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GSK2141795 Catalog No.GC12305

pan-Akt inhibitor

Size Price Stock Qty
10 mM * 1 mL in DMSO
$97.00
Ship Within 10-14 Days
5mg
$89.00
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10mg
$144.00
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50mg
$510.00
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100mg
$667.00
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200mg
$1,159.00
Ship Within 10-14 Days

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1047634-65-0 SDF
Synonyms N/A
Chemical Name N-((S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide
Canonical SMILES CN1C(C(C=C(O2)C(N[C@@](CN)([H])CC3=CC(F)=C(F)C=C3)=O)=C2Cl)=C(Cl)C=N1
Formula C18H16Cl2F2N4O2 M.Wt 429.25
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

Uprosertib (GSK2141795) inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib (GSK2141795) in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

References:
[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
[2]. Jacobsen K, et al. Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer. Nat Commun. 2017 Sep 4;8(1):410.