Isogranulatimide CAS: 244148-46-7
MF: C15H8N4O2
MW: 276.3
Cell-permeable alkaloid that acts as a potent and ATP-competitive inhibitor of Chk1.

Isogranulatimide (CAS 244148-46-7)

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应用; Isogranulatimide is cell-permeable alkaloid that acts as a potent and ATP-competitive inhibitor of Chk1
CAS号码: 244148-46-7
纯度: ≥95%
分子量: 276.3
分子式: C15H8N4O2
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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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.


参考文献

Jiang, X., et al. 2004. Mol. Cancer Ther. 3, 1221. Roberge, M., et al. 1998. Cancer Res. 58, 5701.

物理状态 :
Solid
溶解度 :
Soluble in DMSO.
保存 :
Store at 4° C
熔点 :
296.16° C (Predicted)
沸点 :
678.88° C (Predicted)
密度 :
1.83 g/cm3 (Predicted)
折射率 :
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值 :
pKa: 9.43 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
EC号码 :
MFCD09970584
SMILES :
C1=CC=C2C(=C1)C3=C(N2)N4C=NC=C4C5=C3C(=O)NC5=O

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