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Cathepsin Inhibitors
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ALX-201-006 Revised 04-Sep-08
N-Acetyl-eglin C (recombinant)
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PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-006-MC01   0.1 mg 95.00 USD Add To Cart
ALX-201-006-MC05   0.5 mg 380.00 USD Add To Cart
ALX-201-006-M001   1 mg 670.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Thr-Glu-Phe-Gly-Ser-Glu-Leu-Lys-Ser-Phe-Pro-Glu-Val-Val-Gly-Lys-Thr-Val-Asp-Gln-Ala-Arg-Glu-Tyr-Phe-Thr-Leu-His-Tyr-Pro-Gln-Tyr-Asn-Val-Tyr-Phe-Leu-Pro-Glu-Gly-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-Asp-Arg-Val-Arg-Val-Phe-Tyr-Asn-Pro-Gly-Thr-Asn-Val-Val-Asn-His-Val-Pro-His-Val-Gly-OH
FORMULA: C377H552N96O107
MW: 8141.1
CAS NUMBER: 96380-69-7
SOURCE/HOST: Produced in E. coli.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
Product Description
Eglin C was originally isolated from the leech Hirudo medicinalis [1]. Recombinant N-acetyl-eglin C is a 70 amino acid peptide with identical biological activity to native eglin C. An effective inhibitor of chymotrypsin and subtilisin as well as of leukocyte elastase and cathepsin G.
Product Specific Literature References
[1] Structure of the elastase-cathepsin G inhibitor of the leech Hirudo medicinalis: U. Seemüller, et al.; Hoppe-Seyler's Z. Physiol. Chem. 361, 1841 (1980) Abstract
[2] A large fragment approach to DNA synthesis: total synthesis of a gene for the protease inhibitor eglin c from the leech Hirudo medicinalis and its expression in E. coli: H. Rink, et al.; Nucl. Acids Res. 12, 6369 (1984) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P01051: Eglin C (Hirudo medicinalis)
Further Categories Containing This Product:
Proteases Other ProductsRecombinant Proteins / Fusion Proteins
 
 
ALX-260-136 Revised 16-Jun-05
H-Arg-Lys-Leu-Leu-Trp-NH2
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SYNONYMS RKLLW-NH2
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-136-M001   1 mg 30.00 USD Add To Cart
ALX-260-136-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C35H59N11O5
MW: 713.9
PURITY: ≥98%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Highly potent peptide inhibitor of human cathepsin L.
Product Specific Literature References
Highly potent inhibitors of human cathepsin L identified by screening combinatorial pentapeptide amide collections:: A. Brinker, et al.; Eur. J. Biochem. 267, 5085 (2000) Abstract
 
 
ALX-620-080 Revised 23-May-06
bADA
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SYNONYMS Dibenzyl-1-[(R)-biotin-6-aminohexanoyl-aziridine]-2,3-(S,S+R,R)-dicarboxylate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Proteases Other Products
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ALX-620-080-M002   2 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C34H42N4O7S
MW: 650.8
CAS NUMBER: 744207-03-02
PURITY: ≥98% (HPLC)
APPEARANCE: White to yellow solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible, cell permeable, biotin-labelled inhibitor of cysteine proteases.
Product Specific Literature References
Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylate: C. Gelhaus, et al.; Biol. Chem. 385, 435 (2004) Abstract
Blocking effect of a biotinylated protease inhibitor on the egress of Plasmodium falciparum merozoites from infected red blood cells: C. Gelhaus, et al.; Biol. Chem. 386, 499 (2005) Abstract
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-260-017 Revised 07-Jul-08
CA-074
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SYNONYMS N-[L-3-trans-Propylcarbamoyloxirane-2-carbonyl]-Ile-Pro-OH
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-017-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C18H29N3O6
MW: 383.5
CAS NUMBER: 134448-10-5
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in ethyl acetate (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and specific inhibitor of cathepsin B in vitro and in vivo.
Product Specific Literature References
Novel epoxysuccinyl peptides. Selective inhibitors of cathepsin B, in vitro: M. Murata, et al.; FEBS Lett. 280, 307 (1991) Abstract
Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo: T. Towatari, et al.; FEBS Lett. 280, 311 (1991) Abstract
Specific assay method for the activities of cathepsin L-type cysteine proteinases: T. Inubushi, et al.; J. Biochem. 116, 282 (1994) Abstract
 
 
ALX-260-037 Revised 30-May-07
Calpain Inhibitor I
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SYNONYMS Ac-LL-Norleucinal
Ac-Leu-Leu-Nle-CHO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-037-M010   10 mg 80.00 USD Add To Cart
ALX-260-037-M050   50 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C20H37N3O4
MW: 383.5
CAS NUMBER: 110044-82-1
SOURCE/HOST: Synthetic.
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture.
Product Description
Inhibits calpain I (Ki=190nM), calpain II (Ki=220nM), cathepsin B (Ki=150nM) and cathepsin L (Ki=0.5nM). Inhibits neutral cysteine proteases and the proteasome. Protects against neuronal damage caused by hypoxia and ischemia. Inhibits apoptosis in thymocytes and metamyelocytes. Inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Also prevents nitric oxide production by activated macrophages by interfering with the transcription of inducible nitric oxide synthase (iNOS; NOS II). Inhibits the proteolysis of IκB-α and IκB-β by the ubiquitin-proteasome complex.
Product Specific Literature References
Serine and cysteine proteinase inhibitors prevent nitric oxide production by activated macrophages by interfering with transcription of the inducible NO synthase gene: J.M. Griscavage, et al.; BBRC 215, 721 (1995) Abstract
Further Categories Containing This Product:
Proteasome / Related ProductsCathepsin InhibitorsProteases Other Products
 
 
ALX-260-038 Revised 15-Nov-05
Calpain Inhibitor II
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SYNONYMS Ac-LLM-CHO
Ac-Leu-Leu-Met-CHO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-038-M010   10 mg 75.00 USD Add To Cart
ALX-260-038-M050   50 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C19H35N3O4S
MW: 401.6
CAS NUMBER: 110115-07-6
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light and moisture.
Product Description
Inhibitor of calpain I, calpain II, cathepsin B and cathepsin L.
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-260-014 Revised 19-Aug-08
Calpeptin
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SYNONYMS Z-Leu-norleucinal
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-014-M005   5 mg 85.00 USD Add To Cart
ALX-260-014-M010   10 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H30N2O4
MW: 362.5
CAS NUMBER: 117591-20-5
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 5mg/ml soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 2 months when stored at -20°C.
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture.

Product Description
Membrane permeable inhibitor of calpain I and II and cathepsin L. Promotes neurite elongation in differentiating PC12 cells. Prevents Ca2+-ionophore induced degradation of actin binding protein and P235 in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin (Prod. No. ALX-450-006) or thrombin.
Product Specific Literature References
Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins: T. Sasaki, et al.; J. Enz. Inhib. 3, 195 (1990) Abstract
Cell-penetrating inhibitors of calpain: S. Mehdi; TIBS 16, 150 (1991) Abstract
Specificity of calcium-activated neutral proteinase (CANP) inhibitors for human mu CANP and mCANP: K. Saito and R.A. Nixon; Neurochem. Res. 18, 231 (1993) Abstract
Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells: M. Pinter, et al.; Neurosci. Lett. 170, 91 (1994) Abstract
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-260-005 Revised 03-Mar-05
Chymostatin
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SYNONYMS (S)-1-Carboxy-2-phenylethyl)-carbamoyl-α-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-005-M001   1 mg 22.00 USD Add To Cart
ALX-260-005-M005   5 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C21H38N4O8
MW: 605.0 (average)
CAS NUMBER: 9076-44-2
SOURCE/HOST: Microbial.
SOLUBILITY: Soluble in DMSO (20 mg/ml) or glacial acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of serine proteinases having a chymotrypsin-like specificity like α-, β-, δ- and γ-chymotrypsin, chymases, cathepsin G, and most cysteine proteinases including papain and cathepsin A, B, H, and L. Mixture of type A (R=L-Leu), type B (R=L-Val), type C (R=L-Ile).
Product Specific Literature References
Chymostatin, a new chymotrypsin inhibitor produced by actinomycetes: H. Umezawa, et al.; J. Antibiot. 23, 425 (1970) Abstract
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-007 Revised 16-Feb-05
E-64
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SYNONYMS N-[N-(L-3-trans-Carboxyoxirane-2-carbonyl]-L-leucyl)-agmatine
L-trans-Epoxysuccinyl-leucylamide-(4-guanido)-butane
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-007-M005   5 mg 55.00 USD Add To Cart
ALX-260-007-M025   25 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C15H27N5O5
MW: 357.4
CAS NUMBER: 66701-25-5
SOURCE/HOST: Synthetic.
PURITY: ≥99%
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible inhibitor of cysteine proteinases like papain, cathepsin B and L. Acts by forming a thioether bond with the thiol of the active cysteine. Does not inhibit serine proteinases.
Product Specific Literature References
K. Hanada, et al.; Agric. Biol. Chem. 42, 529 (1978)
K. Hanada, et al.; Agric. Biol. Chem. 42, 523 (1978)
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-164 Revised 24-Sep-07
H-LVK-CHO
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SYNONYMS H-Leu-Val-Lys-CHO
Cathepsin B Inhibitor (Aldehyde)
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-164-M001   1 mg 70.00 USD Add To Cart
ALX-260-164-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C19H36N4O4
MW: 384.5
PURITY: ≥95%
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May form cyclic isomers.
Product Description
Inhibitor of cathepsin B (IC50=4nM). More potent than to leupeptin (IC50=310nM) (Prod. No. ALX-260-009).
Product Specific Literature References
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues: R.M. McConnell, et al.; J. Med. Chem. 36, 1084 (1993) Abstract
 
 
ALX-270-280 Revised 07-Apr-08
clasto-Lactacystin β-lactone (synthetic)
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SYNONYMS Omuralide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-270-280-C200   200 µg 280.00 USD Add To Cart
ALX-270-280-M001   1 mg 1'295.00 USD Add To Cart
Product Specification
FORMULA: C10H15NO4
MW: 213.2
CAS NUMBER: 155975-72-7
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 20mg/ml soluble in DMSO or acetonitrile.
ACTIVITY: Kobs/[I]=20’000M-1s-1 versus 20S:PA28 complex.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR.

Product Description
Highly specific, cell permeable, and irreversible 20S proteasome inhibitor. Inhibits ubiquitin proteasome pathway in cell culture (IC50=1µM). It has been suggested that the natural product lactacystin acts as a precursor for clasto-lactacystin β-lactone and that the latter is the sole species that interacts with the proteasome. Inhibits cathepsin A. Leads to a reduction of adipogenes