PKS3053 | β5i inhibitor | Probechem Biochemicals

Chemical Structure : PKS3053

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PKS3053 (PKS-3053)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	569.66
分子式	C32H35N5O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-(2-(1H-indol-3-yl)-2-oxoacetamido)-N4-(tert-butyl)-N1-((S)-1-((naphthalen-1-ylmethyl)amino)-1-oxopropan-2-yl)succinamide

参考文献

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.

PKS3053 (PKS-3053)

生物&药学活性

物理化学性质&存储条件

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PKS3053 (PKS-3053)

生物&药学活性

物理化学性质&存储条件

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