Inhibitors for peptidase C01.034: cathepsin S

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Inhibitors Pharma

MERID	Inhibitor	Inhibitor name	Ki	Conditions	Reference
I02.036	FhKT1 (Fasciola hepatica)				Smith et al., 2020
I04.008	squamous cell carcinoma antigen 1				Sakata et al., 2004
I04.041	serpin srp-2 (Caenorhabditis elegans)				Pak et al., 2002
I25.001	cystatin A		0.05 nM		Abrahamson, 1994
I25.003	cystatin B		0.07 nM		Abrahamson, 1994
I25.004	cystatin C		0.008 nM		Abrahamson, 1994
I25.005	cystatin D		0.24 nM		Abrahamson, 1994
I25.014	phytocystatin	CaneCPI-2	0.28 nM		Shibao et al., 2020
I25.014	phytocystatin	CaneCPI-3	3.23 nM		Shibao et al., 2020
I25.014	phytocystatin	CaneCPI-5	0.82 nM		Shibao et al., 2020
I25.014	phytocystatin	CaneCPI-6	24 nM		Shibao et al., 2020
I25.014	phytocystatin	CPI-2 ({Citrus sinensis})	0.11 nM		Schneider et al., 2020
I25.045	caneCPI cystatin (Saccharum sp.)	CaneCPI-4	4.38 nM		Shibao et al., 2020
I25.049	sialostatin L (Ixodes scapularis)	ricistatin ({Ixodes ricinus})	34.4 nM		Martins et al., 2023
I25.051	cystatin Hv-CPI1 (Hordeum vulgare)	CaneCPI-1	30 nM		Shibao et al., 2020
I25.054	cystatin Hv-CPI5 (Hordeum vulgare)	CPI-1 ({Citrus clementina})	0.29 nM		Schneider et al., 2020
I25.064	cystatin RHcyst-1 (Rhipicephalus haemaphysaloides)	Rhcyst-1			<%Wang et al., 2015%>
I25.UPA	subfamily I25A unassigned peptidase inhibitors	FhCyLS-2 ({Fasciola hepatica})			Busa et al., 2023
I25.UPB	subfamily I25B unassigned peptidase inhibitors	CPI-1 ({Citrus sinensis})	8.2 nM		Schneider et al., 2020
I25.UPB	subfamily I25B unassigned peptidase inhibitors	CPI-2 ({Citrus clementina})	0.36 nM		Schneider et al., 2020
I25.UPB	subfamily I25B unassigned peptidase inhibitors	CPI-3 ({Citrus clementina})	0.56 nM		Schneider et al., 2020
I29.001	cathepsin L propeptide		65 nM		Guay et al., 2000
I29.004	cathepsin S propeptide		7.6 nM		Guay et al., 2000
I29.007	cathepsin K propeptide		3.6-6.3 nM		Guay et al., 2000
I29.010	cathepsin V propeptide		10.7 nM		Burden et al., 2007
I48.001	clitocypin		3.2 nM	natural inhibitor	Sabotic et al., 2009
I85.001	macrocypin 1		47.1 nm	natural inhibitor	Sabotic et al., 2009
I85.002	macrocypin 3		5.1 nm	recombinant form	Sabotic et al., 2009
I85.003	macrocypin 4		6.3 nm	recombinant form	Sabotic et al., 2009
	paecilopeptin				Shindo et al., 2002
	JNJ 10329670		30 nM		Thurmond et al., 2004
	CSI-75				Baugh et al., 2011
	LY3000328				Payne et al., 2014
	RO5444101				Figueiredo et al., 2015
	RO5459072				Theron et al., 2017
	small-molecule inhibitors of cysteine peptidases	Z-Phe-Gly-NHO-Bz
	small-molecule inhibitors of cysteine peptidases	non-covalent 2-(benzoxazol-2- ylamino)-acetamide			Tully et al., 2006
	small-molecule inhibitors of cysteine peptidases	N-[(1R)-1-[(benzylsulfonyl)methyl]-2-{[(1S)-1-methyl-2-{[4-(trifluoromethoxy)phenyl]amino}ethyl]amino}-2-oxoethyl]morpholine-4-carboxamide	32 nM		Tully et al., 2006
	small-molecule inhibitors of cysteine peptidases	a novel 2- arylphenoxyacetaldehyde inhibitor derived by the substrate activity screening (sas) method	490 nM		Inagaki et al., 2007
	small-molecule inhibitors of cysteine peptidases	morpholine-4-carboxylic acid {(S)-1-[4-cyano-1-(3-morpholin-4-yl-propyl)-piperidin-4-ylcarbamoyl]-4,4-dimethyl-hexyl}-amide			McGrath et al., 1998
	small-molecule inhibitors of cysteine peptidases	RO5461111			Rupanagudi et al., 2013
	small-molecule inhibitors of cysteine peptidases	SAR114137			Feth et al., 2013
	small-molecule inhibitors of cysteine peptidases	N-CBZ-piperidyl derivative 2			Yuan et al., 2018
	small-molecule inhibitors of cysteine peptidases	ortho-benzyloxyl phenylacetyl derivative 1			Yuan et al., 2018
	small-molecule inhibitors of cysteine peptidases	p-toluenesulfonyl derivative 3			Yuan et al., 2018
	small-molecule inhibitors of cysteine peptidases	methyl ((R)-2,5-dioxopyrrolidin-3-yl)-l-threoninate (compound R-4c)			Gorican et al., 2021
	small-molecule inhibitors of cysteine peptidases	3-{[(1S,2R,3'S)-2-hydroxycyclohexyl]amino}pyrrolidine-2,5-dione (compound (1S,2R,3'S-10)			Gorican et al., 2021
	small-molecule inhibitors of cysteine peptidases	SPR38			Previti et al., 2025
	small-molecule inhibitors of cysteine peptidases	SPR39			Previti et al., 2025
	small-molecule inhibitors of cysteine peptidases	SPR41			Previti et al., 2025
	aldehyde, ketone, glyoxal, or semicarbazone inhibitors of cysteine peptidases	dipeptide nitrile inhibitor BLN			Ward et al., 2002
	aldehyde, ketone, glyoxal, or semicarbazone inhibitors of cysteine peptidases	Z-FL-COCHO	0.185 nM		Walker et al., 2000
	nitrile inhibitors of cysteine peptidases	compound 12	4.02 nM		Lemke et al., 2020
	nitrile inhibitors of cysteine peptidases	compound 24	35.5 nM		Lemke et al., 2020
	CLIK-060	CLIK-60			Katunuma et al., 2003
	CLIK-060				Katunuma et al., 1999
	ZFL		185 pM
	DCG-04 biotinylated epoxide				Greenbaum et al., 2000
	BIL-DMK diazomethane inhibitor of cysteine peptidases				Falgueyret et al., 2004
	BIL-DMK diazomethane inhibitor of cysteine peptidases	Z-Phe-Ala fluoromethyl ketone
	Z-DEVD-FMK	z-DEVD-cmk		k2/K1 = 28100 M-1s-1	Rozman-Pungercar et al., 2003
	Ac-YVAD-CMK			k2/K1 = 6900 M-1s-1	Rozman-Pungercar et al., 2003
	Ac-YVAD-CMK	Z-Val-Ala-Asp-CH(2)F		k2/K1 = 160 M-1s-1	Rozman-Pungercar et al., 2003
	MK-0674				Isabel et al., 2010
	vinyl sulfone or other Michael acceptor inhibitors of cysteine peptidases	morpholyl-cyAla-hPhe-F-vinylsulfonate-Ph compound 6c	0.08 nM		Fuchs et al., 2023
	APC2848		18 nM		Bromme et al., 1996
	LHVS				Clark et al., 2007
	benzamidine derivatives	N-cyano-4-ethyl-N-(4-sulfamoylphenyl)benzamide	0.28 muM		Abdoli et al., 2023
	benzamidine derivatives	Benzydamine			Zhang et al., 2024