2. Metabolic Enzyme/Protease Neuronal Signaling
  3. Adenosine Kinase
  4. 5-Iodotubercidin

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

Cat. No.: HY-15424 Purity: 99.64%
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.

For research use only. We do not sell to patients.

5-Iodotubercidin Chemical Structure

5-Iodotubercidin Chemical Structure

CAS No. : 24386-93-4

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Customer Review

Based on 8 publication(s) in Google Scholar

5-Iodotubercidin Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

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.

5-Iodotubercidin Related Antibodies
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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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%

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

Handling Instructions (2659 KB)
References
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

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.

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
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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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