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SL 0101-1

Cat. No. M3200
SL 0101-1 Structure
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50mg USD 620 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 516.45
Formula C25H24O12
CAS Number 77307-50-7
Purity >98%
Solubility DMSO
Storage at -20°C
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Abmole Inhibitor Catalog 2017

Keywords: SL 0101-1 supplier, S6 Kinase, inhibitors

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