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Bisindolylmaleimide IX . methanesulfonate

CHF 80.00
In stock
AG-CR1-0111-M0011 mgCHF 80.00
AG-CR1-0111-M0055 mgCHF 240.00
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Product Details
Synonyms Ro 31-8220; BIM IX
Product Type Chemical
Properties
Formula

C25H23N5O2S . CH4O3S

MW 457.6 . 96.1
CAS 138489-18-6
Purity Chemicals ≥98% (NMR)
Appearance Red solid.
Solubility Soluble in DMSO.
Identity Determined by 1H-NMR.
InChi Key SAWVGDJBSPLRRB-UHFFFAOYSA-N
Smiles CS(O)(=O)=O.CN1C=C(C2=C1C=CC=C2)C1=C(C(=O)NC1=O)C1=CN(CCCSC(N)=N)C2=C1C=CC=C2
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Store solutions at -20°C in the dark.
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Product Specification Sheet
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Description
    • Selective and cell permeable protein kinase C (PKC) inhibitor [1, 2, 3].
    • Inhibits the stimulation of insulin secretion by glucose [4, 11].
    • Inhibits T cell activation [5].
    • Apoptosis inducer [6, 8, 9,10, 13].
    • Potent glycogen synthase kinase-3 (GSK-3) inhibitor [7].
    • Transcription inhibitor [9].
    • Induces TNF receptor family-mediated cell death [10].
    • Pim-1 kinase inhibitor [12].
    • Antitumor compound [13].
    Product References
    1. Potent selective inhibitors of protein kinase C: P.D. Davis, et al.; FEBS Lett. 259, 61 (1989)
    2. RO 31-8220 and RO 31-7549 show improved selectivity for protein kinase C over staurosporine in macrophages: P. Dieter & E. Fitzke; BBRC 181, 396 (1991)
    3. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C: S.E. Wilkinson, et al.; Biochem. J. 294, 335 (1993)
    4. Inhibition of glucose-stimulated insulin secretion by Ro 31-8220, a protein kinase C inhibitor: S.J. Persaud & P.M. Jones; Endocrine 3, 285 (1995)
    5. RO 31-8220, a novel protein kinase C inhibitor, inhibits early and late T cell activation events: L. Geiselhart, et al.; Transplantation 61, 1637 (1996)
    6. Induction of apoptosis in glioblastoma cells by inhibition of protein kinase C and its association with the rapid accumulation of p53 and induction of the insulin-like growth factor-1-binding protein-3: L. Shen & R.I. Glazer; Biochem. Pharmacol. 55, 1711 (1998)
    7. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity: I. Hers, et al.; FEBS Lett. 460, 433 (1999)
    8. The staurosporine analog, Ro-31-8220, induces apoptosis independently of its ability to inhibit protein kinase C: Z. Han, et al.; Cell Death Differ. 7, 521 (2000)
    9. Bisindolylmaleimide IX facilitates tumor necrosis factor receptor family-mediated cell death and acts as an inhibitor of transcription: O.W. Rokhlin, et al.; J. Biol. Chem. 277, 33213 (2002)
    10. Bisindolylmaleimide IX Induces Reversible and Time-Dependent Tumor Necrosis Factor Receptor Family-Mediated Caspase Activation and Cell Death: O.W. Rokhlin & M.B. Cohen; Cancer Biol. Ther. 2, 266 (2003)
    11. Protein kinase C-independent effects of protein kinase D3 in glucose transport in L6 myotubes: J. Chen, et al.; Mol. Pharmacol. 67, 152 (2005)
    12. Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002: M.D. Jacobs, et al.; J. Biol. Chem. 280, 13728 (2005)
    13. Bisindolylmaleimide IX facilitates extrinsic and initiates intrinsic apoptosis in TNF-alpha-resistant human colon adenocarcinoma COLO 205 cells: B. Pajak, et al.; Apoptosis 13, 509 (2008)
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