transplantation

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) intended for the treatment of organ transplantation rejection, graft-versus-host reaction post-transplantation, autoimmune disorders, allergic diseases, and chronic myeloproliferative disorders.

FK-330 (FR-260330) is a novel orally active inducible nitric oxide synthase inhibitor with potential anticancer and antitumor activity that prevents ischemia and reperfusion injury in rat liver transplantation.

FK-330 dihydrate (FR-260330 dihydrate) is a novel and effective nitric oxide synthase inhibitor. It can prevent ischemia and reperfusion injury in rat liver transplantation.

Glycocyamine (2-Guanidinoacetic acid), a precursor of creatine, is a replacement of dietary arginine and could support overall energy homeostasis of the bird. Glycocyamine is an important marker for renal failure, kidney transplantation, and the renal metabolic activity. The compound is a metabolite of guanidine.

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

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

Gigantol is a novel inhibitor of the Wnt β-catenin pathway. It inhibits Wnt β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K Akt NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

RWJ 50271 is a selective lymphocyte function-associated antigen-1 intercellular adhesion molecule-1(LFA-1 ICAM-1) interaction inhibitor( IC50 of 5.0 μM in HL60 cells).

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

DS06652923 is an orally active inhibitor targeting EGFR triple mutations. It exhibits growth-inhibitory effects on Ba F3EGFRdel19 T90M C795S cells, with a GI50 value of 9.4 nM. Additionally, DS06652923 induces tumor regression in the Ba F3 syngeneic transplantation model.

PQA-18, an inhibitor of p21-activated kinase 2 (PAK2; IC50 = 10 nM), is derived from Ppc-1 (product number 42352) and exhibits immunosuppressive properties. It inhibits IL-2 production in Jurkat T cells induced by Concanavalin A (product number 14951) with an IC50 of 400 nM. Topically applied at 0.1%, PQA-18 reduces the severity of atopic dermatitis, serum IgE levels, and skin thickness in the NC Nga mouse model. A lower concentration of 0.05% also decreases skin nerve fiber density in NC Nga mice. Additionally, PQA-18 administered at 4 mg kg improves graft survival in a rat small intestine transplantation model.

Maclurin (NSC-83240) is a phenolic component of mulberry twigs, exerts anti-metastatic effects. Maclurin effectively protects against OH-induced damages to DNA and MSCs and can be used in studies about the prevention of many diseases or MSCs transplantation.

Cardiogenol C is a cardiomyogenesis inducer in embryonic stem cells.

TH9402 is a dibrominated rhodamine derivative and potent photosensitizer and useful in photodynamic therapy. TH9402 eradicates multiple myeloma (MM) and BC cell lines, while sparing more than 50% of normal pluripotential blood stem cells from healthy volu

High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J.Hepatol. 42 850 PMID:15885356 |Ma et al (2007) A pathogenic role for c-Jun amino-terminal kinase signaling in renal fibrosis and tubular cell apoptosis. J.Am.Soc.Nephrol. 18 472 PMID:17202416 |Ma et al (2009) Blockade of the c-Jun amino terminal kinase prevents crescent formation and halts established anti-GBM glomerulonephritis in the rat. Lab.Invest. 89 470 PMID:19188913 |Zhang et al (2015) The c-Jun N-terminal kinase inhibitor SP600125 inhibits human cytomegalovirus replication. J.Med.Virol. 87 2135 PMID:26058558 |Vasilevskaya et al (2015) Inhibition of JNK sensitizes hypoxic colon cancer cells to DNA-damaging agents. Clin.Cancer.Res. 21 4143 PMID:26023085

Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 |Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:27461445 |Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID:27486815

Terevalefim (ANG-3777) is an hepatocyte growth factor (HGF) mimetic. Terevalefim selectively activates the c-Met receptor.

Mitobronitol (Myelobromol; DBM) is a brominated analog of mannitol and an anticancer agent classified as an alkylating agent. Mitobronitol exhibits myelosuppressive effects, significantly reducing the risk of several complications in allogeneic bone marrow transplantation for accelerated chronic granulocytic leukemia [1] [2].

Antitumor agent-60 is a potent antitumor agent that targets the RAS-RAF signaling pathway and binds to CRAF (Kd: 721.3 nM). antitumor agent-60 increases p53 and ROS levels in cancer cells, resulting in oval and irregular nuclei. antitumor agent-60 is sufficient to block the cell cycle in G2 M phase and induce apoptosis. Antitumor agent-60 is sufficient to block the cell cycle in G2 M phase and induce apoptosis. In the A549 tumor transplantation model, Antitumor agent-60 has the ability to inhibit tumor growth.

Basiliximab (CHI 621) is a chimeric mouse human IgG1 monoclonal recombinant antibody targeting the interleukin-2 receptor, demonstrating potent immunosuppressive activity for use in kidney transplantation studies.

Phospholipid-PEG-Biotin (MW 1000 and MW 3400) is a derivative of a phospholipid and PEG, featuring a biotin moiety and a phospholipid connected via a linear PEG linker. This compound, particularly with a molecular weight of 3400, is capable of interacting with avidinylated antibodies. It finds applications in modifying the surface of liposomes, cells, and pancreatic islets, making it useful in cell transplantation [1] [2] [3].

Phospholipid-PEG-Biotin (MW 2000), a biotin-labeled phospholipid PEG derivative, is designed for modifying the surfaces of liposomes, cells, and pancreatic islets intended for cell transplantation. This compound integrates the properties of three distinct components: phospholipids, which are lipids featuring a hydrophilic head and two hydrophobic tails ; PEG, a low-toxicity, water-soluble, hydrophilic polymer; and biotin, an enzyme co-factor utilized in protein labeling [1].

Phospholipid-PEG-Biotin (MW 3400) is a derivative of phospholipid PEG featuring biotin and a phospholipid connected via a linear PEG linker. This compound can bind avidinylated antibodies and is used to modify liposome and cell surfaces, as well as pancreatic islets in cell transplantation applications [1] [2] [3].

Phospholipid-PEG-Biotin (MW 5000), a derivative of phospholipid PEG, serves to modify the surfaces of liposomes, cells, and pancreatic islets for cell transplantation. This compound incorporates a phospholipid (a lipid featuring a hydrophilic head and two hydrophobic tails ), PEG (a hydrophilic, water-soluble polymer with low toxicity), and Biotin (an enzyme co-factor useful for protein labeling) [1].