HKr18 Inhibitors
Chemical inhibitors of HKr18 can modulate its activity through various biochemical mechanisms, targeting different kinases and signaling pathways that are crucial for its functional regulation. Bisindolylmaleimide I, Ro-31-8220, and Go6983 share a common target in protein kinase C (PKC), which plays a pivotal role in signaling cascades that influence the activity of HKr18. These inhibitors can diminish the phosphorylation of specific substrates within the PKC pathway, leading to reduced HKr18 activity. Similarly, H-89 targets protein kinase A (PKA), another kinase that can phosphorylate proteins interacting with HKr18, thereby impacting its activity. By impeding PKA, H-89 can decrease the functional efficacy of HKr18.
Further upstream, LY294002 and Wortmannin are inhibitors of phosphoinositide 3-kinase (PI3K), which indirectly influences HKr18's activity by participating in signaling pathways that regulate cellular functions. These inhibitors prevent the initiation of PI3K-dependent signaling, which is necessary for the activation of HKr18. On a different pathway, PD98059 and U0126 function as selective inhibitors of mitogen-activated protein kinase kinase (MEK), which is upstream of the extracellular signal-regulated kinase (ERK) pathway that can affect HKr18. By inhibiting MEK, these chemicals result in a decreased ERK activity, which then leads to lower HKr18 activity. SB203580 and SP600125 inhibit p38 MAP kinase and c-Jun N-terminal kinase (JNK), respectively, both of which are part of signaling cascades that can modulate transcription factors and proteins that interact with HKr18. The inhibition of these kinases leads to altered cellular responses that can decrease the activity of HKr18. Lastly, Rapamycin targets the mammalian target of rapamycin (mTOR), a central regulatory kinase that, when inhibited, can result in changes to the phosphorylation and activation state of proteins within the mTOR signaling pathway, hence influencing the activity of HKr18.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a potent and selective inhibitor of protein kinase C (PKC), a pathway that can regulate the activity of a broad range of zinc finger proteins, including HKr18. By inhibiting PKC, the phosphorylation of downstream targets is reduced, which can lead to a decrease in HKr18 activity due to altered protein interactions and signaling cascades. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a phosphoinositide 3-kinase (PI3K) inhibitor. PI3K is involved in many signaling pathways, including those that regulate transcription factors and proteins such as HKr18. By inhibiting PI3K, LY294002 can reduce the activity of HKr18 by preventing the activation of pathways necessary for its full functional activity. | ||||||
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 is upstream of the extracellular signal-regulated kinase (ERK) pathway. This pathway can be involved in the regulation of proteins like HKr18. Inhibition of MEK and subsequent reduction in ERK activity can lead to decreased functional activity of HKr18 by altering its regulatory phosphorylation state. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a selective inhibitor of p38 MAP kinase, which is part of a signaling pathway that can influence the function of transcription factors and regulatory proteins such as HKr18. By inhibiting p38 MAP kinase, SB203580 can decrease the HKr18 protein activity through reduced transcription factor activation and altered cellular responses. | ||||||
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 is involved in regulating transcription factors and proteins that interact with regulatory proteins like HKr18. Inhibition of JNK can lead to a reduction in HKr18 activity by preventing the phosphorylation and activation of proteins that are part of HKr18's functional network. | ||||||
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 inhibitor of PI3K, similar to LY294002. It can suppress the activity of HKr18 by blocking PI3K-dependent signaling pathways that would otherwise contribute to the functional activation of HKr18. | ||||||
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 inhibitor of the mammalian target of rapamycin (mTOR), a key regulatory kinase. By inhibiting mTOR, Rapamycin can reduce the activity of HKr18 indirectly by altering the phosphorylation and activation state of proteins within the mTOR signaling pathway that affect HKr18's function. | ||||||
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, a kinase involved in numerous signaling cascades that regulate proteins like HKr18. Through MEK inhibition, U0126 can lead to a decrease in HKr18 activity as a result of impaired signaling required for its regulation. | ||||||
Ro 31-8220 | 138489-18-6 | sc-200619 sc-200619A | 1 mg 5 mg | $90.00 $240.00 | 17 | |
Ro-31-8220 is a potent PKC inhibitor that can also inhibit other kinases such as protein kinase A (PKA) and protein kinase G (PKG). Given PKC's role in regulating proteins like HKr18, Ro-31-8220 can inhibit HKr18 activity by obstructing the kinase activity necessary for its regulation. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
Go6983 is a pan-PKC inhibitor that can reduce the activity of all PKC isozymes. Since PKC isozymes can modulate the function of various proteins including HKr18, Go6983's inhibition of PKC can lead to decreased HKr18 activity by blocking essential phosphorylation events. | ||||||