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Isogranulatimide (CAS 244148-46-7)

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Application:Cell-permeable alkaloid that acts as a potent and ATP-competitive inhibitor of Chk1
CAS Number:244148-46-7
Molecular Weight:276.3
Molecular Formula:C15H8N4O2
Refer to Certificate of Analysis for lot specific data (including water content).
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Product NameCatalog #UnitPriceQtyAddFavorites
Isogranulatimide sc-202667 1 mg $700
Isogranulatimide is 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). Isogranulatimide 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). Isogranulatimide 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.
Technical Information
Physical State:Solid
Solubility:Soluble in DMSO.
Storage:Store at 4° C
Melting Point:296.16 °C (Predicted)
Boiling Point:678.88 °C (Predicted)
Density:1.83 g/cm3 (Predicted)
Refractive Index:n20D 1.97 (Predicted)
IC50:Chk1: IC50 = 100 nM; GSK-3β: IC50 = 500 nM; Chk2: IC50 = 3 µM; Cdk1: IC50 = 10 µM; DNA-PK: IC50 = 10 µM; DU-145 : IC50 = 13.1 µM (human); L1210 : IC50 = 10 µM (mouse)
pK Values:pKa: 9.43 (Predicted)
Safety and Reference Information
PubChem CID:6419741
EC Number:MFCD09970584
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221. Roberge, M., et al. 1998. Cancer Res. 58, 5701.
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