Uprosertib hydrochloride
Based on 20 publication(s) in Google Scholar
Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
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- CAS. Nr.: 1047635-80-2
- Formel: C18H17Cl3F2N4O2
- Molecular Weight:465.71
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Uprosertib hydrochloride
More- Immunity. 2020 Jan 14;52(1):109-122.e6. [Abstract]
- Nat Commun. 2022 Nov 29;13(1):7345. [Abstract]
- Nat Commun. 2017 Sep 4;8(1):410. [Abstract]
- Cancer Biol Med. 2021 Mar 12;19(1):104-119. [Abstract]
- Clin Cancer Res. 2016 Nov 15;22(22):5514-5526. [Abstract]
- NPJ Precis Oncol. 2021 Jul 15;5(1):65. [Abstract]
- Cell Prolif. 2026 Apr 22:e70214. [Abstract]
- Mol Cancer Ther. 2017 Apr;16(4):614-624. [Abstract]
- Ecotoxicol Environ Saf. 2021 Sep 15:221:112447. [Abstract]
- Oncoimmunology. 2018 Aug 6;7(10):e1488565. [Abstract]
- Biol Proced Online. 2025 Oct 15;27(1):39. [Abstract]
- iScience. 2023 Jun 7;26(7):107025. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105641. [Abstract]
- Cell Biol Int. 2020 Feb;44(2):610-620. [Abstract]
- Biomed Res Int. 2019 May 16:2019:2821731. [Abstract]
- Meat and Muscle Biology. 2026.
- Research Square Preprint. 2021 Sep.
- Radboud University Nijmegen. 2019 Oct.
- Oncotarget. 2018 Jul 31;9(59):31549-31558. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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Biologische Aktivität
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Akt3 38 nM (IC50) |
Akt1 180 nM (IC50) |
Akt2 328 nM (IC50) |
ROCK1 1570 nM (IC50) |
ROCK2 1850 nM (IC50) |
CDK7 2100 nM (IC50) |
Uprosertib 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 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1047635-80-2
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Molecular Weight 465.71
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Formel C18H17Cl3F2N4O2
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SMILES
O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN.Cl
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Synonyms
GSK2141795 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (20)
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Journal Impact Factor
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Most Recent
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Immunity
Targeting 7-Dehydrocholesterol Reductase Integrates Cholesterol Metabolism and IRF3 Activation to Eliminate Infection. [Abstract]2020 Jan 14;52(1):109-122.e6. PMID: 31882361 -
Nat Commun
2022 Nov 29;13(1):7345. PMID: 36446858 -
Nat Commun
2017 Sep 4;8(1):410. PMID: 28871105
Uprosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Sep 4;8(1):410. [Abstract]
Effect of EGFR TKIs and Akt inhibitors on key signal transduction proteins in parental and resistant PC9 cells. Western blot analysis of PC9 and PC9-ER treated for 4 h with Erlotinib (30 µM), GSK2141795 (2.5 µM) or the combination.
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Cancer Biol Med
SNORA23 inhibits HCC tumorigenesis by impairing the 2'-O-ribose methylation level of 28S rRNA. [Abstract]2021 Mar 12;19(1):104-119. PMID: 33710804 -
Clin Cancer Res
High CDK6 Protects Cells from Fulvestrant-Mediated Apoptosis and is a Predictor of Resistance to Fulvestrant in Estrogen Receptor-Positive Metastatic Breast Cancer. [Abstract]2016 Nov 15;22(22):5514-5526. PMID: 27252418 -
NPJ Precis Oncol
Combined FGFR and Akt pathway inhibition abrogates growth of FGFR1 overexpressing EGFR-TKI-resistant NSCLC cells. [Abstract]2021 Jul 15;5(1):65. PMID: 34267282 -
Cell Prolif
Targeting Egfr-Mediated Cell Proliferation and Lipid Metabolism Separation Effectively Accelerate Liver Regeneration. [Abstract]2026 Apr 22:e70214. PMID: 42019507 -
Mol Cancer Ther
Akt Activation Mediates Acquired Resistance to Fibroblast Growth Factor Receptor Inhibitor BGJ398. [Abstract]2017 Apr;16(4):614-624. PMID: 28255027
Uprosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Apr;16(4):614-624. [Abstract]
Western blot analysis is performed with lysates from resistant cell lines treated either with vehicle (DMSO) or GSK2141795 (1 μM) for 24 hours to assess inhibition of Akt (pAKT) and downstream (pGSK3) signaling (three experimental replicates).
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Ecotoxicol Environ Saf
Clusterin inhibits Cr(VI)-induced apoptosis via enhancing mitochondrial biogenesis through AKT-associated STAT3 activation in L02 hepatocytes. [Abstract]2021 Sep 15:221:112447. PMID: 34175824 -
Oncoimmunology
Ex vivo AKT-inhibition facilitates generation of polyfunctional stem cell memory-like CD8+ T cells for adoptive immunotherapy. [Abstract]2018 Aug 6;7(10):e1488565. PMID: 30288356 -
Biol Proced Online
Rap2B-mediated reprogramming of the PI3K/AKT signaling axis drives resistance to cetuximab-targeted therapy in colorectal carcinoma. [Abstract]2025 Oct 15;27(1):39. PMID: 41094393 -
iScience
Resistin targets TAZ to promote osteogenic differentiation through PI3K/AKT/mTOR pathway. [Abstract]2023 Jun 7;26(7):107025. PMID: 37389179 -
J Biol Chem
Disruption of lysosomal nutrient sensing scaffold contributes to pathogenesis of a fatal neurodegenerative lysosomal storage disease. [Abstract]2024 Feb;300(2):105641. PMID: 38211816 -
Cell Biol Int
Reversing microtubule-directed chemotherapeutic drug resistance by co-delivering α2β1 inhibitor and paclitaxel with nanoparticles in ovarian cancer. [Abstract]2020 Feb;44(2):610-620. PMID: 31743535 -
Biomed Res Int
MiR-21-3p Plays a Crucial Role in Metabolism Alteration of Renal Tubular Epithelial Cells during Sepsis Associated Acute Kidney Injury via AKT/CDK2-FOXO1 Pathway. [Abstract]2019 May 16:2019:2821731. PMID: 31223614 -
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Oncotarget
Deep analysis of acquired resistance to FGFR1 inhibitor identifies MET and AKT activation and an expansion of AKT1 mutant cells. [Abstract]2018 Jul 31;9(59):31549-31558. PMID: 30140389
Uprosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jul 31;9(59):31549-31558. [Abstract]
Western blots of the indicated proteins in the DMS114-P and DMS114-R cells treated with (+) and without (-) the AKT inhibitor, Uprosertib (200 nM) for 6 h (left panel) or 24 h (right panel). In the case of DMS114-P, extracts with (+) and without (-) treatment with PD173074 (1 µM) are also shown.
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Protokoll
For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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