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STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.

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

STK16-IN-1 Chemical Structure

STK16-IN-1 Chemical Structure

CAS No. : 1223001-53-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.

IC50 & Target

IC50: 295 nM (STK16)[1]

In Vitro

STK16-IN-1, which exhibits potent inhibitory activity against STK16 kinase (IC50=0.295 μM) with excellent selective across the kinome as assessed using the KinomeScanTM profiling assay. STK16-IN-1 inhibits mTOR kinase with an IC50 of 5.56 μM. In MCF-7 cells, treatment with STK16-IN-1 results in a reduction in cell number and accumulation of binucleated cells, which can be recapitulated by RNAi knockdown of STK16. Co-treatment of STK16-IN-1 with chemotherapeutics such as cisplatin, doxorubicin, colchicine and paclitaxel results in a slight potentiation of the anti-proliferative effects of the chemotherapeutics. STK16-IN-1 provides a useful tool compound for further elucidating the biological functions of STK16)[1].

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

Molecular Weight

293.30

Formula

C17H12FN3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(N2C(C(C=CC2=O)=CN3)=C4C3=NC=C4)C=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (51.14 mM; Need ultrasonic and warming; 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 3.4095 mL 17.0474 mL 34.0948 mL
5 mM 0.6819 mL 3.4095 mL 6.8190 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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 (8.52 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.52 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.

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
References
Kinase Assay
[1]

STK16-IN-1 is generally prepared with 1:3 serial dilutions for 4 concentrations (100 nM, 50 nM, 20 nM, and 10 nM); 6 concentrations are used (1 mM to 10 μM) for ATP competition experiments. The kinase reaction is performed with 1×kinase reaction buffer. Reactions in each well are started immediately by adding ATP and kept going for half an hour under 37°C. After the plate cooled for 5 minutes at room temperature, 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ADP within 40 minutes. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 1 hour to produce a luminescence signal[1].

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

Cell Assay
[1]

MCF-7, HCT116, HeLa cells are treated with STK16-IN-1 (0, 5, 10 μM) for 72 hours and apoptotic cells are analyzed by flow cytometry using Annexin V/PI apoptosis detection kit[1].

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4095 mL 17.0474 mL 34.0948 mL 85.2370 mL
5 mM 0.6819 mL 3.4095 mL 6.8190 mL 17.0474 mL
10 mM 0.3409 mL 1.7047 mL 3.4095 mL 8.5237 mL
15 mM 0.2273 mL 1.1365 mL 2.2730 mL 5.6825 mL
20 mM 0.1705 mL 0.8524 mL 1.7047 mL 4.2618 mL
25 mM 0.1364 mL 0.6819 mL 1.3638 mL 3.4095 mL
30 mM 0.1136 mL 0.5682 mL 1.1365 mL 2.8412 mL
40 mM 0.0852 mL 0.4262 mL 0.8524 mL 2.1309 mL
50 mM 0.0682 mL 0.3409 mL 0.6819 mL 1.7047 mL
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  • 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.

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Product Name:
STK16-IN-1
Cat. No.:
HY-101270
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