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BiochemicalTargets

Proteases

Proteases hydrolyze α-peptide bonds of proteins, either at the terminal amino acid (exoprotease) or an internal amino acid (endoprotease). Some proteases instead cleave isopeptide bonds (e.g. DUBs) or γ-glutamyl bonds (e.g. glutamate carboxypeptidase). Proteases play roles in development, wound healing, pregnancy, and many other processes, making them therapeutic targets for diseases such as cancer, inflammation, and infectious disease.

ACE

Captopril | Angiotensin-converting enzyme inhibitor

CAS:
62571-86-2
Catalog Number:
10-2253
Activity:
Angiotensin-converting enzyme inhibitor
Chemical Name:
(2S)-1-(3-Mercapto-2-methyl-propionyl)-L-proline
Molecular Weight:
217.28
Molecular Formula:
C9H15NO3S
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Water (up to 20 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 1 month
Shipping Code:
RT

ADAM

1,10-Phenanthroline HCl | Zn metalloprotease inhibitor

CAS:
18851-33-7
Catalog Number:
10-3017
Activity:
Zn metalloprotease inhibitor
Alternate Names:
o-Phenanthroline hydrochloride hydrate
Molecular Weight:
234.68
Molecular Formula:
C13H8N2 • HCl &bul; H2O
Solubility:
Soluble in DMSO (up to 5 mg/ml) or in Water (up to 2 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Aminopeptidases

gamma-L-Glutamyl-p-nitroanilide HCl | L-Glutamine uptake inhibitor and gamma-glutamyl transpeptidase substrate

CAS:
67953-08-6
Catalog Number:
10-4568
Activity:
L-Glutamine uptake inhibitor and gamma-glutamyl transpeptidase substrate
Alternate Names:
GPNA
Molecular Weight:
303.7
Molecular Formula:
C11H13N3O5 HCl
Solubility:
Soluble in Water (up to 5 mg/ml).
Physical Properties:
Off-white solid
Purity:
98%
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Actinonin | Leucyl aminopeptidase inhibitor

CAS:
13434-13-4
Catalog Number:
10-2549
Activity:
Leucyl aminopeptidase inhibitor
Chemical Name:
3-[[1-[-2-Hydroxymethyl)-1-pyrrolidinyl)carbonyl]-2-methylpropyl]carbamoyl]-octanohydroxamic acid
Molecular Weight:
385.51
Molecular Formula:
C19H36N3O5
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Puromycin | Translation inhibitor

CAS:
58-58-2
Catalog Number:
10-2100
Activity:
Translation inhibitor
Chemical Name:
(S)-3′-[[2-Amino-3-(4-methoxyphenyl)-1-oxopropyl]-amino]-3′-deoxy-N,N-dimethyl-adenosine dihydrochloride
Molecular Weight:
544.43
Molecular Formula:
C22H29N7O5 2HCl
Solubility:
Soluble in DMSO (up to 50 mg/ml), or in Water (up to 50 mg/ml).
Physical Properties:
Tan solid
Purity:
98%
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Carboxypeptidases

ZJ43 | Potent inhibitor of glutamate carboxypeptidases II and III

CAS:
723331-20-2
Catalog Number:
10-3904
Activity:
Potent inhibitor of glutamate carboxypeptidases II and III
Chemical Name:
N-[[[(1S)-1-Carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid
Molecular Weight:
304.30
Molecular Formula:
C12H20N2O7
Solubility:
Soluble in DMSO (up to at least mg/ml) or in Water (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 2 months.
Shipping Code:
RT

Caspases

Z-DEVD-FMK | Caspase-3 inhibitor

CAS:
210344-95-9
Catalog Number:
10-2904
Activity:
Caspase-3 inhibitor
Chemical Names:
Benzyloxycarbonyl-Asp(OMe)-Glu(OMe)-Val-Asp(OMe)-fluoromethylketone
Molecular Weight:
668.67
Molecular Formula:
C30H41FN4O12
Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
Lyophilized solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Emricasan | pan-Caspase inhibitor

CAS:
254750-02-2
Catalog Number:
10-4280
Activity:
pan-Caspase inhibitor
Chemical Names:
(3S)-3-[[(2S)-2-[[2-(2-tert-butylanilino)-2-oxoacetyl]amino]propanoyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
Alternate Name:
IDN-6556; PF-03491390
Molecular Weight:
569.51
Molecular Formula:
C26H27F4N3O7
Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

SM-164 | Smac mimetic

CAS:
957135-43-2
Catalog Number:
10-5464
Activity:
Smac mimetic
Chemical Names:
(3S,3′S,6S,6′S,10aS,10′aS)-N,N′-[1,4-phenylenebis[4,1-butanediyl-1H-1,2,3-triazole-1,4-diyl[(S)-phenylmethylene]]]bis[decahydro-6-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-5-oxo-pyrrolo[1,2-a]azocine-3-carboxamide
Molecular Weight:
1121.45
Molecular Formula:
C62H84N14O6
Solubility:
Soluble in DMSO (50 mg/ml)
Physical Properties:
White to pale-yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Cathepsins

SSAA09E1 | SARS-CoV viral entry inhibitor

CAS:
433212-75-0
Catalog Number:
10-5075
Activity:
SARS-CoV viral entry inhibitor
Chemical Names:
[(Z)-1-Thiophene-2-ylethylideneamino]thiourea
Molecular Weight:
199.29
Molecular Formula:
C17H9N3S2
Solubility:
Soluble in DMSO (100 mg/ml); ethanol (10 mg/ml with warming
Physical Properties:
Beige solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years at-20°C from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Z-Leu-Arg-AMC | Fluorogenic Cathepsin K substrate

CAS:
156192-32-4
Catalog Number:
10-5386
Activity:
Fluorogenic cathepsin substrate
Alternate Name:
Z-LR-AMC hydrochloride; Cbz-Leu-Arg-AMC hydrochloride
Molecular Weight:
615.13
Molecular Formula:
C30H38N6O6·HCl
Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
White solid
Purity:
>97% HPLC
Amino acid analysis and identity: Confirmed
Peptide content:
93%
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. Protect from light!
Shipping Code:
RT

Z-Phe-Arg-AMC | Fluorogenic cathepsin substrate

CAS:
70382-26-2
Catalog Number:
10-5385
Activity:
Fluorogenic cathepsin substrate
Alternate Name:
Z-FR-AMC hydrochloride; Cbz-Phe-Arg-AMC hydrochloride
Molecular Weight:
619.14
Molecular Formula:
C33H36N6O6·HCl
Solubility:
Soluble in DMSO (50 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
Amino acid analysis and identity: Confirmed
Peptide content:
94%
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. Protect from light!
Shipping Code:
RT

Coagulation proteases

Apixaban | Factor Xa inhibitor

CAS:
503612-47-3
Catalog Number:
10-5660
Activity:
Factor Xa inhibitor
Chemical Names:
4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
Molecular Weight:
459.51
Molecular Formula:
C25H25N5O4
Solubility:
Soluble in DMSO (40 mg/ml)
Physical Properties:
White solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

gamma Secretase

DAPT | gamma-secretase inhibitor

CAS:
208255-80-5
Catalog Number:
10-4514
Activity:
γ-secretase inhibitor
Alternate Names:
LY-374973
Chemical Name:
N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester
Molecular Weight:
432.46
Molecular Formula:
C23H26F2N2O4
Solubility:
Soluble in DMSO (up to 18 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Metalloproteases

Doxycycline monohydrate | Broad spectrum antibiotic

Doxycycline monohydrate (17086-28-1) is a  broad-spectrum tetracycline antibiotic.1 Inhibits matrix metalloproteases.2  Promotes wound repair by inhibiting collagen degradation in rat models.3  Displays neuroprotective effects in neurodegenerative

MMPs

PNF1 | Angiogenesis inducer

CAS:
10442-95-2
Catalog Number:
10-5556
Activity:
Angiogenesis inducer
Chemical Names:
2-(2-Oxocyclopentyl)isoindoline-1,3-dione; SC-3-149
Molecular Weight:
229.24
Molecular Formula:
C13H11NO3
Solubility:
Soluble in DMSO (35 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Batimastat | Matrix metalloprotease inhibitor (pan-specific)

CAS:
130370-60-4
Catalog Number:
10-1589
Activity:
Matrix metalloproteinase inhibitor (pan-specific)
Chemical Name:
(2R,3S)-N4-Hydroxy-N1-[(1S)-2-(methylamine)-2-oxo-1-(phenylmethyl)ethyl]-2-(2-methylpropyl)-3-[(2-thienylthio)methyl]butanediamide
Alternate Names:
BB-94
Molecular Weight:
477.64
Molecular Formula:
C23H31N3O4S2
Solubility:
Soluble in DMSO (up to 45 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

1,10-Phenanthroline HCl | Zn metalloprotease inhibitor

CAS:
18851-33-7
Catalog Number:
10-3017
Activity:
Zn metalloprotease inhibitor
Alternate Names:
o-Phenanthroline hydrochloride hydrate
Molecular Weight:
234.68
Molecular Formula:
C13H8N2 • HCl &bul; H2O
Solubility:
Soluble in DMSO (up to 5 mg/ml) or in Water (up to 2 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Neprilysin

Phosphoramidon | Neutral endopeptidase inhibitor

CAS:
119942-99-3
Catalog Number:
10-2548
Activity:
Neutral endopeptidase inhibitor
Chemical Name:
N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-tryptophan•2Na
Molecular Weight:
587.47
Molecular Formula:
C23H32N3O10P • 2Na
Solubility:
Soluble in DMSO, methanol, or distilled water
Physical Properties:
White solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO, methanol, or distilled water may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Proteasome

Z-Leu-Leu-Leu-vinylsulfone | Proteasome inhibitor

Z-Leu-Leu-Leu-vinylsulfone (193482-47-2) blocks the trypsin-like, chymotrypsin-like, and peptidylglutamyl peptidase activity in isolated proteasomes and in living cells via covalent modification of active site threonine residues.1,2 References/Citations: Bogyo et al.

Bz-Val-Gly-Arg-AMC | Proteasome substrate

CAS:
87779-49-5
Catalog Number:
10-2969
Activity:
Proteasome substrate
Chemical Name:
Benzoyl-Val-Gly-Arg-(7-amido-4-methylcoumarin)·trifluoroacetate
Molecular Weight:
705.7
Molecular Formula:
C30H37N7O6·CF3COOH
Solubility:
Soluble in DMSO.
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Carfilzomib | Proteasome inhibitor

CAS:
868540-17-4
Catalog Number:
10-1477
Activity:
Proteasome inhibitor
Alternate Names:
PR-171
Chemical Name:
(αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]- L-Phenylalaninamide
Molecular Weight:
719.93
Molecular Formula:
C40H57N5O7
Solubility:
Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
Shipping Code:
RT

Serine porteases

Apixaban | Factor Xa inhibitor

CAS:
503612-47-3
Catalog Number:
10-5660
Activity:
Factor Xa inhibitor
Chemical Names:
4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
Molecular Weight:
459.51
Molecular Formula:
C25H25N5O4
Solubility:
Soluble in DMSO (40 mg/ml)
Physical Properties:
White solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Viral proteases

Atazanavir | HIV protease inhibitor

CAS:
198904-31-3
Catalog Number:
10-5630
Activity:
HIV protease inhibitor
Chemical Names:
Methyl N-[(2S)-1-[2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
Alternate Name:
BMS 232632; CGP 73547; Latazanavir
Molecular Weight:
704.87
Molecular Formula:
C38H52N6O7
Solubility:
Soluble in DMSO (45 mg/ml)
Physical Properties:
White to off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Telaprevir | Hepatitis C protease inhibitor

CAS:
402957-28-2
Catalog Number:
10-4929
Activity:
HCV protease inhibitor
Chemical Names:
(3S,3aS,6aR)-2-[(2S)-2-[[(2S)-2-cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide
Alternate Name:
VX-950
Molecular Weight:
679.86
Molecular Formula:
C36H53N7O6
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Darunavir | HIV-1 protease inhibitor

CAS:
206361-99-1
Catalog Number:
10-4930
Activity:
HIV-1 protease inhibitor
Chemical Names:
[(3aS,4R,6aR)-2,3,3a,5,6a-Hexahydrofuro[2,3-b]furan-4-yl] N-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate; UIC-94017; TMC114
Molecular Weight:
547.67
Molecular Formula:
C27H37N3O7S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Other

1G244 | DPP8/9 inhibitor

CAS:
847928-32-9
Catalog Number:
10-4584
Activity:
DPP8/9 inhibitor
Chemical Names:
(S)-2-Amino-4-{4-[bis-(4-fluorophenyl)-methyl]piperazin-1-yl}-1-(1,3-dihydro-isoindol-2-yl)-butane-1,4-dione
Alternate Name:
PTX-1210
Molecular Weight:
504.57
Molecular Formula:
C29H30F2N4O2
Solubility:
Soluble in DMSO (>20 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

TIC10 | Mitochondrial caseinolytic protease P activator / Anticancer agent

CAS:
1616632-77-9
Catalog Number:
10-4090
Activity:
Mitochondrial caseinolytic protease P activator / Anticancer agent
Chemical Name:
7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one
Alternate Name:
ONC201
Molecular Weight:
386.49
Molecular Formula:
C24H26N4O
Solubility:
Soluble in DMSO (up to 25 mg/ml with warming).
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Benzamidine HCl | Trypsin and serine protease inhibitor

CAS:
1670-14-0
Catalog Number:
10-2687
Activity:
Trypsin and serine protease inhibitor
Chemical Name:
Amidinobenzene hydrochloride
Molecular Weight:
156.61
Molecular Formula:
C7H8N2 • HCl
Solubility:
Soluble in water (up to 50 mg/ml with warming).
Physical Properties:
White solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions are not stable and must be prepared fresh daily
Shipping Code:
RT