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经验公式(希尔记法):
C21H20N4O
化学文摘社编号:
分子量:
344.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
N4(CCCC4)CCOc1nc2c(nc1C#Cc3ccccc3)nccc2
InChI
1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2
InChI key
MNYJJHBAEYKXEG-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
, Faint yellow to very dark orange
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Orally active transglutaminase 2 (TG2, TGase 2) inhibitor in vitro and in vivo.
GK921 is an orally active transglutaminase 2 (TG2, TGase 2) inhibitor (IC50 = 7.71 μM) that effectively inhibits TG2-mediated I-κBα and p53 polymerization. GK921 induces growth arrest/cell death in renal cell carcinoma (RCC) cultures (ave GI50 = 9.05 μM) and abrogates RCC with increase in p53 level in mice in vivo (8 mg/kg 5x per wk; ACHN or CAKI-1 cells).
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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To test whether transglutaminase 2 (TGase 2) inhibitor GK921 alone reverses renal cell carcinoma (RCC) tumor growth. RCC is resistant to both radiation and chemotherapy, and the prognosis remains poor. Despite the recent therapeutic success of vascular endothelial growth factor
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