935888-08-7
Chemical Structure
PR-825
- CAS No.: 935888-08-7
- Formula:C22H34N4O8
- Molecular Weight:482.53
IUPAC Name: N-((S)-3-methoxy-1-(((S)-3-methoxy-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)-5-methylisoxazole-3-carboxamide
InChIKey: RQDDUSFPICWDPV-KLMMPHRKSA-N
SMILES: O=C(C1=NOC(C)=C1)N[C@@H](COC)C(N[C@@H](COC)C(N[C@@H](CC(C)C)C([C@]2(CO2)C)=O)=O)=O
Biological Activity: PR-825 is a selective constitutive proteasome β5 chymotrypsin-like active site inhibitor with an IC50 value of 17 nM for X/β5. PR-825 reduces MHC-I expression. PR-825 has no effect on collagen antibody-induced arthritis. PR-825 delays the onset and reduces the severity of experimental autoimmune encephalomyelitis in LMP7-deficient mice while inhibiting IFN-γ/IL-17 production, but has no such effect in wild-type mice[1][2][3][4][5][6][7][8][9].
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PR-825 | PR-825 is a selective constitutive proteasome β5 chymotrypsin-like active site inhibitor with an IC50 value of 17 nM for X/β5. PR-825 reduces MHC-I expression. PR-825 has no effect on collagen antibody-induced arthritis. PR-825 delays the onset and reduces the severity of experimental autoimmune encephalomyelitis in LMP7-deficient mice while inhibiting IFN-γ/IL-17 production, but has no such effect in wild-type mice. | |||||||||||||||||||||
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References
- [1]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis. Nature medicine. 2009 Jul;15(7):781-7. [Content Brief]
- [2]. Basler M, et al. Inhibition of the immunoproteasome ameliorates experimental autoimmune encephalomyelitis. EMBO molecular medicine. 2014 Feb;6(2):226-38.
- [3]. Kisselev AF, et al. Subunit specific inhibitors of proteasomes and their potential for immunomodulation. Current opinion in chemical biology. 2014 Dec 1;23:16-22.
- [4]. Basler M, et al. Prevention of experimental colitis by a selective inhibitor of the immunoproteasome. Journal of immunology (Baltimore, Md. : 1950). 2010 Jul 01;185(1):634-41.
- [5]. Basler M, et al. The immunoproteasome subunit LMP7 is required in the murine thymus for filling up a hole in the T cell repertoire. European journal of immunology. 2018 Mar;48(3):419-29.
- [6]. Schmidt C, et al. Immunoproteasome inhibition impairs T and B cell activation by restraining ERK signaling and proteostasis. Frontiers in immunology. 2018 Oct 26;9:2386.
- [7]. Orre M, et al. Reactive glia show increased immunoproteasome activity in Alzheimer's disease. Brain : a journal of neurology. 2013 May;136(Pt 5):1415-31.
- [8]. Basler M, et al. The immunoproteasome: a novel drug target for autoimmune diseases. Clinical and experimental rheumatology. 2015;33(4 Suppl 92):S74-9.
- [9]. Yeo IJ, et al. A dual inhibitor of the proteasome catalytic subunits LMP2 and Y attenuates disease progression in mouse models of Alzheimer's disease. Scientific reports. 2019 Dec 05;9(1):18393.
