adenosine kinase

NITD008 (7-Deaza-2'-C-acetylene-adenosine) is a potent and selective adenosine nucleoside inhibitor.NITD008 is an adenosine nucleoside analog with broad-spectrum antiviral activity that inhibits dengue, animal cupripoxvirus, and Zika virus.

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

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.

Adenosine Kinase siRNA-2 is a small interfering RNA that targets adenosine kinase messenger RNA (mRNA).

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.

Ritodrine hydrochloride (NSC 291565) binds to and activates beta-2 adrenergic receptors of myometrial cells in the uterus, which decreases the intensity and frequency of uterine contractions. Ritodrine hydrochloride (NSC 291565) is a phenethylamine derivative with tocolytic activity. Specifically, Ritodrine hydrochloride (NSC 291565) probably activates adenyl cyclase, thereby increasing production of cyclic adenosine monophosphate (cAMP), which in turn enhances the efflux of calcium from vascular smooth muscle cells. A lack of intracellular calcium prevents uterine myometrial contractions. In addition, this agent may directly inactivate myosin light chain kinase, a critical enzyme necessary for the initiation of muscle contractions.

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.

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

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.

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.

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%.

Anisodine hydrobromide is an inhibitor of adenosine kinase.

Benzoadenosine suppresses kinase activity slightly less than does adenosine.

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.

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.

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.

ABT-702 is an orally active, competitive, and reversible non-nucleoside adenosine kinase (AK) inhibitor with an IC50 value of 1.7 nM, exhibiting analgesic and anti-inflammatory properties, and effectively reducing acute thermal pain in mice.

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

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.

RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1 2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf MEK ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.

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......

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

7-Methoxyisoflavone is an activator of adenosine monophosphate-activated protein kinase (AMPK).