| Identification | Back Directory | [Name]
GK921 | [CAS]
1025015-40-0 | [Synonyms]
GK921
GK921, >98%
GK-921;GK 921
3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine
3-(2-Phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]pyrido[2,3-b]pyrazine
Pyrido[2,3-b]pyrazine, 3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]- | [Molecular Formula]
C21H20N4O | [MDL Number]
MFCD28167818 | [MOL File]
1025015-40-0.mol | [Molecular Weight]
344.41 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
DMSO:31.5(Max Conc. mg/mL);91.46(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.41(Max Conc. mM) | [form ]
A solid | [color ]
Off-white to brown |
| Hazard Information | Back Directory | [Biological Activity]
GK921 is an orally active transglutaminase 2 (TG2TGase 2) inhibitor (IC50 = 7.71 μM) th at effectively inhibits TG2-mediated I-KBα 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). |
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