| 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 | [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 | [InChIKey]
MNYJJHBAEYKXEG-UHFFFAOYSA-N | [SMILES]
N4(CCCC4)CCOc1nc2c(nc1C#Cc3ccccc3)nccc2 |
| Hazard Information | Back Directory | [Uses]
GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2. | [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). | [in vivo]
A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models[1]. | [References]
[1] Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014 May;140(5):757-67. DOI:10.1007/s00432-014-1623-5 |
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