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GW406108X

Cat. No. M9851
GW406108X Structure
Synonym:

GW108X

Size Price Availability Quantity
5mg USD 225  USD225 In stock
10mg USD 360  USD360 In stock
25mg USD 685  USD685 In stock
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Quality Control & Documentation
Biological Activity

GW406108X is a potent autophagy inhibitor, with a pIC50 6.37 (427 nM) against ULK1. GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signalling kinases mTORC1 and AMPK. GW406108X inhibits VPS34 and AMPK with pIC50 of 6.34 (457 nM) and 6.38 (417 nM), respectively.

Chemical Information
Molecular Weight 400.21
Formula C20H11Cl2NO4
CAS Number 1644443-92-4
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Maria Zachari, et al. Biochem J. The identification and characterisation of autophagy inhibitors from the published kinase inhibitor sets

[2] Megan E Dumas, et al. Bioorg Med Chem Lett. Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes

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Keywords: GW406108X, GW108X supplier, Autophagy, inhibitors, activators


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