77307-50-7 Usage
Description
SL0101, also known as SL0101-1, is a kaempferol glycoside derived from the tropical plant F. refracta. It is a potent and selective inhibitor of p90 Rsk, specifically RSK2, with an IC50 value of 89 nM (Ki = 1 μM). SL0101-1 does not interfere with upstream activators of RSK, such as ERK, MEK, EGFR, and PKC. It is a tan solid and has been used to study intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation.
Uses
Used in Pharmaceutical Industry:
SL0101 is used as a potent and selective inhibitor of p90 Rsk for targeting the RSK2 enzyme, which plays a role in various cellular processes. Its selectivity allows for specific inhibition without affecting upstream kinases such as MEK, Raf, or PKC.
Used in Cancer Research:
SL0101 is used in cancer research to study the effects of inhibiting RSK2 on the proliferation of cancer cells, such as MCF-7 breast cancer cells. At 100 μM, SL0101-1 arrests cells in the G1 phase of the cell cycle, providing insights into the potential use of RSK2 inhibition in cancer treatment.
Used in Signal Transduction Research:
SL0101 is used in signal transduction research to investigate the role of RSK2 in intracellular signaling events associated with angiotensin II-induced tyrosine kinase activation. A concentration of 30 μM attenuates angiotensin II-induced cell proliferation, offering a tool to study the underlying mechanisms of this process.
Biological Activity
Selective inhibitor of p90 ribosomal S6 kinase (RSK) (IC 50 = 89 nM for RSK2). Does not inhibit upstream kinases such as MEK, Raf and PKC.? Inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
Check Digit Verification of cas no
The CAS Registry Mumber 77307-50-7 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,7,3,0 and 7 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 77307-50:
(7*7)+(6*7)+(5*3)+(4*0)+(3*7)+(2*5)+(1*0)=137
137 % 10 = 7
So 77307-50-7 is a valid CAS Registry Number.
InChI:InChI=1/C25H24O12/c1-10-21(34-11(2)26)24(35-12(3)27)20(32)25(33-10)37-23-19(31)18-16(30)8-15(29)9-17(18)36-22(23)13-4-6-14(28)7-5-13/h4-10,20-21,24-25,28-30,32H,1-3H3/t10-,20+,21?,24?,25?/m0/s1
77307-50-7Relevant articles and documents
SYNTHESIS OF INHIBITORS OF P90RSK
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Page/Page column 5; 30; 35, (2008/06/13)
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Synthesis of a potent and selective inhibitor of p90 Rsk
Maloney, David J.,Hecht, Sidney M.
, p. 1097 - 1099 (2007/10/03)
(Chemical Equation Presented) The synthesis of the naturally occurring kaempferol glycoside SL0101 has been accomplished, as has its biochemical evaluation. SL0101 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthesis verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.