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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).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | , Faint yellow to very dark orange |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | 2-8°C |
| 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 |
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¥ 1259.40
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¥ 1956.41
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无菌，PETG 方形有刻度培养基瓶，带盖，聚对苯二酸乙二醇酯共聚物，天然高密度聚乙烯盖，500毫升容量，每箱40，40/箱，342020-0500，Nalgene，Thermofisher，赛默飞世尔¥ 3684.34
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