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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 146 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 135 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

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.
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
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (25.51 mM; ultrasonic and adjust pH to 1 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0412 mL 10.2060 mL 20.4119 mL
5 mM 0.4082 mL 2.0412 mL 4.0824 mL
10 mM 0.2041 mL 1.0206 mL 2.0412 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  50% PEG300    50% saline

    Solubility: 10 mg/mL (20.41 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.25 mg/mL (2.55 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (2.55 mM); Suspended solution

  • 4.

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

    Solubility: ≥ 1.25 mg/mL (2.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • 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.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK621GSK 621GSK-621AMPKAutophagyApoptosisAMP-activated protein kinaseUPRER StressPERKATF4CHOPInhibitorinhibitorinhibit

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:
GSK621
Cat. No.:
HY-100548
Quantity:
MCE Japan Authorized Agent: