BCKDK Inhibitors
Branched Chain Ketoacid Dehydrogenase Kinase (BCKDK) inhibitors belong to a category of compounds that target the regulatory enzyme BCKDK. BCKDK is an enzyme that phosphorylates and inactivates the mitochondrial enzyme complex known as branched-chain ketoacid dehydrogenase (BCKD). The BCKD complex plays a pivotal role in the catabolic pathway of branched-chain amino acids (BCAAs), which include leucine, isoleucine, and valine. These amino acids are essential for human health, as they cannot be synthesized endogenously and must be obtained through diet. Inhibition of BCKDK leads to a decrease in the phosphorylation of the BCKD complex, resulting in increased BCKD activity. Consequently, this can lead to an elevated rate of BCAA catabolism. The inhibitors of BCKDK, therefore, are critical modulators of the metabolic pathways that are responsible for the breakdown of BCAAs.
The design of BCKDK inhibitors is often informed by the understanding of the enzyme's structure and the molecular dynamics of its interaction with the BCKD complex. BCKDK inhibitors may be structured to specifically bind to the ATP-binding site of BCKDK, thereby preventing the transfer of a phosphate group to the BCKD complex. Alternatively, they might interact with other regulatory domains of the BCKDK enzyme to inhibit its activity. The specificity of BCKDK inhibitors is crucial, as it ensures the targeted modulation of BCAA catabolism without interfering with other kinases that have similar structural features. The development of these inhibitors usually involves a careful balance between potency, selectivity, and the ability to interact with the enzyme in a physiologically relevant environment. BCKDK inhibitors are typically the product of extensive research into the enzyme's function, the regulatory roles it plays in amino acid metabolism, and the structural biology that underpins its action.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
AICAR | 2627-69-2 | sc-200659 sc-200659A sc-200659B | 50 mg 250 mg 1 g | $65.00 $280.00 $400.00 | 48 | |
AICAR is an analog of adenosine monophosphate (AMP) that can activate AMP-activated protein kinase (AMPK). AMPK activation can affect BCKDK through phosphorylation, which can alter BCKDK's activity and subsequently the catabolism of BCAAs. | ||||||
Sodium phenylbutyrate | 1716-12-7 | sc-200652 sc-200652A sc-200652B sc-200652C sc-200652D | 1 g 10 g 100 g 1 kg 10 kg | $77.00 $166.00 $622.00 $5004.00 $32783.00 | 43 | |
Phenylbutyrate is a histone deacetylase inhibitor that can induce hyperacetylation of BCKDK, leading to its degradation. By reducing BCKDK levels, phenylbutyrate can indirectly increase the activity of BCKDC, enhancing the breakdown of BCAAs. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin is an mTOR inhibitor that can influence BCKDK levels indirectly by affecting the mTOR pathway, which has a role in protein synthesis and degradation. By inhibiting mTOR, rapamycin can lead to a reduction in BCKDK levels through mechanisms associated with protein turnover, indirectly affecting BCAA catabolism. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium chloride can activate glycogen synthase kinase 3 beta (GSK-3β), which can phosphorylate BCKDK, potentially leading to its inactivation or degradation. Through this mechanism, lithium chloride can indirectly decrease BCKDK activity. | ||||||
Metformin-d6, Hydrochloride | 1185166-01-1 | sc-218701 sc-218701A sc-218701B | 1 mg 5 mg 10 mg | $292.00 $822.00 $1540.00 | 1 | |
Metformin is another AMPK activator that can indirectly affect BCKDK activity through AMPK-mediated phosphorylation. This can lead to altered BCKDK function and BCAA metabolism. | ||||||
BML-275 | 866405-64-3 | sc-200689 sc-200689A | 5 mg 25 mg | $96.00 $355.00 | 69 | |
Compound C, also known as dorsomorphin, is an AMPK inhibitor. By inhibiting AMPK, it may indirectly affect BCKDK activity, because AMPK can phosphorylate and regulate BCKDK. | ||||||
Valproic Acid | 99-66-1 | sc-213144 | 10 g | $87.00 | 9 | |
Sodium valproate is a histone deacetylase inhibitor similar to phenylbutyrate. It can potentially induce hyperacetylation and subsequent degradation of BCKDK, leading to increased BCKDC activity and enhanced BCAA catabolism. | ||||||
Rosiglitazone | 122320-73-4 | sc-202795 sc-202795A sc-202795C sc-202795D sc-202795B | 25 mg 100 mg 500 mg 1 g 5 g | $120.00 $326.00 $634.00 $947.00 $1259.00 | 38 | |
Rosiglitazone is a PPARγ agonist that can indirectly influence BCKDK activity through the PPARγ signaling pathway, which can affect energy metabolism and potentially BCKDK regulation. | ||||||
Fenofibrate | 49562-28-9 | sc-204751 | 5 g | $41.00 | 9 | |
STO-609 is an inhibitor of the calcium/calmodulin-dependent protein kinase kinase (CaMKK). Since CaMKK can activate AMPK, inhibition by STO-609 can indirectly affect BCKDK activity through AMPK-mediated regulation. | ||||||
Berberine | 2086-83-1 | sc-507337 | 250 mg | $92.00 | 1 | |
Berberine is an isoquinoline derivative that can activate AMPK. Through AMPK activation, berberine can indirectly influence BCKDK activity, potentially altering BCKDK's regulatory effects on BCKDC and BCAA metabolism. | ||||||