Inhibitors
Kinases/Phosphatases

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Acetylation and Methylation:
Epigenetic Modulators of Gene Expression
The dynamic structural and functional scaffold of chromatin plays a vital role in many cellular processes, and is influenced by both genetic and epigenetic factors. DNA methylation and the post-translational modifications of histones are regarded as the major epigenetic factors.

DNA methylation and the post-translational modifications of histones are regarded as the major epigenetic factors.
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Protein kinases are enzymes that phosphorylate proteins on specific serine, threonine, or tyrosine residues. Stimulation of protein kinases is one of the most common mechanisms of signal transduction in cellular growth and differentiation. Protein kinases can be activated by calcium/calmodulin, phospholipids, cAMP and cGMP, growth factors, cytokines, and even toxins.

Protein Phosphatases modulate physiological responses by causing dephosphorylation of protein kinases and other proteins. They act on proteins involved in muscle contraction, protein synthesis, cholesterol metabolism, and several other biological processes. They can be inhibited by okadaic acid, calyculin, tautomycin, certain vanadium compounds, and other phosphatase inhibitors.

Small molecule inhibitors offer a powerful tool to assess the biological effects of perturbing signaling mediated by various protein kinases and phosphatases. Calbiochem® provides high quality small molecules that potently inhibit a broad-spectrum of protein kinases and phosphatases, which have been cited in numerous peer-reviewed publications.



Akt/PI 3-K/mTOR Signaling Pathway inhibitors Panel
Inhibitors included in the InhibitorSelect™ Akt/PI 3-K/mTOR Signaling Pathway inhibitors Panel (Cat. No. 124031). Click image to enlarge.
AKT (Protein Kinase B) Inhibitors

Akt, also known as protein kinase B (PKB), a serine/threonine kinase, is a critical enzyme in several signal transduction pathways involved in cell proliferation, apoptosis, angiogenesis, and diabetes. Four different isoforms of Akt (α, β1, β2, and γ) have been reported that differ slightly in the localization of their regulatory phosphorylation sites. Activation of Akt involves growth factor binding to a receptor tyrosine kinase and activation of PI 3-K, which phosphorylates the membrane bound PI(4,5)P2 (PIP2) to generate PI(3,4,5)P3 (PIP3) ...

MAPK Signaling Pathway inhibitors Panel
Inhibitors included in the InhibitorSelect™ MAPK Signaling Pathway inhibitors Panel (Cat. No. 444189). Click image to enlarge.
MAP Kinase Inhibitors

The mitogen-activated protein (MAP) kinases are a group of evolutionarily conserved protein serine/threonine kinases that are activated in response to a variety of extracellular stimuli and mediate signal transduction from the cell surface to the nucleus. They regulate several physiological and pathological cellular phenomena, including inflammation, apoptotic cell death, oncogenic transformation, tumor cell invasion, and metastasis. MAP kinases, in combination with several other signaling pathways, can differentially alter the phosphorylation status of transcription factors in a pattern unique to a given external signal ...


Protein Kinase C Inhibitors

Protein kinase C (PKC), a ubiquitous, phospholipid-dependent enzyme, is involved in signal transduction associated with cell proliferation, differentiation, and apoptosis. At least eleven closely related PKC isozymes have been reported that differ in their structure, biochemical properties, tissue distribution, subcellular localization, and substrate specificity. They are classified as conventional (α, β1, β2, and γ), novel (δ, ε, η, θ, &micro), and atypical (ζ,λ) isozymes. PKC isozymes negatively or positively regulate critical cell cycle transitions, including cell cycle entry and exit and the G1 and G2 checkpoints ...


Protein Phosphatase Inhibitors

Phosphorylation and dephosphorylation of structural and regulatory proteins are major intracellular control mechanisms in eukaryotes. Protein kinases transfer a phosphate from ATP to a specific protein, typically at serine, threonine, or tyrosine residues. Phosphatases remove the phosphoryl group and restore the protein to its original dephosphorylated state. Hence, the phosphorylation-dephosphorylation cycle can be regarded as a molecular "on-off" switch. Protein phosphatases (PPs) have been classified into three distinct categories: serine/threonine (Ser/Thr)-specific, tyrosine-specific, and dual-specificity phosphatases ...


EGFR Signaling Pathway inhibitors Panel
Inhibitors included in the InhibitorSelect™ EGFR Signaling Pathway inhibitors Panel (Cat. No. 324839). Click image to enlarge.
Protein Tyrosine Kinase Inhibitors

Phosphorylation of tyrosine residues modulate enzymatic activity and create binding sites for recruitment of downstream signaling proteins. Protein tyrosine kinases (PTKs) play a key role in the regulation of cell proliferation, differentiation, metabolism, migration, and survival. They are classified as receptor PTKs and non-receptor PTKs. Selective receptor and non-receptor PTK inhibitors represent a promising class of anti-tumor agents. These agents are shown to inhibit multiple features of cancer cells, including proliferation, survival, invasion, and angiogenesis ...

Rho Kinase (ROCK) Inhibitors

Rho kinase (ROCK), a serine/threonine kinase, serves as a target protein for small GTP-binding protein Rho. It serves as an important mediator of numerous cellular functions, including focal adhesions, motility, smooth muscle contraction, and cytokinesis. Since the ROCK-mediated pathway plays important roles in vascular smooth muscle contraction, cell adhesion, and cell motility, it has gained importance in the pathogenesis of atherosclerosis. Higher ROCK activity has been associated with endothelial cell dysfunction, cerebral ischemia, coronary vasospasms, and metabolic syndrome. Hence, ROCK inhibitors are gaining importance as therapeutic tools ...


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