1. PI3K/Akt/mTOR Stem Cell/Wnt Apoptosis Autophagy
  2. GSK-3 Apoptosis Autophagy
  3. 9-ING-41

9-ING-41  (Synonyms: Elraglusib)

Cat. No.: HY-113914 Purity: 99.13%
COA Handling Instructions

9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents.

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

9-ING-41 Chemical Structure

9-ING-41 Chemical Structure

CAS No. : 1034895-42-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
1 mg USD 41 In-stock
5 mg USD 132 In-stock
10 mg USD 220 In-stock
25 mg USD 462 In-stock
50 mg USD 740 In-stock
100 mg USD 1185 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents[1][2][3][4].

IC50 & Target[1]

GSK-3β

0.71 μM (IC50)

In Vitro

9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis[2].
9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2].
9-ING-41 (10 μM; for 72 hours) increases the expression of LC3, an autophagy marker[3].
9-ING-41 (compound 26; 5 μM; for 6, 12, 24, 36 h) results in a pronounced decrease in NFκB-mediated expression of XIAP, the most potent antiapoptotic protein, leading to subsequent apoptosis in BXPC3 pancreatic cancer cells[1].
9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM[2].
9-ING-41 (10 μM; for 72 hours) causes cell cycle blockage at G2/M after 24 hours. 9-ING-41 treatment induces apoptotic cell death in bladder cancer cells[3].
9-ING-41 (25 μM; for 96 hours) significantly decreases expression of Cdk1 and Cyclin B1 proteins and leads to a decreased expression of antiapoptotic molecules, Bcl-2 and XIAP[3].
9-ING-41 (0.1-1 µM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker[4].

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

Cell Viability Assay[2]

Cell Line: TCL and MCL lines
Concentration: 2, 4 μM
Incubation Time: 48 hours
Result: Induced apoptosis.

Cell Cycle Analysis[2]

Cell Line: Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines)
Concentration: 1, 2 μM
Incubation Time: 24 hours
Result: Led to cell cycle arrest in G2/M.

Cell Autophagy Assay[3]

Cell Line: T24 cancer cells
Concentration: 25 μM
Incubation Time: 24 hours
Result: Showed extensive vacuolation and formation of autophagosome like structures in the cytoplasm.
Showed an increased expression of LC3, an autophagy marker.

Western Blot Analysis[4]

Cell Line: SK-N-DZ and SK-N-BE neuroblastoma cells
Concentration: 0.1, 1 µM
Incubation Time: 48 hours
Result: Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP.
In Vivo

9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL[2].

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

Animal Model: NSG (NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ) mice[2]
Dosage: 40 mg/kg
Administration: Every other day; for 17 days
Result: Had single-agent antitumor activity in a mouse model of MCL.
Molecular Weight

404.35

Formula

C22H13FN2O5

CAS No.
Appearance

Solid

Color

Pink to red

SMILES

O=C(C(C1=COC2=CC=C(F)C=C12)=C3C4=CN(C)C5=C4C=C6C(OCO6)=C5)NC3=O

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 : 50 mg/mL (123.66 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 2.4731 mL 12.3655 mL 24.7310 mL
5 mM 0.4946 mL 2.4731 mL 4.9462 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.

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

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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 (6.18 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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: 99.13%

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 2.4731 mL 12.3655 mL 24.7310 mL 61.8276 mL
5 mM 0.4946 mL 2.4731 mL 4.9462 mL 12.3655 mL
10 mM 0.2473 mL 1.2366 mL 2.4731 mL 6.1828 mL
15 mM 0.1649 mL 0.8244 mL 1.6487 mL 4.1218 mL
20 mM 0.1237 mL 0.6183 mL 1.2366 mL 3.0914 mL
25 mM 0.0989 mL 0.4946 mL 0.9892 mL 2.4731 mL
30 mM 0.0824 mL 0.4122 mL 0.8244 mL 2.0609 mL
40 mM 0.0618 mL 0.3091 mL 0.6183 mL 1.5457 mL
50 mM 0.0495 mL 0.2473 mL 0.4946 mL 1.2366 mL
60 mM 0.0412 mL 0.2061 mL 0.4122 mL 1.0305 mL
80 mM 0.0309 mL 0.1546 mL 0.3091 mL 0.7728 mL
100 mM 0.0247 mL 0.1237 mL 0.2473 mL 0.6183 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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9-ING-41
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HY-113914
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