CRF21 Inhibitors
CRF21 inhibitors represent a chemical class specifically designed to antagonize the activity of the CRF21 protein, a protein involved in a cellular signaling pathway. These inhibitors are characterized by their ability to bind selectively to the CRF21 protein, thereby blocking its interaction with its natural ligands or substrates. This blockage results in the disruption of the downstream signaling cascade that CRF21 typically mediates. The precise mechanism of action for these inhibitors can vary; some may compete with the natural ligand for the active site on CRF21, while others might induce a conformational change in the protein structure, which prevents its proper functioning. The design of CRF21 inhibitors often incorporates molecular structures that mimic the shape and charge distribution of the natural binding partners of CRF21, enabling a tight and specific binding affinity. By doing so, these compounds ensure high specificity and reduce off-target effects that could arise from interaction with other proteins within the cell.
The development of CRF21 inhibitors is rooted in the understanding of the protein's role in its specific signaling pathway. By studying the endogenous function of CRF21, scientists can identify key domains of the protein that are essential for its activity. Inhibitors that target these domains are typically the result of rational drug design, where computational modeling plays a crucial role in predicting how the inhibitor will interact with the protein. This is complemented by empirical methods such as high-throughput screening to identify promising chemical compounds that exhibit inhibitory effects. Once identified, these compounds undergo further refinement to enhance their potency and selectivity. The inhibitors' efficacy is quantitatively measured by their impact on the biochemical processes mediated by CRF21, usually through assays that can register changes in the protein's activity. This data allows for the iterative optimization of the inhibitors, fine-tuning their chemical properties for maximum inhibitory effect while minimizing any unintended interactions with other proteins.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 is a potent and selective inhibitor of mitogen-activated protein kinase kinase (MEK), which in turn regulates the ERK pathway. By inhibiting MEK, PD98059 indirectly leads to reduced ERK activity, which could downregulate CRF21 activity if CRF21 is downstream of ERK signaling. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a phosphatidylinositol 3-kinase (PI3K) inhibitor. By blocking PI3K, it prevents the activation of AKT, a kinase involved in survival pathways. If CRF21 activity is dependent on PI3K/AKT signaling for membrane localization or stability, LY294002 would result in CRF21 inhibition. | ||||||
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. mTOR is a central cell-growth regulator, and by inhibiting it, rapamycin could decrease protein synthesis and cell proliferation. If CRF21 function is tied to these processes, its activity would also be inhibited. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a p38 MAPK inhibitor. By inhibiting p38 MAPK, SB203580 could impede the phosphorylation of downstream substrates required for CRF21 activation if CRF21 is part of stress response pathways regulated by p38 MAPK. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is an inhibitor of both MEK1 and MEK2, which are upstream of ERK in the MAPK pathway. Inhibition of MEK1/2 by U0126 would lead to decreased ERK activity, potentially leading to reduced activity of CRF21 if it is regulated by the MAPK pathway. | ||||||
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). JNK participates in regulatory processes such as apoptosis and cellular differentiation. If CRF21 function is associated with JNK signaling, SP600125 would result in its inhibition. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a potent PI3K inhibitor, like LY294002, and would similarly lead to inhibition of AKT signaling. This would impede any CRF21-related activity that relies on the PI3K/AKT pathway for its function. | ||||||
Nutlin-3 | 548472-68-0 | sc-45061 sc-45061A sc-45061B | 1 mg 5 mg 25 mg | $56.00 $212.00 $764.00 | 24 | |
Nutlin-3 disrupts the interaction between p53 and MDM2, leading to stabilization and activation of p53. If CRF21 is negatively regulated by p53, activation of p53 by Nutlin-3 would result in the inhibition of CRF21. | ||||||
Apigenin | 520-36-5 | sc-3529 sc-3529A sc-3529B sc-3529C sc-3529D sc-3529E sc-3529F | 5 mg 100 mg 1 g 5 g 25 g 100 g 1 kg | $32.00 $210.00 $720.00 $1128.00 $2302.00 $3066.00 $5106.00 | 22 | |
Apigenin is a flavonoid that can inhibit protein kinase C (PKC). Since PKC is involved in a vast array of signaling pathways, including those regulating proliferation and apoptosis, inhibition by apigenin could lead to reduced CRF21 activity if CRF21 is modulated by PKC. | ||||||
ZM-447439 | 331771-20-1 | sc-200696 sc-200696A | 1 mg 10 mg | $150.00 $349.00 | 15 | |
ZM-447439 is an Aurora kinase inhibitor. Aurora kinases are essential for cell division, and their inhibition by ZM-447439 could lead to cell cycle arrest. If CRF21 function is linked to cell division, this inhibitor would decrease CRF21 activity. | ||||||