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Inhibitors

Score 9.06

X80 SKU : X3629

Sigma-Aldrich

Inhibitor Type
/
/
Purity
/
/
CAS Number
/
/
From
$ 121.00 (5 mg)
Sizes
2 (5 - 25 mg)
Catalog IDs
X3629-5MG, X3629-25MG
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Inhibitors

Score 9.95

Atezolizumab

Selleck Chemicals

Inhibitor Type
/
/
Purity
/
/
CAS Number
/
/
From
$ 707.00 (5 mg)
Sizes
1 (5 mg)
Catalog IDs
A2004
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Inhibitors

Score 4.84

sFRP-1 Inhibitor

Merck

From
$ 246.15 (5 mg)
Sizes
1 (5 mg)
Catalog IDs
344300-5MG
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Inhibitors

Score 1.03

BACE Inhibitor

EZBiolab

From
$ 171.05 (1 mg)
Sizes
2 (1 - 5 mg)
Catalog IDs
CP7219, CP7219-m5
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Inhibitors

Score 1.80

Pepstatin SKU: M183

AMRESCO

From
$ 63.36 (5 mg)
Sizes
2 (5 - 25 mg)
Catalog IDs
M183-5MG, M183-25MG
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Inhibitors

Score 1.03

Ribonuclease Inhibitor

AMRESCO

From
$ 226.71 (2 kU)
Sizes
1 (2 kU)
Catalog IDs
E633-2KU
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Inhibitors

Score 7.92

Prostaglandin D Synthase (hematopoietic-type) Inhibitor I SKU: 16256

Cayman Chemical

From
$ 111.86 (1 mg)
Sizes
3 (1 - 10 mg)
Catalog IDs
16256-1, 16256-5, ...
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Inhibitors

Score 8.18

ALK5 Inhibitor II (hydrochloride) SKU: 15526

Cayman Chemical

From
$ 31.02 (1 mg)
Sizes
4 (1 - 25 mg)
Catalog IDs
15526-1, 15526-5, ...
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Inhibitors

Score 8.19

AP39 SKU: 17100

Cayman Chemical

From
$ 29.14 (1 mg)
Sizes
4 (1 - 25 mg)
Catalog IDs
17100-1, 17100-5, ...
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Inhibitors

Score 7.94

AZD 8055 SKU: 16978

Cayman Chemical

From
$ 41.36 (1 mg)
Sizes
4 (1 - 50 mg)
Catalog IDs
16978-1, 16978-5, ...
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Inhibitors

Score 7.95

Baricitinib SKU: 16707

Cayman Chemical

From
$ 46.06 (1 mg)
Sizes
4 (1 - 25 mg)
Catalog IDs
16707-1, 16707-5, ...
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Inhibitors

Score 4.66

CHIR124 SKU: 16553

Cayman Chemical

From
$ 41.36 (1 mg)
Sizes
4 (1 - 25 mg)
Catalog IDs
16553-1, 16553-5, ...
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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.