5-Iodotubercidin (Synonyms: NSC 113939; 5-ITu)

Name: 5-Iodotubercidin
Brand: MedChemExpress
SKU: HY-15424
Rating: 5.0 (8 reviews)

Cat. No.: HY-15424 Purity: 99.64%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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5-Iodotubercidin Chemical Structure

CAS No. : 24386-93-4

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Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE 5-Iodotubercidin

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Protocol
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Description

IC₅₀ & Target

IC50: 26 nM (adenosine kinase)

In Vitro

5-Iodotubercidin (NSC 113939) inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC, and the IC₅₀ values are 0.4, 3.5, 5-10, 5-10, 10.9 and 27.7 μM respectively^[1].
? 5-Iodotubercidin (20 μM) causes an important decrease in ATP concentration, and a concomitant smaller increase in AMP concentration. 5-Iodotubercidin decreases the activity of ACC and the rates of synthesis of fatty acids and cholesterol. In line with the iodotubercidin-mediated inhibition of ACC, 5-iodotubercidin induces a marked decrease in the intracellular concentration of malonyl-CoA^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

5-Iodotubercidin (1 mL/kg, i.p.) is in agreement with activity observed against bicuculline-induced seizures following local administration of the AKI into the prepiriform cortex^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

392.15

Formula

C₁₁H₁₃IN₄O₄

CAS No.

24386-93-4

Appearance

Solid

Color

White to gray

SMILES

NC1=C2C(N([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C=C2I)=NC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (63.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5500 mL	12.7502 mL	25.5004 mL
5 mM	0.5100 mL	2.5500 mL	5.1001 mL
10 mM	0.2550 mL	1.2750 mL	2.5500 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.28 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (285 KB) SDS (394 KB)

COA (254 KB) RP-HPLC (243 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Massillon D, et al. Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor. Biochem J. 1994 Apr 1;299 (Pt 1):123-8. [Content Brief]

[2]. Ugarkar BG, et al. Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues. J Med Chem. 2000 Jul 27;43(15):2883-93. [Content Brief]

[3]. García-Villafranca J, et al. Effects of 5-iodotubercidin on hepatic fatty acid metabolism mediated by the inhibition of acetyl-CoA carboxylase. Biochem Pharmacol. 2002 Jun 1;63(11):1997-2000. [Content Brief]

[4]. De Antoni A, et al. A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B. J Cell Biol. 2012 Oct 15;199(2):269-84. [Content Brief]

[5]. Acharya MM, et al. Adenosine Kinase Inhibition Protects against Cranial Radiation-Induced Cognitive Dysfunction. Front Mol Neurosci. 2016 Jun 3;9:42. [Content Brief]

Kinase Assay ^[2]	AK activity is measured in a radiochemical assay. The final reaction volume is 100 µL and contained 70 mM Tris-maleate (pH 7.0), 0.1% (w/v) bovine serum albumin, 1.0 mM MgCl₂, 1.0 mM ATP, 1.0 µM [U-¹⁴C]adenosine (400-600 mCi/mmol) and various inhibitor concentrations. Inhibitors are prepared as 10 mM stock solutions in DMSO. The final DMSO concentration in the assay is 5% (v/v). Eleven different concentration of the test solutions ranging from 0.001 to 10.0 µM are utilized to determine a dose response curve of the inhibition of the enzyme. Reactions are started by adding the appropriate amount of purified human recombinant AK and incubated for 20 min at 37°C. The reactions are terminated by addition of the potent AKI GP3269. A 30-µL aliquot of each reaction is spotted on DEAE cellulose filter paper (cut in squares of appr 1×1 cm) and air-dried for 30 min. The dry filters are then washed for 3 min in deionized water to remove residual [U-¹⁴C]adenosine, rinsed with ethanol and dried at 90°C for 20 min. The filter papers are counted in 5.5 mL of Ready Safe liquid scintillation cocktail using a Beckman LS3801 scintillation counter. Control AK activity is determined from the amount of [¹⁴C]AMP formed in the presence of 5% DMSO. The concentration of inhibitor required to inhibit 50% of the AK activity (IC₅₀) is determined graphically from plots of inhibitor concentration versus percent (%) control enzyme activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[4]	HeLa cells are grown in DME supplemented with 10% fetal bovine serum (FBS) and 2 mM l-glutamine. Nocodazole is used at a concentration of 3.3 µM unless differently specified. Thymidine (2.5 mM) is used in the asssay. For transfection, FuGENE 6 Transfection Agent is used at a 3:1 ratio with plasmid DNA. Cells are analyzed 24-48 h after transfection. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Male SA rats (100-150 g) are maintained on a 12:12 light:dark cycle in temperaturecontrolled facilities with free access to food and water. One hour prior to seizure testing, the animals are injected intraperitoneally (1 mL/kg) with DMSO vehicle or with test compound dissolved in DMSO. At the time of the test, an electrolyte solution (2% lidocaine in 0.9% sodium chloride) is applied to the eyes. Maximal electroshock seizures are induced by administering a 60-Hz current of 150 mA for 0.2 s via corneal electrodes, using a Wahlquist Model H stimulator. The endpoint measured is suppression of hindlimb tonic extension (HTE) and expressed as percentage of animals in which the response is inhibited. At this supramaximal stimulation level, virtually 100% of control (vehicle-treated) animals show HTE. ED₅₀ values are calculated from a dose-response curve using probit analysis. The N for the screening doses is 6-8; doseresponse determinations are conducted with at least 5 animals/dose. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Massillon D, et al. Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor. Biochem J. 1994 Apr 1;299 (Pt 1):123-8. [Content Brief] [2]. Ugarkar BG, et al. Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues. J Med Chem. 2000 Jul 27;43(15):2883-93. [Content Brief] [3]. García-Villafranca J, et al. Effects of 5-iodotubercidin on hepatic fatty acid metabolism mediated by the inhibition of acetyl-CoA carboxylase. Biochem Pharmacol. 2002 Jun 1;63(11):1997-2000. [Content Brief] [4]. De Antoni A, et al. A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B. J Cell Biol. 2012 Oct 15;199(2):269-84. [Content Brief] [5]. Acharya MM, et al. Adenosine Kinase Inhibition Protects against Cranial Radiation-Induced Cognitive Dysfunction. Front Mol Neurosci. 2016 Jun 3;9:42. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5500 mL	12.7502 mL	25.5004 mL	63.7511 mL
	5 mM	0.5100 mL	2.5500 mL	5.1001 mL	12.7502 mL
	10 mM	0.2550 mL	1.2750 mL	2.5500 mL	6.3751 mL
	15 mM	0.1700 mL	0.8500 mL	1.7000 mL	4.2501 mL
	20 mM	0.1275 mL	0.6375 mL	1.2750 mL	3.1876 mL
	25 mM	0.1020 mL	0.5100 mL	1.0200 mL	2.5500 mL
	30 mM	0.0850 mL	0.4250 mL	0.8500 mL	2.1250 mL
	40 mM	0.0638 mL	0.3188 mL	0.6375 mL	1.5938 mL
	50 mM	0.0510 mL	0.2550 mL	0.5100 mL	1.2750 mL
	60 mM	0.0425 mL	0.2125 mL	0.4250 mL	1.0625 mL

5-Iodotubercidin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

5-Iodotubercidin24386-93-4NSC 113939 5-ITuNSC113939NSC-113939Adenosine KinaseADKInhibitorinhibitorinhibit

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5-Iodotubercidin (Synonyms: NSC 113939; 5-ITu)

Customer Review

5-Iodotubercidin Related Antibodies

8 Publications Citing Use of MCE 5-Iodotubercidin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

5-Iodotubercidin Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

5-Iodotubercidin Related Classifications

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