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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 |
| Related S6 Kinase Products |
|---|
| BI-D1870
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of the p90 RSK (ribosomal S6 kinase) with IC50 values of 31 nM, 24 nM, 18 nM, 15 nM for RSK1, RSK2, RSK3, RSK4, respectively. |
| PF-4708671
PF-4708671 is a novel cell-permeable inhibitor of S6K1 with Ki/IC50 value of 20 nM/160 nM. PF4708671 inhibits MSK1 (IC50 of 0.95 μM) 4-fold more weakly than S6K1. |
| FMK
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants. |
| Quercitrin
Quercitrin (Quercitrin) is a natural compound in bitter buckwheat, which has anti-inflammatory effects and has the potential to be used in cardiovascular disease research. |
| LY2584702
LY2584702 is a selective, ATP-competitive p70 S6 kinase inhibitor with IC50 of 4 nM. |
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