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

XST-14 

Cat. No.: HY-137506
Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
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10 mg USD 450 In-stock
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25 mg USD 850 In-stock
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50 mg USD 1350 In-stock
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100 mg USD 1950 In-stock
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Based on 1 publication(s) in Google Scholar

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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]

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].

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].

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)

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
10 mM 0.3432 mL 1.7162 mL 3.4324 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

XST-14XST14XST 14ULKp38 MAPKTGF-β ReceptorALKCaMKUnc-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

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