SL 0101-1 is a selective p90 ribosomal S6 kinase (RSK) inhibitor for RSK2 with an IC50 of 89 nM. The IC50 of kaempferol, the flavonoid constituent of SL 0101-1, is 15 μM for RSK. The rhamnose moiety of SL 0101-1 increases the affinity for RSK by >150-fold. Purified SL 0101-1 is specific for inhibition of RSK activity compared with that of p70 S6K and MSK1.SL 0101-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. Prevention of RSK by SL 0101-1 could occur through interaction with either the NTKD or the CTKD. SL 0101-1 effectively inhibits the isolated RSK2 NTKD. SL 0101-1 is much less effective in suppressing the mutant in comparison with wild-type RSK2 or wild-type RSK1. Additionally, prevention of RSK by SL 0101-1 occurs through competition with ATP for the nucleotide-binding site of the NTKD and further attests to the specificity of SL 0101-1. SL 0101-1 is membrane permeable and is effective in intact cells. SL 0101-1 does not affect the phosphorylation of RSK2. SL 0101-1 inhibits proliferation of the MCF-7 line with an efficacy paralleling its ability to inhibit RSK in intact cells but has no effect on the growth of the normal breast cell line MCF-10A. SL 0101-1 is not toxic and preferentially inhibits the growth of the breast cancer cell line relative to that of the normal breast cell line.
| Molecular Weight | 516.45 |
| Formula | C25H24O12 |
| CAS Number | 77307-50-7 |
| Solubility (25°C) | DMSO |
| 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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