Ro-31-8220
3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC; IC50 = 10 nM) over CaM kinase II (IC50 = 17 µM) and protein kinase A (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3β immunoprecipitates (IC50 = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC50 = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 µg/181 µl) solution of Ro-31-8220 (Cat. No. 557521) in H2O is also available.
產(chǎn)品信息
Form  Red solid
Primary Target  PKC
Primary Target IC50  10 nM
Secondary target  CaM kinase II (IC50 = 17 µM), PKA (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3β immunoprecipitates (IC50 = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells.
Molar mass  553.7
Protect from Light  是的
Hygrocopic  是的
Cell permeable  是的
Purity  ≥95% by HPLC
Solubility  DMSO or H2O
Chemical formula  C25H23N5O2S · CH4O3S
CAS number  138489-18-6
商店和運(yùn)輸信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling