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

A cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects.

Aloisine A - CAS 496864-16-5 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: RP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine

Primary Target: Cyclin-dependent kinases
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
496864-16-5C₁₆H₁₇N₃O

Products

Catalog NumberPackaging Qty/Pack
128125-5MG Plastic ampoule 5 mg
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
Global Trade Item Number
Catalog Number GTIN
128125-5MG 04055977222210

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.
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 Protect from light
+2°C to +8°C
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.