Protease Inhibitors

Product Specifications
1,10-Phenanthroline monohydrate

Formula: C₁₂H₈N₂ • H₂O

MW: 198.22 g/mol

Storage/Handling: Store desiccated at room temperature under inert gas.
Product is hygroscopic. 

PubChem Chemical ID: 21226

International shipments MUST be shipped by air (including Canada and Mexico). Shipments of 50 g, 100 g, and 250 g will be shipped as multiples of 25 g units to qualify for the small quantity exception.

AEBSF is an irreversible serine protease inhibitor. AEBSF has been shown to inhibit trypsin, chymotrypsin, plasmin, kallikrein and thrombin. It inhibits by acylation of the active site of the enzyme. As an alternative to PMSF and DFP, AEBSF offers lower toxicity, improved solubility in water and improved stability in aqueous solutions. AEBSF has been used in cell culture in concentrations of up to 0.25mM. Aqueous solutions are stable between pH 5-6; limited stability above pH 7.5.

Attention Canadian and Mexican customers: This product is a hazardous and can only ship via Air.

Product Specifications
AEBSF·HCl;
Pefabloc SC;
4-(2-Aminoethyl)-benzenesulfonylfluoride hydrochloride

MOLECULAR BIOLOGY GRADE

Formula: C₈H₁₀FNO₂S · HCl

MW: 239.69 g/mol

Storage and Handling: Store at -20°C. Protect from light.

PubChem Chemical ID: 186136

Aprotinin – from Bovine Lung

Aprotinin is a monomeric globular polypeptide derived from bovine lung tissue. It consists of a chain of 58 amino acids that fold into a stable, compact tertiary structure of the ‘small SS-rich” type, containing 3 disulfides, a twisted β-hairpin and a C-terminal α-helix.

Aprotinin inhibits several serine proteases, specifically trypsin, chymotrypsin, plasmin and kallikrein. Its action on kallikrein leads to the inhibition of the formation of factor XIIa. Binding is reversible with most aprotinin-protease complexes dissociating at pH >10 or < 3. Aprotinin is freely soluble in water (>10 mg/ml) as well as low ionic strength aqueous buffers.

Product Specifications:
Aprotinin
(Trasylol, Trypsin inhibitor (basic), Iniprol)

Formula: C₂₈₄H₄₃₂N₈₄O₇₉S₇

MW: 6511.44 g/mol

Color: White to off-white

Storage/Handling: Store at 2-8° C.

PubChem Chemical ID: 16130295

Asunaprevir is a potent inhibitor of the enzyme serine protease NS3 in hepatitis C viruses (HCV) and is currently in phase III clinical trials. This enzyme’s C terminal functions as a helicase for host DNA allowing access for viral manipulation. Asunaprevir is used in tandem with ribavirin and other direct or indirect acting antiviral compounds results in a thorough eradication of HCV.

Product Specifications
Asunaprevir

Formula: C₃₅H₄₆ClN₅O₉S

MW: 748.28 g/mol

Storage/Handling: Store at -20°C.

PubChem Chemical ID: 74891317

NOT FOR HUMAN USE!

Benzamidine hydrochloride monohydrate is an aromatic amidine. It is used in protein extractions as a strong reversible inhibitor of serine proteases such as trypsin, thrombin, plasmin and other trypsin-like proteases. Compared to aprotinin, benzamidine is considered to be just as effective in preventing the degradation of glucogon.

Product Specifications
Benzamidine Hydrochloride Monohydrate

Amidinobenzene Hydrochloride

Formula: C₇H₈N₂ · HCl · H₂O

MW: 174.630 g/mol

Storage/Handling: Store desiccated at -20°C. Protect from light.

PubChem CID: 16219042

Product Specifications
Bestatin
Ubenimex

Formula: C₁₆H₂₄N₂O₄

MW: 308.37

Storage/Handling: Store at room temperature.

PubChem Chemical ID: 72172

Carfilzomib is a second generation proteasome inhibitor that has been used in oncology research.Being a derivative of epoxomicin, carfilzomib has a tetrapeptide epoxyketone structure.

The anti-cancer activity of carfilzomib on proteasomes is attributed to irreversibly binding to a 20S subunit on proteasomes. Affinity of carfilzomib for the subunit has been shown to be fairly significant, allowing carfilzomib to be effective at targeting multiple myeloma and lymphoma.

Proteasomes degrade excess or damaged proteins in both the nucleus and cytosol by cleaving hydrophobic residue peptide bonds. When proteasomes are inhibited by carfilzomib, polyubiquinated proteins accumulate. Polyubiquinated proteins will upregulate p21 synthesis, which activates cell cycle arrest and eventually apoptosis.

Carfilzomib has also been shown to have poor solubility in aqueous solutions, but greater solubility in organic solvents such as DMSO. Aqueous solubility can be enhanced by diluting carfilzomib-organic solvent solution in aqueous buffers. Using aqueous carfilzomib in biological settings should be done in dilute concentrations to limit organic solvent presence. Because carfilzomib organic-aqueous solutions only have a shelf life of approximately 24 hours, it is recommended to make small portions for immediate use.

Product Specifications
Carfilzomib
CFZ

Formula: C₄₀H₅₃N₅O₇

MW: 719.91 g/mol

Storage/Handling: Store at 4°C.
Soluble in DMSO.

PubChem Chemical ID: 11556711

Dexamethasone is a fluorinated steroid and synthetic adrenal glucocorticoid which acts as an immunosuppressive and anti-inflammatory agent in pharmaceuticals. It is a corticosteroid hormone receptor agonist to annexin A and glucocorticoid receptors. In cell signaling activity, it regulates the survival, growth, and differentiation of T-cells.

Dexamethasone inhibits multidrug resistance-associated protein (MRP). As an antineoplastic agent, it negatively modulates inducible nitric oxide synthase (iNOS), a molecule highly expressed in tumors. This substance is capable of interfering with NF-kB activation and apoptosis pathways. Dexamethasone can also increase antiemetic or anti-nausea effects of 5-HT3 receptor antagonists and is given to chemotherapy patients to counteract such symptoms.

Medicinally, this chemical is classified with anti-inflammatories. It’s used to treat rheumatic diseases, autoimmune or immunological responses like allergies, asthma, swelling and allergic anaphylactic shock among others. It’s been incorporated into chemotherapy treatment for multiple myeloma. Endocrine and adrenal disorders are also treated with dexamethasone.

Product Specifications
Dexamethasone
Prednisolone F
9alpha-Fluoro-16alpha-methylprednisolone

Formula: C₂₂H₂₉FO₅

MW: 392.46 g/mol

Storage/Handling: Store at 4°C. Protect from light.

PubChem Chemical ID: 5743

E-64 (trans-Epoxysuccinyl-L-leucylamido(4-guanidino)butane) irreversibly inhibits cysteine proteases without affecting other enzymes that contain cysteine residues. E-64 is capable of inhibiting bromelain, trypsin, papain, staphopain, calpain, collagenase, ficain, cathepsin B, H and L. Inhibition of serine proteases is not seen with E-64, excepting trypsin.

E-64 is usually used in a concentration range of 1 to 10μM. It is widely used for in vivo studies due to its cell permeability, low toxicity, and potency. E-64 is being investigated for the treatment of diseases caused by cysteine protease activity. It has been observed to inhibit programmed cell death and restore antigen and mitogen activity related to normal proliferative responses in T cells obtained from HIV+ donors.

Product Specifications
E-64
trans-Epoxysuccinyl-L-leucylamido(4-guanidino)butane

MOLECULAR BIOLOGY GRADE

Formula: C₁₅H₂₇N₅O₅

MW: 357.41 g/mol

Storage/Handling: Store at -20°C.

PubChem Chemical ID: 123985

Ixazomib citrate is a citrate salt that is a second generation proteasome inhibitor used for anti-cancer research. In vivo research has shown ixazomib citrate to hydrolyze into its active ixazomib form which reversibly inhibits 20S proteasomes in multiple myeloma cancer cells. Ceasing this enzyme’s activity has been shown to decrease angiogenesis, induce apoptotic pathways and upregulate tumor suppressor genes.

Product Specifications
Ixazomib citrate

Formula: C₂₀H₂₃BCl₂N₂O₉

MW: 517.12 g/mol

Storage/Handling: Store at 4°C.

PubChem Chemical ID: 56844015

Leupeptin hemisulfate (Ac-Leu-Leu-argininal) is a reversible inhibitor of serine and cysteine endopeptidases. Leupeptin hemisulfate is capable of inhibiting plasmin, trypsin, papain, kallikrein, calpain and cathepsin B. No inhibition has been found with pepsin, cathepsins A and D, elastase, renin or chymotrypsin.

Leupeptin is also a lysosomal inhibitor, which promotes axon elongation due to the overexpression of FGFR1 in neurons. Through the inhibition of calpain, it prevents apoptosis of motoneurons and increases muscle function after nerve injury. Leupeptin is capable of reacting with various opioid receptors, reversibly inhibiting opioid receptor-ligand binding.

Leupeptin is usually used in a concentration range of 10 to 100μM. Leupeptin is widely used in many protease inhibitor cocktails due to its potency, low toxicity, and range of inhibition. Leupeptin is also used in a quantitative assay to measure macroautophagic flux in mammals and is being investigated for its use in treating malaria.

Product Specifications
Leupeptin Hemisulfate

MOLECULAR BIOLOGY GRADE

Formula: C₂₀H₃₈N₆O₄ ∙ 0.5 H₂SO₄

MW: 475.59 g/mol

Storage/Handling: Store at -20°C.

PubChem Chemical ID: 2733491

Pepstatin A is a competitive, reversible aspartic protease inhibitor and inhibits proteases such as pepsin, chymosin, renin, HIV proteases, and cathepsins D and E. Peptstatin A is highly selective and is often used in a mixture with other enzyme inhibitors. In vitro studies have shown pepstatin A is the only aspartic acid inhibitor that exhibits inhibitory effects on HIV proteases.

Pepstatin A is effective at inhibiting most affected proteases at a concentration of 1μM, but can inhibit pepsin at the picomolar range of concentrations. It is believed to function by way of a collected-substrate inhibition mechanism. Pepstatin A may also suppress differentiation of osteoclasts by inhibiting phosphorylation of MAP kinase and inhibiting NFATc1 expression.

Product Specifications
Pepstatin A

MOLECULAR BIOLOGY GRADE

Formula: C₃₄H₆₃N₅O₉

MW: 685.89 g/mol

PubChem Chemical ID: 5478883

Storage/Handling: Store at 4°C.
Pepstatin A is soluble in acetic acid, DMSO, ethanol, and methanol

PMSF is a serine protease inhibitor that irreversibly inhibits serine proteases by sulfonylation of the serine residue in the active site of the protease. It is widely used in protocols for the isolation of proteins.

PMSF is inactivated in aqueous solutions. The rate of inactivation increases with increasing pH and is faster at 25°C than at 4°C. The half-life of a 20mM aqueous solution of PMSF is ~35 minutes at pH 8.0. This short half-life means that aqueous solutions of PMSF can be safely discarded after they have been rendered alkaline (pH >8.6) and stored for several hours at room temperature.

Product Specifications:
Phenylmethylsulfonyl fluoride; PMSF
Phenylmethanesulfonyl fluoride;
α-Toluenesulfonyl fluoride

MOLECULAR BIOLOGY GRADE

Formula: C₇H₇FO₂S

MW: 174.19 g/mol

White to slightly off white cyrstalline powder

Storage/Handling: Store desiccated at 4°C.
Soluble in DMSO or 100% Ethanol.
Protect from light. Hygroscopic.

PubChem Chemical ID: 4784

Trypsin inhibitor is a serine protease inhibitor from soybeans that is specific for trypsin and trypsin-like proteases. Trypsin inhibitor from soybeans is a monomeric protein containing 181 amino acid residues in a single polypeptide chain cross-linked by two disulfide bridges. Soybean trypsin inhibitor forms a 1:1 complex with the active protease site. Inhibition may be reversed and is pH dependent. The optimal pH for trypsin binding is 8.0.

Product Specifications
Trypsin Inhibitor, Soybean, Purified >10,000 U/mg

HIGH PURITY GRADE

Storage/Handling: Store desiccated at -20°C.