GDC inhibitors represent a class of chemical compounds designed to selectively target and inhibit the activity of certain proteins encoded by genes that are often referred to by the prefix 'GDC', which stands for Genentech Developed Compounds. These inhibitors are typically small molecules that have been engineered to bind with high affinity to specific active sites or allosteric sites of their target proteins. The binding action of GDC inhibitors is aimed at altering the conformation of the protein in such a way that its activity is reduced or completely abrogated. This mechanism of action is predicated on the precise molecular interaction between the inhibitor and specific amino acid residues within the protein structure that are crucial for its functional state. The design of GDC inhibitors often involves a detailed understanding of the protein's three-dimensional structure, gained through techniques like X-ray crystallography or nuclear magnetic resonance spectroscopy, allowing for the strategic placement of functional groups within the inhibitor that can interact favorably with the protein's active site.
The specificity of GDC inhibitors is such that they can distinguish between closely related protein isoforms, which allows for a high degree of selectivity in their inhibitory action. This selectivity is important for minimizing off-target effects and ensuring that the inhibitors' action is confined to the intended protein of interest. In the development of these inhibitors, computational modeling and medicinal chemistry are integral for iteratively refining the chemical structure to enhance binding affinity and selectivity. The mode of action involves the stabilization of the protein in an inactive state, preventing it from undergoing conformational changes required for catalysis or interaction with other cellular components. By doing so, GDC inhibitors interfere with the protein's ability to partake in its normal biological processes, which may include signal transduction, gene expression regulation, or metabolic control. The ultimate effect of this inhibition is to halt the biological pathway in which the protein is involved, thereby preventing the downstream effects that would normally result from its activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Trichostatin A is a histone deacetylase inhibitor; it promotes acetylation of histones, leading to an open chromatin structure and increased transcription. Given that GDC activity is regulated at the transcriptional level, increased acetylation would result in the upregulation of genes that can suppress GDC expression or activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a potent inhibitor of phosphoinositide 3-kinases (PI3K). PI3K pathway activation is crucial for many cellular processes including growth and survival, which are indirectly related to GDC activity. By inhibiting PI3K, LY294002 could reduce cellular proliferation signals, thereby decreasing the functional activity of GDC. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 is a selective inhibitor of mitogen-activated protein kinase kinase (MEK), which in turn reduces extracellular signal-regulated kinase (ERK) pathway activity. Since the ERK pathway can regulate the function of numerous proteins, including GDC, inhibition by PD98059 could lead to decreased GDC activity. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
Rapamycin is an mTOR inhibitor that impedes the mTOR pathway, which is essential for protein synthesis and cell cycle progression. By inhibiting mTOR, rapamycin can decrease the synthesis of proteins that are involved in the activation of GDC. | ||||||
GW4869 | 6823-69-4 | sc-218578 sc-218578A | 5 mg 25 mg | $199.00 $599.00 | 24 | |
GW4869 is an inhibitor of neutral sphingomyelinase (nSMase), which is involved in the production of ceramide. Ceramide participates in pathways that regulate apoptosis and cellular stress, which can impact GDC activity. Inhibition of nSMase by GW4869 might lead to reduced ceramide levels, thereby influencing GDC function. | ||||||
Wiskostatin | 253449-04-6 | sc-204399 sc-204399A sc-204399B sc-204399C | 1 mg 5 mg 25 mg 50 mg | $48.00 $122.00 $432.00 $812.00 | 4 | |
WZB117 is a glucose transporter 1 (GLUT1) inhibitor, leading to decreased glucose uptake by cells. Since cellular energy metabolism can affect various signaling pathways, inhibition of glucose uptake could alter the metabolic state of a cell, potentially downregulating GDC activity. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is another MEK inhibitor that prevents the activation of ERK pathway. The inhibition of MEK, and consequently the ERK pathway, can lead to a decrease in GDC activity due to the ERK pathway's involvement in GDC regulation. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a specific inhibitor of p38 MAP kinase, which is implicated in the response to stress signals and cellular inflammation. By inhibiting p38 MAP kinase, SB203580 could influence cellular responses in a way that indirectly reduces GDC activity. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an inhibitor of c-Jun N-terminal kinase (JNK), which can regulate apoptosis and cell survival. Inhibition of JNK by SP600125 could affect cellular stress and survival pathways that indirectly modulate GDC activity. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC 23766 inhibits the Rac1 GTPase, which is involved in actin cytoskeleton organization. Disruption of actin cytoskeleton can affect cell motility and signaling, which may have downstream effects on GDC activity. | ||||||