1. Epigenetics
    PI3K/Akt/mTOR
    Autophagy
    Apoptosis
  2. AMPK
    Autophagy
    Apoptosis
  3. GSK621

GSK621 

Cat. No.: HY-100548 Purity: 98.82%
Handling Instructions

GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.

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

GSK621 Chemical Structure

GSK621 Chemical Structure

CAS No. : 1346607-05-3

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5 mg USD 135 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
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25 mg USD 450 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation[1].

In Vitro

GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation[1].
GSK621 (30 μM) induces autophagy and apoptosis[1].
GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells[1].

Cell Proliferation Assay[1]

Cell Line: MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 AML cell lines. 0-30 μM.
Concentration: 0-30 μM.
Incubation Time: 4 d.
Result: IC50 values ranged from 13 to 30 μM.
Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines.

Cell Autophagy Assay[1].

Cell Line: AML cell lines and primary AML samples.
Concentration: 30 μM.
Incubation Time: 24 h.
Result: Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes.
In Vivo

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft[1].

Animal Model: MOLM-14 cells xenografted into nude mice[1].
Dosage: 30 mg/kg.
Administration: IP twice daily.
Result: Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.
Molecular Weight

489.91

Formula

C₂₆H₂₀ClN₃O₅

CAS No.

1346607-05-3

SMILES

O=C1NC2=C(N(C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C(Cl)=C2)C(N1C5=CC=CC(OC)=C5)=O

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
References
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Keywords:

GSK621GSK 621GSK-621AMPKAutophagyApoptosisAMP-activated protein kinaseUPRER StressPERKATF4CHOPInhibitorinhibitorinhibit

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GSK621
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