| Identification | Back Directory | [Name]
L-Phenylalaninamide, N-(1,1-dimethylethoxy)-N2-(1-oxo-3-phenylpropyl)-L-asparaginyl-4-fluoro-N-(1-naphthalenylmethyl)- | [CAS]
1801379-22-5 | [Synonyms]
DPLG3
L-Phenylalaninamide, N-(1,1-dimethylethoxy)-N2-(1-oxo-3-phenylpropyl)-L-asparaginyl-4-fluoro-N-(1-naphthalenylmethyl)- | [Molecular Formula]
C37H41FN4O5 | [MOL File]
1801379-22-5.mol | [Molecular Weight]
640.74 |
| Hazard Information | Back Directory | [Uses]
DPLG3 is a specific chymotryptic-like β5i subunits inhibitor, with an IC50 of 4.5 nM. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 downregulates the protein levels of NF-κB p50 and p65. DPLG3 can be used for immune disease research[1][2][3]. | [in vivo]
DPLG3 (2.5-5 mg/kg, i.p., daily, starts on day 0 until day 12) attenuates disease progression in DSS-induced experimental colitis mice[1].
DPLG3 (25 mg/kg, i.p., per day, 14 d) induces prolongation of heart allograft survival in mice (transplants BALB/c mice hearts into fully allogeneic C57BL/6 mice recipients)[2].
DPLG3 (25 mg/kg) shows reduced CD4+ and CD8+ effector T cells in RAG-/- C57BL/6 mice transferred into CD3+ CD25- T cells[3].
| [IC 50]
p50; p65 | [References]
[1] Moallemian R, et al. Immunoproteasome inhibitor DPLG3 attenuates experimental colitis by restraining NF-κB activation. Biochem Pharmacol. 2020 Jul;177:113964. DOI:10.1016/j.bcp.2020.113964
[2] Sula Karreci E, et al. Brief treatment with a highly selective immunoproteasome inhibitor promotes long-term cardiac allograft acceptance in mice. Proc Natl Acad Sci U S A. 2016 Dec 27;113(52):E8425-E8432. DOI:10.1073/pnas.1618548114
[3] Basler M, et al. On the role of the immunoproteasome in transplant rejection. Immunogenetics. 2019 Mar;71(3):263-271. DOI:10.1007/s00251-018-1084-0 |
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