GrpEL1 Inhibitors
GrpEL1 inhibitors are chemical compounds that specifically target and modulate the function of the GrpEL1 protein, a co-chaperone within the heat shock protein 70 (Hsp70) family. GrpEL1 plays a crucial role in the mitochondrial protein folding process by regulating the activity of Hsp70 through nucleotide exchange. This regulation ensures the proper folding of nascent mitochondrial proteins and their maintenance in a functional state. Inhibitors of GrpEL1 disrupt this process by interfering with its ability to promote the release of ADP from Hsp70, which is a key step in the ATP hydrolysis cycle. This inhibition leads to alterations in the protein-folding machinery, potentially causing an accumulation of misfolded or unfolded proteins within the mitochondrial matrix, which can stress the mitochondrial function and cellular homeostasis.
Chemically, GrpEL1 inhibitors vary in structure but are typically small molecules designed to bind either directly to the GrpEL1 protein or its interaction site with Hsp70. By binding to GrpEL1, these inhibitors alter its conformational dynamics, impeding its ability to undergo the conformational changes necessary for nucleotide exchange. This blockage affects the ATPase activity of Hsp70, leading to downstream effects on protein folding, stabilization, and mitochondrial integrity. Researchers often design GrpEL1 inhibitors based on structural data obtained from X-ray crystallography or NMR studies of the protein, allowing precise targeting of its functional sites. The development of these inhibitors involves a detailed understanding of protein-protein interactions and enzyme kinetics, ensuring they specifically affect GrpEL1 without disturbing other components of the mitochondrial chaperone system.
SEE ALSO...
Items 1 to 10 of 11 total
Display:
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Geldanamycin | 30562-34-6 | sc-200617B sc-200617C sc-200617 sc-200617A | 100 µg 500 µg 1 mg 5 mg | $38.00 $58.00 $102.00 $202.00 | 8 | |
Geldanamycin binds to Hsp90 and inhibits its chaperone activity. Given that GrpEL1 requires proper chaperone function for its activity, inhibition of Hsp90 can lead to a functional decrease in GrpEL1 due to improper folding or stabilization. | ||||||
17-AAG | 75747-14-7 | sc-200641 sc-200641A | 1 mg 5 mg | $66.00 $153.00 | 16 | |
17-AAG is an Hsp90 inhibitor, structurally similar to Geldanamycin. It interferes with the chaperone cycle of Hsp90, ultimately leading to decreased activity of client proteins including GrpEL1, by promoting their degradation. | ||||||
Radicicol | 12772-57-5 | sc-200620 sc-200620A | 1 mg 5 mg | $90.00 $326.00 | 13 | |
Radicicol binds competitively to the ATP-binding site of Hsp90, thus inhibiting its function. This results in destabilization of client proteins, including GrpEL1, as they rely on Hsp90's chaperone activity. | ||||||
Novobiocin | 303-81-1 | sc-362034 sc-362034A | 5 mg 25 mg | $96.00 $355.00 | ||
Novobiocin is an antibiotic that also acts as an Hsp90 C-terminal inhibitor, disrupting the chaperone's binding to client proteins. This would indirectly lead to a decrease in GrpEL1 activity due to lack of proper chaperone support. | ||||||
Silybin | 22888-70-6 | sc-202812 sc-202812A sc-202812B sc-202812C | 1 g 5 g 10 g 50 g | $54.00 $112.00 $202.00 $700.00 | 6 | |
Silibinin is known to inhibit STAT3 signaling. Since STAT3 can be a client protein of Hsp90, its inhibition might also decrease the stability and activity of GrpEL1 through reduced Hsp90 functionality. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
EGCG is known to bind and inhibit Hsp90, which could lead to reduced chaperoning and maturation of GrpEL1, decreasing its functional activity. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $155.00 | 6 | |
Celastrol is a potent Hsp90 inhibitor that leads to the degradation of its client proteins. As GrpEL1 depends on Hsp90 for stability, celastrol would indirectly reduce GrpEL1 activity. | ||||||
Withaferin A | 5119-48-2 | sc-200381 sc-200381A sc-200381B sc-200381C | 1 mg 10 mg 100 mg 1 g | $127.00 $572.00 $4090.00 $20104.00 | 20 | |
Withaferin A binds to Hsp90 and disrupts its function, leading to the degradation of client proteins, including GrpEL1. | ||||||
Herbimycin A | 70563-58-5 | sc-3516 sc-3516A | 100 µg 1 mg | $272.00 $1502.00 | 13 | |
Herbimycin A is a benzoquinoid ansamycin antibiotic that inhibits Hsp90's chaperone activity, which is essential for the stability and function of GrpEL1. | ||||||
NVP-AUY922 | 747412-49-3 | sc-364551 sc-364551A sc-364551B sc-364551C sc-364551D sc-364551E | 5 mg 25 mg 100 mg 250 mg 1 g 5 g | $150.00 $263.00 $726.00 $1400.00 $2900.00 $11000.00 | 3 | |
Luminespib is an isoxazole-derived Hsp90 inhibitor which would lead to decreased stability and function of GrpEL1 by inhibiting its chaperone, Hsp90. | ||||||