LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation.LY2584702 exhibited anti-tumour activity in preclinical analysis.
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Source | PLoS One (2017). Figure 1. LY2584702 |
| Method | Isolation of human neutrophils and cell stimulations | |
| Cell Lines | human neutrophils cell | |
| Concentrations | 10 μM | |
| Incubation Time | 5 minutes | |
| Results | This led to a decrease in 20-OH- and 20-COOH-LTB4 levels, and an increase in LTB4 levels. In contrast, LY2584702 did not prevent the metabolism of LTB4 into 20-OH- and 20-COOH-LTB4 in thapsigargin-stimulated neutrophils |
| Molecular Weight | 445.42 |
| Formula | C21H19F4N7 |
| CAS Number | 1082949-67-4 |
| Solubility (25°C) | DMSO > 4.5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related S6 Kinase Products |
|---|
| S6K1-IN-DG2
S6K1-IN-DG2 is a p70S6K inhibitor (IC50: < 100 nM). |
| BRD7389
BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells. |
| M2698
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity. |
| Bisindolylmaleimide V
Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 µM. Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 of 8 µM. |
| S6K-18
S6K-18 is a highly selective inhibitor of ribosomal protein S6 kinase beta-1 (S6K1, p70S6K, p70-S6K). |
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