Chemical Structure : PKS3053
CAS No.:
1801380-55-1
PKS3053
(PKS-3053)
Catalog No.: PC-25747Not For Human Use, Lab Use Only.
PKS3053 is a potent, selective inhibitor of immunoproteasome (i-20S) subunit LMP7 (β5i/PSMB8) with IC50 of 0.5 nM, 118-fold selective over constitutive proteasome (c-20S) β5c (PSMB5).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PKS3053 is a potent, selective inhibitor of immunoproteasome (i-20S) subunit LMP7 (β5i/PSMB8) with IC50 of 0.5 nM, 118-fold selective over constitutive proteasome (c-20S) β5c (PSMB5).
PKS3053 inhibits i-20S β5i in Karpas-1106P cells with IC50 of 15 nM, 20-fold selective for c-20S β5c in Hela cells.
PKS3053 inhibits T cell proliferation in PBMCs upon stimulation by anti-CD3 antibody with EC50 of 15 nM.
PKS3053 induces ROS production in immune cells, prevents ILC2 inhibition by targeting i-20S.
PKS3053 shows mouse i-20S (IC50 5470 nM) inhibition far less than for human i-20S (IC50 15 nM).
PKS3053 decreases enzymatic activity of ACO2 in hILC2 cells.
Physicochemical Properties
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M.Wt
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569.66
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Formula
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C32H35N5O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-2-(2-(1H-indol-3-yl)-2-oxoacetamido)-N4-(tert-butyl)-N1-((S)-1-((naphthalen-1-ylmethyl)amino)-1-oxopropan-2-yl)succinamide
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References
1. Laurent P, et al. Proc Natl Acad Sci U S A. 2025 Nov 25;122(47):e2518190122.
2. Zhan W, et al. J Med Chem. 2020 Nov 12;63(21):13103-13123.
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