dCK Inhibitors
Deoxycytidine kinase (dCK) inhibitors constitute a class of chemicals specifically designed or identified to decrease the enzymatic activity of dCK, a crucial enzyme in the nucleoside salvage pathway that phosphorylates deoxyribonucleosides into their monophosphate forms. These inhibitors often mimic the structure of natural nucleosides, yet are modified to impede the catalytic process of the enzyme. By occupying the active site of dCK, these molecules can prevent the binding and subsequent phosphorylation of physiological substrates such as deoxycytidine, thereby reducing the production of essential deoxyribonucleotide triphosphates (dNTPs) necessary for DNA synthesis and repair. Some inhibitors achieve their effect by inducing a conformational change in the enzyme structure, rendering it less effective or entirely inactive. Others may bind to allosteric sites, shifting the enzyme into a less active conformation or preventing necessary conformational changes required for its activation.
The diversity in the chemical structures of dCK inhibitors allows for a range of interactions and specificities. While some molecules in this class are broad-acting and may affect related kinases, others have been developed to exhibit a high degree of specificity towards dCK, thus limiting their interaction with other cellular kinases. In addition to active site competition, certain dCK inhibitors function by destabilizing the enzyme-substrate complex, reducing the enzyme's affinity for its substrates, or by interfering with the enzyme's post-translational modifications, which are essential for its full activity.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
2-Chloro-2′-deoxyadenosine | 4291-63-8 | sc-202399 | 10 mg | $144.00 | 1 | |
Cladribine is a synthetic antineoplastic agent that, after being phosphorylated by dCK, disrupts DNA synthesis and repair, leading to cell death. It also has high affinity for dCK, potentially inhibiting the enzyme by feedback inhibition. | ||||||
Clofarabine | 123318-82-1 | sc-278864 sc-278864A | 10 mg 50 mg | $185.00 $781.00 | ||
Clofarabine is a purine nucleoside analog that requires activation by dCK. It competes with natural substrates, effectively inhibiting the enzyme's activity by substrate competition. | ||||||
Fludarabine | 21679-14-1 | sc-204755 sc-204755A | 5 mg 25 mg | $57.00 $200.00 | 15 | |
Fludarabine phosphate is a fluorinated nucleotide analog of adenosine that inhibits dCK by competing with its natural substrates for phosphorylation. | ||||||
Gemcitabine Hydrochloride | 122111-03-9 | sc-204763 sc-204763A | 25 mg 100 mg | $94.00 $283.00 | 13 | |
Gemcitabine is a cytidine analog that is phosphorylated by dCK. It competitively inhibits dCK while also incorporating into DNA, leading to chain termination. | ||||||
α-Decitabine | 22432-95-7 | sc-500301 sc-500301A | 10 mg 100 mg | $347.00 $2448.00 | ||
Decitabine is a deoxycytidine analog that can inhibit dCK by substrate competition. Once phosphorylated, it can also incorporate into DNA and act as a DNA methyltransferase inhibitor. | ||||||
1-β-D-Arabinofuranosylcytosine | 147-94-4 | sc-201628 sc-201628A sc-201628B sc-201628C sc-201628D | 1 g 5 g 25 g 100 g 250 g | $147.00 $258.00 $508.00 $717.00 $1432.00 | 1 | |
1-β-D-Arabinofuranosylcytosine, a cytosine nucleoside analog, is activated by dCK and competitively inhibits the enzyme. It is also incorporated into DNA, causing DNA chain termination. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine is a nucleoside analog of cytidine that can inhibit dCK by competing with natural nucleosides for the active site of the enzyme. | ||||||
Pentostatin | 53910-25-1 | sc-204177 sc-204177A | 10 mg 50 mg | $172.00 $702.00 | 5 | |
Pentostatin is an inhibitor of adenosine deaminase, which increases levels of dATP, a feedback inhibitor of dCK, thus indirectly inhibiting dCK activity. | ||||||
6-Thioguanine | 154-42-7 | sc-205587 sc-205587A | 250 mg 500 mg | $41.00 $53.00 | 3 | |
Thioguanine is converted to the active triphosphate form by dCK. This nucleotide analog then inhibits the enzyme through feedback mechanisms. | ||||||
Ribavirin | 36791-04-5 | sc-203238 sc-203238A sc-203238B | 10 mg 100 mg 5 g | $62.00 $108.00 $210.00 | 1 | |
Ribavirin is a guanosine analog that can be phosphorylated by dCK, which can result in inhibition through competitive binding. | ||||||