1. Autophagy MAPK/ERK Pathway TGF-beta/Smad Protein Tyrosine Kinase/RTK Neuronal Signaling Apoptosis
  2. ULK p38 MAPK TGF-β Receptor Anaplastic lymphoma kinase (ALK) CaMK Apoptosis
  3. XST-14

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.

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XST-14 Chemical Structure

XST-14 Chemical Structure

CAS No. : 2607143-50-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE XST-14

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Description

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects[1].

IC50 & Target[1]

CaMK II

 

ULK1

26.6 nM (IC50)

In Vitro

XST-14 inhibits ULK1 (IC50=13.6 nM), MAP2K1/MEK1 (IC50=721.8 nM), MAPK14/p38 alpha (IC50=283.9 nM), TGFBR2 (IC50=809.3 nM), ACVR1/ALK2 (IC50=183.8 nM), ULK2 (IC50=70.9 nM) and CAMK2A (IC50=66.3 nM) by the 10-point titration results from SelectScreen Kinase Profiling Services[1].
XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity[1].
XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells[1].
XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3[1].
XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1[1].

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

Cell Proliferation Assay[1]

Cell Line: HepG2 cells
Concentration: 20, 40, 60, 80 μM
Incubation Time: 24 hours
Result: Led a decrease in cell proliferation activity.

Apoptosis Analysis[1]

Cell Line: HepG2 and human primary cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Induced apoptosis in HepG2 and human primary HCC cells.

Cell Autophagy Assay[1]

Cell Line: CHO, HepG2 cells stably expressing GFP-LC3
Concentration: 5 μM
Incubation Time: 12 hours
Result: Strongly inhibited the conversion of LC3-I to LC3-II in CHO cells.
Dramatically decreased the number of GFP-LC3 puncta in HepG2 cells.
Decreased autophagosome formation and blocked autophagosome/lysosome fusion in HepG2 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 12 hours
Result: Inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.
In Vivo

XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice[1].
XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T1/2 of 2.31 hours for IV and a T1/2 of 2.69 hours for IP[1].

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

Animal Model: Nude mice bearing HepG2 tumor xenografts[1]
Dosage: 15, 30 mg/kg
Administration: IP; daily; for 4 consecutive weeks
Result: Displayed anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice.
Animal Model: Sprague-Dawley rat[1]
Dosage: 2 mg/kg for IV; 10 mg/kg for IP (Pharmacokinetic Analysis)
Administration: IV or IP
Result: Had a T1/2 of 2.31 hours, a CL of 26.28 mL/min•kg, and and an AUC of 1269 hr•ng/mL for IV.
Had a T1/2 of 2.69 hours, a Cmax of 2033 ng/mL, and an AUC of 5979 hr•ng/mL for IP.
Molecular Weight

291.34

Formula

C16H21NO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)C1=CC2=C(OC(C)C)C=C(OC(C)C)C=C2N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (858.10 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 3.4324 mL 17.1621 mL 34.3242 mL
5 mM 0.6865 mL 3.4324 mL 6.8648 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4324 mL 17.1621 mL 34.3242 mL 85.8104 mL
5 mM 0.6865 mL 3.4324 mL 6.8648 mL 17.1621 mL
10 mM 0.3432 mL 1.7162 mL 3.4324 mL 8.5810 mL
15 mM 0.2288 mL 1.1441 mL 2.2883 mL 5.7207 mL
20 mM 0.1716 mL 0.8581 mL 1.7162 mL 4.2905 mL
25 mM 0.1373 mL 0.6865 mL 1.3730 mL 3.4324 mL
30 mM 0.1144 mL 0.5721 mL 1.1441 mL 2.8603 mL
40 mM 0.0858 mL 0.4291 mL 0.8581 mL 2.1453 mL
50 mM 0.0686 mL 0.3432 mL 0.6865 mL 1.7162 mL
60 mM 0.0572 mL 0.2860 mL 0.5721 mL 1.4302 mL
80 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0726 mL
100 mM 0.0343 mL 0.1716 mL 0.3432 mL 0.8581 mL
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