Adenosine Kinase

ADK

Adenosine Kinase

Related Products

Adenosine kinase (AK) is a cytosolic enzyme that catalyzes the conversion of adenosine to AMP. One potential adenosine regulating agent (ARA) target is adenosine kinase. Adenosine kinase activation represents the major clearance route of adenosine and is partly responsible for its extremely short plasma half-life (<1 s). Inhibition of adenosine kinase results in increased intracellular adenosine which passes out of the cell via passive diffusion or via nucleoside transporter(s) to activate nearby cell-surface adenosine receptors. Thus, adenosine kinase inhibition can represent an alternative mechanism for activation of adenosine receptors and production of adenosine-associated pharmacologies.

Adenosine kinase inhibitors (AKIs) represent an alternative strategy, since AKIs may raise local adenosine levels in a more site- and event-specific manner and thereby elicit the desired pharmacology with a greater therapeutic window. Several potent AKIs are shown to exhibit anticonvulsant activity in the rat maximal electric shock (MES) induced seizure assay.

Adenosine Kinase Related Products (14)
Antibodies (1)

By Effects:	Inhibitors (12) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-15424

5-Iodotubercidin	Inhibitor	99.95%
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC₅₀ of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.

HY-103161

ABT-702 dihydrochloride	Inhibitor	99.45%
ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC₅₀=1.7 nM).

HY-148327

AK-IN-1	Inhibitor	99.21%
AK-IN-1 (compound 4072-2732) is an adenosine kinase (AK) inhibitor that is competitive for adenosine (Ado) but not for ATP. AK-IN-1 inhibits 86%, 87% and 89% of AK activity at concentrations of 2, 4 and 10 µM, respectively. AK-IN-1 has good potential for research in many disease areas, including ischaemia, inflammation and seizures.

HY-112482

ABT-702	Inhibitor	99.61%
ABT-702 (Adenosine Kinase Inhibitor) is a potent, orally active, and selective adenosine kinase (AK) inhibitor with an IC₅₀ of 1.7 nM. ABT-702 shows >1300-fold selectivity for AK over other biological targets, including cyclooxygenases-1 and -2. ABT-702 attenuates inflammation in diabetic retinopathy by increasing free adenosine levels. ABT-702 shows analgesic and anti-inflammatory effects in vivo. ABT-702 can be used for diabetic retinopathy research.

HY-179690

Antiparasitic agent-30	Activator
Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC₅₀=38 nM, K_a=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness).

HY-182503

GP515	Inhibitor
GP515 is a potent and selective adenosine kinase inhibitor with a human IC₅₀ of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC₅₀ of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock.

HY-183362

Antileishmanial agent-42
Antileishmanial agent-42 is an antileishmanial agent. Antileishmanial agent-42 has favorable interactions with key active site residues (e.g., Ser63, Asn66/295/299) of adenosine kinase. Antileishmanial agent-42 exerts activity against promastigote and amastigote forms of L. amazonensis, L. braziliensis, L. infantum, and L. donovani.

HY-112482A

ABT-702 hydrochloride	Inhibitor	98.29%
ABT-702 hydrochloride is a potent, orally active, and selective adenosine kinase (AK) inhibitor with an IC₅₀ of 1.7 nM. ABT-702 hydrochloride shows >1300-fold selectivity for AK over other biological targets, including cyclooxygenases-1 and -2. ABT-702 hydrochloride attenuates inflammation in diabetic retinopathy by increasing free adenosine levels. ABT-702 hydrochloride shows analgesic and anti-inflammatory effects in vivo. ABT-702 hydrochloride can be used for diabetic retinopathy research.

HY-114901

A-134974	Inhibitor
A-134974 is a novel, high-selectivity adenosine kinase (IC₅₀ = 60 pM) inhibitor. A-134974 enhances endogenous adenosine signaling in the spinal cord, effectively alleviates neuropathic pain, and does not cause movement disorders. A-134974 can be used for the study of neuropathic pain.

HY-19259

GP3269	Inhibitor
GP3269 is a selective and orally active human adenosine kinase (AK) inhibitor with an IC₅₀ of 11 nM against human adenosine kinase. GP3269 increases adenosine levels at epileptic foci, activates A1 receptors on excitatory neurons, and exhibits anticonvulsant activity in rats. GP3269 does not induce hemodynamic effects including changes in blood pressure or heart rate in rats. GP3269 can be used for epilepsy-related research.

HY-145654

MRS-4203	Inhibitor
MRS-4203 is an ADK (IC₅₀ = 88 nM) inhibitor. MRS-4203 can reduce DNA methylation. MRS-4203 is commonly used in cancer research.

HY-15424R

5-Iodotubercidin (Standard)	Inhibitor
5-Iodotubercidin (Standard) is the analytical standard of 5-Iodotubercidin. This product is intended for research and analytical applications. 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.

HY-116005

A-286501	Inhibitor
A-286501 is an orally active and potent carbocyclic nucleoside adenosine kinase inhibitor with an IC₅₀ value of 0.47 nM, which shows analgesic and anti-inflammatory effects. A-286501 reduces nociception in animal models of acute (thermal), inflammatory (formalin and carrageenan) and neuropathic (L5/L6 nerve ligation and streptozotocin-induced diabetic) pain. A-286501 also reduces Carrageenan (HY-125474)-induced paw edema and myeloperoxidase activity in the injured paw. A-286501 is promising for research of analgesic and anti-inflammatory agents.

HY-103161R

ABT-702 dihydrochloride (Standard)	Inhibitor
ABT-702 dihydrochloride (Standard) is the analytical standard of ABT-702 dihydrochloride (HY-103161). This product is intended for research and analytical applications. ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC₅₀=1.7 nM).

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Adenosine Kinase

Adenosine Kinase

Adenosine Kinase Related Products (14)

Antibodies (1)

Adenosine Kinase Related Products (14):