PASK Inhibitors
Chemical inhibitors of PASK can be diverse in their mechanisms of action, each targeting the kinase in different ways to achieve inhibition. Staurosporine is a well-known kinase inhibitor that acts by occupying the ATP binding site of PASK, which is essential for its kinase activity. This competitive inhibition prevents PASK from phosphorylating its substrates, leading to a functional inhibition of its activity. Similarly, H-89 targets the ATP binding site of PASK, acting as a competitor and thereby hindering the enzyme's catalytic action. The inhibition is also observed with 5-Iodotubercidin, which, by competing with ATP, can block the phosphorylating action PASK is supposed to carry out. K252a, another kinase inhibitor, binds to the same site and prevents ATP from engaging with PASK, ensuring that the kinase cannot exert its normal function.
Furthermore, compounds like Indirubin-3'-monoxime and Roscovitine disrupt the kinase activity of PASK by preventing ATP from binding to its active site, which is a crucial step for the kinase to function. SP600125, although primarily a JNK inhibitor, can also inhibit PASK by blocking the ATP binding domain, thereby preventing activation. SB 203580 and PD 98059 exert their inhibitory effects on PASK by interfering with the phosphorylation process, which is a critical activity that PASK performs. LY294002 and Wortmannin target the PI3K/AKT pathway, which is indirectly related to PASK's regulatory functions. By inhibiting PI3K, these compounds reduce the downstream signaling events that would otherwise contribute to PASK activation. Rapamycin, an mTOR inhibitor, disrupts the nutrient and energy sensing pathway, which is intimately connected to the regulatory functions of PASK, leading to a decrease in PASK activity as part of the broader inhibition of the pathway.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a potent inhibitor of protein kinases. PASK is a serine/threonine kinase, and staurosporine inhibits PASK by blocking its ATP binding site, thereby preventing phosphorylation events that PASK would catalyze. | ||||||
H-89 dihydrochloride | 130964-39-5 | sc-3537 sc-3537A | 1 mg 10 mg | $94.00 $186.00 | 71 | |
H-89 is known to inhibit protein kinase A (PKA). PASK is a kinase, and H-89 can inhibit PASK by competing with ATP for binding to the kinase domain, thus inhibiting its kinase activity. | ||||||
5-Iodotubercidin | 24386-93-4 | sc-3531 sc-3531A | 1 mg 5 mg | $153.00 $464.00 | 20 | |
5-Iodotubercidin is an adenosine kinase inhibitor that may inhibit PASK by competing with ATP, which is required for PASK's kinase activity. | ||||||
K-252a | 99533-80-9 | sc-200517 sc-200517B sc-200517A | 100 µg 500 µg 1 mg | $129.00 $214.00 $498.00 | 19 | |
K252a is an indolocarbazole that inhibits a wide range of kinases. It can inhibit PASK by binding to the ATP binding site, thus blocking the kinase activity of PASK. | ||||||
Indirubin-3′-monoxime | 160807-49-8 | sc-202660 sc-202660A sc-202660B | 1 mg 5 mg 50 mg | $79.00 $321.00 $671.00 | 1 | |
Indirubin-3'-monoxime is a known inhibitor of cyclin-dependent kinases (CDKs) and can inhibit PASK by competing with ATP for the active site of the kinase, thereby reducing its activity. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an anthrapyrazolone inhibitor of c-Jun N-terminal kinase (JNK) and can inhibit PASK by preventing ATP from binding to the kinase domain, thus inhibiting PASK's enzymatic activity. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
SB 203580 is a pyridinyl imidazole that inhibits p38 MAP kinase. It can inhibit PASK by inhibiting the phosphorylation process which is vital for PASK's kinase activity. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD 98059 is a synthetic compound that inhibits MEK, which is upstream of ERK in the MAP kinase pathway. By inhibiting this pathway, PD 98059 indirectly reduces PASK activity, which is influenced by MAP kinase pathway signaling. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a morpholine derivative that inhibits PI3K. PASK activity is influenced by insulin signaling, which involves PI3K; thus, LY294002 can reduce PASK kinase activity by inhibiting this pathway. | ||||||
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 a macrolide compound that inhibits mTOR. Since mTOR is part of the nutrient and energy sensing pathway that PASK is involved in, rapamycin can indirectly inhibit PASK activity by inhibiting mTOR signaling. | ||||||