128125 Aloisine A - CAS 496864-16-5 - Calbiochem

128125
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Empirical FormulaCAS #
C₁₆H₁₇N₃O496864-16-5

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128125-5MG
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      Description
      OverviewA cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC50 = ~ 3 - 10 µM). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC50 ≥ 100 µM). Shown to arrest cells in both G1 and G2 phases (IC50 = 7 µM and 10.5 µM for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).
      Catalogue Number128125
      Brand Family Calbiochem®
      SynonymsRP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
      References
      ReferencesNoel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
      Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.
      Product Information
      CAS number496864-16-5
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₆H₁₇N₃O
      Chemical formulaC₁₆H₁₇N₃O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCyclin-dependent kinases
      Primary Target IC<sub>50</sub>150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively; 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively
      Primary Target K<sub>i</sub>EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin, respectively
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Aloisine A - CAS 496864-16-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Aloisine A - CAS 496864-16-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      128125

      References

      Reference overview
      Noel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
      Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.

      Brochure

      Title
      Alzheimer's Disease Brochure & Technical Guide
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision13-December-2007 JSW
      SynonymsRP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
      DescriptionA cell-permeable, pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM for Cdk1/cyclin B, 120 nM for Cdk2/cyclin A, 400 nM for Cdk2/cyclin E, and 160 nM for Cdk5/p25), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM for GSK-3α and 1.5 µM for GSK-3β), and c-Jun N-terminal kinase (JNK; IC50 ~3-10 µM). Also inhibits extracellular signal-regulated kinases (ERKs; IC50 = 18 µM for ERK1 and 22 µM for ERK2), PIM1 (IC50 > 10 µM), and insulin receptor tyrosine kinase (IC50 = 60 µM) at higher concentrations. Does not significantly inhibit Cdk4/cyclin D1, CK1, CK2, MAPKK, PKA, PKG, PKCs, or c-raf (IC50 = ≥ 100 µM). Shown to arrest undifferentiated human teratocarcinoma cells (NT2) and differentiated post-mitotic neurons (hNT) in both G1 and G2 phases (IC50 = 7 µM and 10.5 µM, respectively). Also shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM of Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number496864-16-5
      Chemical formulaC₁₆H₁₇N₃O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesNoel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
      Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.