371957
Isogranulatimide - CAS 244148-46-7 - Calbiochem
Isogranulatimide, also referenced under CAS 244148-46-7, modulates the biological activity of Chk1 and GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Isogranulatimide - CAS 244148-46-7 - Calbiochem, IGR, Chk1 Inhibitor III, Chk2 Inhibitor III, IGR, Chk2 Inhibitor III, Chk1 Inhibitor III
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About This Item
Empirical Formula (Hill Notation):
C15H8N4O2
CAS Number:
Molecular Weight:
276.25
UNSPSC Code:
12352200
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
dark red
solubility
DMSO: 50 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable alkaloid containing indole/maleimide/imidazole skeleton that acts as a potent, reversible and ATP-competitive inhibitor of Chk1 (IC50 = 100 nM) and GSK-3β (IC50 = 500 nM). Inhibits G2 DNA damage checkpoint-associated kinases, Chk2, Cdk1, and DNA-PK only at much higher concentrations (IC50 = 3 µM, 10 µM, and 10 µM, respectively). Only minimally affects the activities of a panel of 11 other kinases tested (IC50 ≥ 40 µM). When used in combination with γ-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function.
A cell-permeable, potent, reversible, and ATP-competitive inhibitor of Chk1 (IC50 = 100 nM) and GSK-3β (IC50 = 500 nM). Inhibits G2 DNA damage checkpoint-associated kinases, Chk2, Cdk1, and DNA-PK only at much higher concentrations (IC50 = 3 µM, 10 µM, and 10 µM, respectively). Only minimally affects the activities of a panel of 11 other kinases tested (IC50 ≥ 40 µM). When used in combination with γ-irradiation, it is also reported to selectively arrest the growth of MCF-7 cells lacking p53 function.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Chk1
Chk1
Product competes with ATP.
Reversible: yes
Target IC50: 100 nM, 500 nM, against Chk1 and GSK-3β, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Jiang, X., et al. 2004. Mol. Cancer Ther.3, 1221.
Roberge, M., et al. 1998. Cancer Res.58, 5701.
Roberge, M., et al. 1998. Cancer Res.58, 5701.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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