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Fluorometric Granzyme B Inhibitor Screening Kit SKU: PK-CA577-K169
Inhibitor Type
/
Purity
/
CAS Number
/
Scientific Score
3.85
Brand
PromoCell
Sizes
1 (100 Reactions)
Available From
1 Vendor
Price
$ 786.38
Catalog IDs
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Protease Inhibitor Cocktail SKU: PK-MB577-K271
Inhibitor Type
/
Purity
/
CAS Number
/
Scientific Score
3.85
Brand
PromoCell
Sizes
1 (1 Vial)
Available From
1 Vendor
Price
$ 298.80
Catalog IDs
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17-DMAG SKU: SIH-114
Inhibitor Type
/
Purity
> 98 % (TLC); NMR conforms
> 98 % (TLC); NMR conforms
CAS Number
467214-20-6
467214-20-6
Scientific Score
8.35
Brand
StressMarq Biosciences
Sizes
2 (1 - 5 mg)
Available From
1 Vendor
Price Range
$ 110.00 - $ 360.00
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AG 879 SKU: SIH-429
Inhibitor Type
/
Purity
≥ 99 % (TLC)
≥ 99 % (TLC)
CAS Number
148741-30-4
148741-30-4
Scientific Score
8.42
Brand
StressMarq Biosciences
Sizes
2 (5 - 25 mg)
Available From
1 Vendor
Price Range
$ 78.00 - $ 325.00
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AG490 SKU: SIH-428
Inhibitor Type
/
Purity
≥ 98 % (TLC)
≥ 98 % (TLC)
CAS Number
133550-30-8
133550-30-8
Scientific Score
8.42
Brand
StressMarq Biosciences
Sizes
2 (5 - 25 mg)
Available From
1 Vendor
Price Range
$ 60.00 - $ 195.00
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AP-18 SKU: SIH-310
Inhibitor Type
/
Purity
> 98 %
> 98 %
CAS Number
55224-94-7
55224-94-7
Scientific Score
8.35
Brand
StressMarq Biosciences
Sizes
2 (10 - 50 mg)
Available From
1 Vendor
Price Range
$ 88.00 - $ 370.00
Added to comparison remove item
AR A014418 SKU: SIH-492
Inhibitor Type
/
Purity
≥ 95 % (HPLC)
≥ 95 % (HPLC)
CAS Number
487021-52-3
487021-52-3
Scientific Score
8.42
Brand
StressMarq Biosciences
Sizes
2 (5 - 25 mg)
Available From
1 Vendor
Price Range
$ 95.00 - $ 375.00
Added to comparison remove item
AS 041164 SKU: SIH-433
Inhibitor Type
/
Purity
≥ 98 % (TLC)
≥ 98 % (TLC)
CAS Number
6318-41-8
6318-41-8
Scientific Score
6.57
Brand
StressMarq Biosciences
Sizes
2 (10 - 50 mg)
Available From
1 Vendor
Price Range
$ 69.00 - $ 295.00
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AZD6244 SKU: SIH-495
Inhibitor Type
/
Purity
≥ 98 %
≥ 98 %
CAS Number
606143-52-6
606143-52-6
Scientific Score
6.57
Brand
StressMarq Biosciences
Sizes
2 (5 - 25 mg)
Available From
1 Vendor
Price Range
$ 130.00 - $ 475.00
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CCT241161 SKU: SIH-186
Inhibitor Type
/
Purity
98 %
98 %
CAS Number
1163719-91-2
1163719-91-2
Scientific Score
4.85
Brand
StressMarq Biosciences
Sizes
1 (10 mg)
Available From
1 Vendor
Price
$ 560.00
Catalog IDs
Added to comparison remove item
Cyclopamine SKU: SIH-226
Inhibitor Type
/
Purity
> 98 %
> 98 %
CAS Number
4449-51-8
4449-51-8
Scientific Score
6.57
Brand
StressMarq Biosciences
Sizes
2 (1 - 5 mg)
Available From
1 Vendor
Price Range
$ 92.00 - $ 366.00
Added to comparison remove item
Dimethyloxaloylglycine (DMOG) SKU: SIH-382
Inhibitor Type
/
Purity
> 99 %
> 99 %
CAS Number
89464-63-1
89464-63-1
Scientific Score
6.57
Brand
StressMarq Biosciences
Sizes
2 (10 - 50 mg)
Available From
1 Vendor
Price Range
$ 57.00 - $ 226.00
Added to comparison remove item

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Inhibitor Function

As its name implies, inhibitors simply slow the activity of its target enzyme. Although inhibitors may seem counterintuitive to use for medical treatment, as most enzymatic activity is required for biological processes, inhibitors are quite effective at stopping pathogens or correcting imbalances. This is not to say inhibitors are solely synthetic. Organisms use inhibitors to protect themselves from potentially damaging proteins like nucleases or to regulate their metabolism. Such negative feedback slows overproduction of certain molecules and maintains the homeostasis of a cell. So, many drugs are enzymatic and are a key area in drug discovery within biochemistry and pharmacology. Inhibitors are used in a range of treatment, including chemotherapy, antibiotics, metabolic control, pesticides, and poisons.

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Inhibitor Discovery

As its name implies, inhibitors simply slow the activity of its target enzyme. Although inhibitors may seem counterintuitive to use for medical treatment, as most enzymatic activity is required for biological processes, inhibitors are quite effective at stopping pathogens or correcting imbalances. This is not to say inhibitors are solely synthetic. Organisms use inhibitors to protect themselves from potentially damaging proteins like nucleases or to regulate their metabolism. Such negative feedback slows overproduction of certain molecules and maintains the homeostasis of a cell. So, many drugs are enzymatic and are a key area in drug discovery within biochemistry and pharmacology. Inhibitors are used in a range of treatment, including chemotherapy, antibiotics, metabolic control, pesticides, and poisons.

Inhibitor Mechanism

Inhibitors work by either obstructing an enzyme’s active site to prevent a substrate from binding with its designated enzyme or by preventing an enzyme from catalyzing its reaction. The concentration necessary to inhibit effectively (its potency), and its ability to not bind to other molecules (specificity) are how the quality of new inhibitors are judged. A new inhibitor with a high specificity and potency ensures a drug will have few side effects and low toxicity.

Inhibitor Types

Inhibitors can then be categorized into two categories: reversible or irreversible. Reversible inhibitors are those whose chemical modifications can be undone. Unsurprisingly, irreversible inhibitors covalently modify an enzyme, thus making permanent changes.

Reversible Inhibitors

When reversible inhibitors attach to enzymes, they do not undergo chemical reactions and can thus be effectively removed via dilution or dialysis. To classify reversible inhibitors, scientists look at the effects of varying their concentration.

Types of RI:

Competitive Inhibition: Enzyme’s target substrate and inhibitor compete for the active site.

Uncompetitive Inhibition: The inhibitor is only activated once the substrate binds to the enzyme.

Non-Competitive Inhibition: when the inhibitor merely slows the activity of the enzyme but does not restrict the substrate-enzyme complex formation.

Mixed Inhibition: the inhibitor and substrate can bind to the enzyme at the same time, resulting in a slowing of activity with a reduction in affinity.

Irreversible Inhibitors

Irreversible inhibition occurs when an enzyme is covalently modified. This occurs when a functional group, usually containing nitrogen mustards, aldehydes, haloalkanes, alkenes, Michael acceptors, phenyl sulfonates, or fluorophosphonates bind with the amino acid side chains present on enzymes to form covalent adducts. Such chemical reactions do not denature proteins, but rather alter their specific enzyme’s active site.