1047635-80-2
1047635-80-2 structure
- Name: GSK2141795 (hydrochloride)
- Chemical Name: N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide,hydrochloride
- CAS Number: 1047635-80-2
- Molecular Formula: C18H17Cl3F2N4O2
- Molecular Weight: 465.70900
- Catalog: Research Areas Cancer
- Create Date: 2016-09-26 20:36:53
- Modify Date: 2024-01-02 20:27:02
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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.
| Name | N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide,hydrochloride |
|---|---|
| Synonyms |
Uprosertib hydrochloride
UNII-50IE5H22B2 GSK2141795 (hydrochloride) |
| Description | 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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| Related Catalog | |
| Target |
Akt1:180 nM (IC50) Akt2:328 nM (IC50) Akt3:38 nM (IC50) CDK7:2100 nM (IC50) ROCK1:1570 nM (IC50) ROCK2:1850 nM (IC50) |
| In Vitro | 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]. |
| Kinase Assay | 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. |
| References |
| Molecular Formula | C18H17Cl3F2N4O2 |
|---|---|
| Molecular Weight | 465.70900 |
| Exact Mass | 464.03900 |
| PSA | 86.08000 |
| LogP | 5.45810 |
| Storage condition | 2-8℃ |