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Inhibitors

DAPT

Cell Signaling Technology

Inhibitor Type
/
/
Purity
/
/
CAS Number
/
/
From
$ 103.00 (5 mg)
Sizes
1 (5 mg)
Catalog IDs
15020S
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Inhibitors

Cycloheximide

Cell Signaling Technology

Inhibitor Type
/
/
Purity
/
/
CAS Number
/
/
From
$ 103.00 (1 g)
Sizes
1 (1 g)
Catalog IDs
2112S
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Inhibitors

U-0126

Invivogen

From
$ 114.00 (5 mg)
Sizes
1 (5 mg)
Catalog IDs
tlrl-u0126
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Inhibitors

ARP 100, Selective inhibitor of MMP-2

Tocris

Inhibitor Type
/
/
Purity
>99%
>99%
CAS Number
704888-90-4
704888-90-4
From
$ 135.00 (5 mg)
Sizes
1 (5 mg)
Catalog IDs
2621/5
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Inhibitors

Cmpd101

Hello Bio

From
$ 135.00 (10 mg)
Sizes
2 (10 - 50 mg)
Catalog IDs
HB2840-10MG, HB2840-50MG
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Inhibitors

ABT-737 (Inhibitor for Bcl-2 family) SKU: BBC1006

Biospes

From
$ 1,150.00 (500 mg)
Sizes
2 (1 - 500 g)
Catalog IDs
BBC1006-1G, BBC1006-500MG
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Inhibitors

Protease Inhibitor Cocktail (Plant) SKU: BWR1021

Biospes

From
$ 25.00 (1 ml)
Sizes
1 (1 ml)
Catalog IDs
BWR1021-1ML
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Inhibitors

Protease, Phosphatase and PMSF (Combined) SKU: BWR1022

Biospes

From
$ 60.00 (1 Set)
Sizes
1 (1 Set)
Catalog IDs
BWR1022-1SET
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Inhibitors

17-DMAG SKU: SIH-114

StressMarq Biosciences

Inhibitor Type
/
/
Purity
> 98 % (TLC); NMR conforms
> 98 % (TLC); NMR conforms
CAS Number
467214-20-6
467214-20-6
From
$ 110.00 (1 mg)
Sizes
2 (1 - 5 mg)
Catalog IDs
SIH-114A, SIH-114-5MG
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Inhibitors

AG 879 SKU: SIH-429

StressMarq Biosciences

Inhibitor Type
/
/
Purity
≥ 99 % (TLC)
≥ 99 % (TLC)
CAS Number
148741-30-4
148741-30-4
From
$ 78.00 (5 mg)
Sizes
2 (5 - 25 mg)
Catalog IDs
SIH-429-5MG, SIH-429-25MG
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Inhibitors

AG490 SKU: SIH-428

StressMarq Biosciences

Inhibitor Type
/
/
Purity
≥ 98 % (TLC)
≥ 98 % (TLC)
CAS Number
133550-30-8
133550-30-8
From
$ 60.00 (5 mg)
Sizes
2 (5 - 25 mg)
Catalog IDs
SIH-428-5MG, SIH-428-25MG
Added to comparison remove item

Inhibitors

AP-18 SKU: SIH-310

StressMarq Biosciences

Inhibitor Type
/
/
Purity
> 98 %
> 98 %
CAS Number
55224-94-7
55224-94-7
From
$ 88.00 (10 mg)
Sizes
2 (10 - 50 mg)
Catalog IDs
SIH-310-10MG, SIH-310-50MG
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.