Adenosine Kinase Inhibitor

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.

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

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.

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.

Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC₅₀ values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC₅₀ values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its K_i for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer.

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.

Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC₅₀ values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC₅₀ values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its K_i for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer.

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.

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.

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.

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

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.

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.

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).