2. Autophagy MAPK/ERK Pathway TGF-beta/Smad Protein Tyrosine Kinase/RTK Neuronal Signaling Apoptosis
  3. ULK p38 MAPK TGF-β Receptor Anaplastic lymphoma kinase (ALK) CaMK Apoptosis
  4. 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.

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

XST-14 Chemical Structure

XST-14 Chemical Structure

CAS No. : 2607143-50-8

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 163 In-stock
Solution
10 mM * 1 mL in DMSO USD 163 In-stock
Solid
5 mg USD 148 In-stock
10 mg USD 222 In-stock
25 mg USD 400 In-stock
50 mg USD 600 In-stock
100 mg USD 900 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

XST-14 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE XST-14

View All ULK Isoform Specific Products:

View All Isoforms
ULK1 ULK2

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

View All CaMK Isoform Specific Products:

View All Isoforms
CaMK III CaMK II

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

XST-14 Related Antibodies

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.

  • 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    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:

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

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

XST-14 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:

XST-142607143-50-8XST14XST 14ULKp38 MAPKTGF-β ReceptorAnaplastic lymphoma kinase (ALK)CaMKApoptosisUnc-51 like kinaseTransforming growth factor beta receptorsAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Calmodulin-dependent protein kinasesCalmodulin-dependent kinasesHepG2LC3-ILC3-IICHOGFP-LC3Ser249PIK3C3Ser15BECN1MAP2K1/MEK1MAPK14/p38TGFBR2ACVR1/ALK2ULK2CAMK2AInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
XST-14
Cat. No.:
HY-137506
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.