SMALS-329
SMALS-329 is an LKB1 activator with EC50 = 8.5 μM. SMALS-329 binds to the ATP-binding pocket of STRADα and enhances the binding of the LKB1-STRAD-MO25 trimeric complex as well as the thermal stability of STRAD and LKB1. SMALS-329 enhances LKB1 kinase catalytic activity and promotes phosphorylation of downstream AMPK and SIK family substrates. SMALS-329 inhibits proliferation of multiple tumor cell lines harboring wild-type LKB1 and induces cell cycle arrest. SMALS-329 can be used for research on LKB1-related diseases, such as cancer.
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- CAS. Nr.: 2684270-22-0
- Formel: C23H27N4O6PS
- Molecular Weight:518.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
AMPK |
SIK1 |
QIK/SIK2 |
In Vitro
SMALS-329 competes with SMALS-c3 for binding to the ATP pocket of STRADα in the STRADα-MO25α dimer[1].
SMALS-329 (1.7-15 μM IP and 20 μM CETSA; 1 hour) stabilizes and increases the LKB1-STRAD-MO25 complex in A549 cells[1].
SMALS-329 (0.3-25 μM; 0-24 hours) activates LKB1-dependent AMPK and SIK phosphorylation in H358 cells[1].
SMALS-329 (8 μM) increases phosphorylation of LKB1 substrates in A549 cells only when LKB1 expression is restored[1].
SMALS-329 (8 μM) activates LKB1 effector signaling in ACHN and RL95-2 cells with cell line-dependent kinetics[1].
SMALS-329 (5 μM; co-administration) enhances the antiproliferative potency of the AKT inhibitor GSK2141795 (HY-15965) and the KRASG12C inhibitor Adagrasib (HY-130149) in sensitive tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H358 LKB1WT lung cancer cells
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Concentration:8 μM (0-24 h)
0.31, 0.93, 2.8, 8.3, 25 μM (4 h) -
Incubation Time:0, 15 min, 1 h, 4 h, 24 h (8 μM)
4 h (0.31-25 μM) -
Result:Observed that 8 μM SMALS-329 resulted in increased phosphorylation of AMPK1/2 and SIK1-3.
SIK phosphorylation peaked at 4 h and was maintained for 24 h, whereas AMPK phosphorylation was maximal at 15 min and returned to baseline by 24 h.
When the cells were subjected to doses of SMALS-329 ranging from 0.3 to 25 μM for 4 h, we observed dose-responsive activation up to 8.3 μM, with inhibition at the highest dose.
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Cell Line:ACHN cells
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Concentration:10 μM
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Incubation Time:12 days
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Result:Inhibited ACHN proliferation.
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Cell Line:ACHN cells
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Concentration:10 μM
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Incubation Time:120 h
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Result:induced G2/M‑phase cell‑cycle accumulation in sensitive cancer cell lines.
Chemical Information
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CAS. Nr. 2684270-22-0
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Molecular Weight 518.52
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Formel C23H27N4O6PS
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SMILES
CCOP(OCC)(CS(=O)(C1=CC=C(NC(C2=C(N=CC(C(C=C3)=CC=C3C)=N2)N)=O)C=C1)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SMALS-329 Related Classifications
HY-189758 Related Classifications
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