adenosine kinase inhibitor

Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associa

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

Adenosine monophosphate (AMP) is a purine ribonucleoside 5'-monophosphates and a key cellular metabolite in signal transduction and regulation of energy homeostasis.It has a role as an EC 3.1.3.11 (fructose-bisphosphatase) inhibitor, an EC 3.1.3.1 (alkaline phosphatase) inhibitor and an adenosine A1 receptor agonist.

ABT-702 dihydrochloride is a highly potent inhibitor of adenosine kinase (AK).

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A B C(IC50s=150-500 nM).

Anisodine hydrobromide is an inhibitor of adenosine kinase.

Potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase). Displays oral activity in animal models of pain and inflammation.

ABT-702 hydrochloride effectively inhibits adenosine kinase, exhibiting an IC50 value of 1.7 nM [1] [2].

A-286501 is an orally active adenosine kinase inhibitor (IC50=0.47 nM). A-286501 effectively attenuates nociception by a non-opioid, non-non-steroidal anti-inflammatory drug ADO, receptor mediated mechanism.

GP-515 HCl is an adenosine kinase inhibitor. In cultured rat myocardial myocytes (RMMs), GP-515 can induce the expression of vascular endothelial growth factor (VEGF). Under severe hypoxia (1% O(2)), GP-515 (20 microM) does not affect VEGF protein expression, but under mild hypoxic conditions, it increases VEGF expression by 27%.

GP-1-515 is an adenosine kinase inhibitor with anti-inflammatory effects.

GP3269 is a selective, potent, orally active human adenosine kinase (AK) inhibitor (IC50: 11 nM) with anticonvulsant effects in rats.

5'-Amino-5'-deoxyadenosine (NH2dAdo) is an adenosine kinase inhibitor targeting malignant tumors of the inert lymphatic system with antitumor and anticancer effects. Its mechanism is mediated by the inhibition of DNA synthesis and induction of apoptosis.

5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

Sp-Adenosine-5'-O-(1-thiodiphosphate) (Sp-ADP-α-S), an isomer of the sulfur-containing nucleotide derivative ADP-α-S, functions as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also promotes aggregation of isolated human platelets with an effective concentration (EC50) of 20 µM and induces relaxation in carbamoylcholine-precontracted guinea pig taenia coli with an EC50 of 58.9 µM.

Rp-Adenosine-5'-O-(1-thiodiphosphate) (Rp-ADP-α-S), a sulfur-containing isomer of the nucleotide derivative ADP-α-S, acts as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also induces aggregation in isolated human platelets with an effective concentration (EC50) of 20 µM and promotes relaxation in guinea pig taenia coli that has been precontracted with carbamoylcholine, with an EC50 of 58.9 µM.

Adenosine 5'-phosphosulfate is an ATP and sulfate competitive inhibitor of ATP sulfurylase in humans, S. cerevisiae, and P. chrysogenum (Ki = 18, 2500, and 1500 nM, respectively). Adenosine 5'-phosphosulfate also inhibits human adenosine 5'-phosphosulfate kinase (Ki = 47.5 μM) to prevent sulfation.

AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the low nanomolar cellular and biochemical inhibitory properties of AP23464 extend to frequently observed imatinib mesylate-resistant Bcr-Abl mutants, including nucleotide binding P-loop mutants Q252H, Y253F, E255K, C-terminal loop mutant M351T, and activation loop mutant H396P. AP23464 was ineffective against mutant T315I, an imatinib mesylate contact residue. The potency of AP23464 against imatinib mesylate-refractory Bcr-Abl and its distinct binding mode relative to imatinib mesylate warr......

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.