1. Cytoskeleton
    Cell Cycle/DNA Damage
    Autophagy
  2. Kinesin
    ULK
    Autophagy
  3. GW406108X

GW406108X (Synonyms: GW108X)

Cat. No.: HY-115570 Purity: 96.02%
Handling Instructions

GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signalling kinases mTORC1 and AMPK.

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

GW406108X Chemical Structure

GW406108X Chemical Structure

CAS No. : 1644443-92-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signalling kinases mTORC1 and AMPK[1][2].

In Vitro

GW406108X acts upon ULK1 and autophagy without affecting mTOR or AMPK activity as shown by monitoring ULK1 pS758 (mTOR site) or pS556 (AMPK site) levels. GW406108X inhibits VPS34 and AMPK with pIC50 of 6.34 (457 nM) and 6.38 (417 nM), respectively. In the presence of 5 µΜ GW406108X, the starvation-induced increase in ATG13 phosphorylation is significantly reduced[1].
GW406108X inhibits Kif15-N420 ATPase activity by 76%[2].

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

Molecular Weight

400.21

Formula

C₂₀H₁₁Cl₂NO₄

CAS No.

1644443-92-4

SMILES

O=C1NC2=C(C=C(C(C3=CC=CO3)=O)C=C2)/C1=C/C4=CC(Cl)=C(O)C(Cl)=C4

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 : 50 mg/mL (124.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4987 mL 12.4934 mL 24.9869 mL
5 mM 0.4997 mL 2.4987 mL 4.9974 mL
10 mM 0.2499 mL 1.2493 mL 2.4987 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 2.08 mg/mL (5.20 mM); Suspended solution; Need ultrasonic

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

GW406108XGW108XKinesinULKAutophagyUnc-51 like kinaseautophagicfluxATPcompetitiveU2OScellsInhibitorinhibitorinhibit

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GW406108X
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