplanted cells and tissues, transplant-related diseases or disorders, allergies, and autoimmune diseases) .
Castanospermine is a natural alkaloid that can be extracted from black beans or the Moreton Bay chestnut tree (Castanospermum australae). Castanospermine is an α/ β-glucosidase inhibitor. Castanospermine has anti-inflammatory, antiviral replication and anti-metastatic effects on prostate cancer. Castanospermine can be used as an immunosuppressant to prevent transplant rejection .
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice .
Belatacept (BMS 224818) is a selective T-cell costimulation blocker. Belatacept binds to CD 80/86 ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants .
Cyclosporin B is a group of nonpolar cyclic oligopeptides with immunosuppressive activity. Cyclosporin B is used for the prevention of graft rejection in organ transplantation .
Muromonab is a monoclonal antibody targeting the CD3 receptor. Muromonab can block all cytotoxic T cell function. Muromonab also as an immunosuppressant agent given to reduce acute solid organ transplant rejection .
Letolizumab (BMS-986004) is a monoclonal antibody targeting CD40L, which is produced to express mutant IgG1 lacking effector function, including Fc binding and complement fixation. Letolizumab reduces rejection, thromboembolism and prolongs the survival time .
Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection .
Clazakizumab is a monoclonal antibody with high affinity and specificity for the IL-6 (interleukin-6) cytokine. Clazakizumab may be helpful in inhibiting the cytokine response to SARS-CoV-2 in COVID-19. Clazakizumab can be used for the research of psoriatic arthritis (PsA) and renal antibody-mediated rejection .
Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease .
Empasiprubart (ARGX-117) a humanized inhibitory monoclonal antibody against complement C2. Empasiprubart prevents the formation of the C3 proconvertase and inhibits classical and lectin pathway activation upstream of C3 activation through binding to the Sushi-2 domain of C2. Empasiprubart exhibits pH- and calcium-dependent target binding. Empasiprubart prevents complement-mediated cytotoxicity in in vitro models for autoimmune hemolytic anemia and antibody-mediated rejection of organ transplants .
Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research .
Castanospermine is a natural alkaloid that can be extracted from black beans or the Moreton Bay chestnut tree (Castanospermum australae). Castanospermine is an α/ β-glucosidase inhibitor. Castanospermine has anti-inflammatory, antiviral replication and anti-metastatic effects on prostate cancer. Castanospermine can be used as an immunosuppressant to prevent transplant rejection .
TYR protein, a copper-containing oxidase, initiates melanin production by catalyzing the hydroxylation of tyrosine to DOPA. This essential step is rate-limiting in the synthesis of melanins and polyphenolic compounds. TYR further enables the oxidation of DOPA to DOPA-quinone and potentially mediates the conversion of DHI to indole-5,6 quinone, playing a crucial role in the intricate cascade of reactions involved in melanin biosynthesis. TYR Protein, Human (P.pastoris, His) is the recombinant human-derived TYR protein, expressed by P. pastoris , with N-His, N-6*His labeled tag. The total length of TYR Protein, Human (P.pastoris, His) is 359 a.a., with molecular weight of ~48 kDa.
