SML3321
GK921
≥98% (HPLC)
Synonym(s):
3-(2-Phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]pyrido[2,3-b]pyrazine, 3-(Phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine, GK 921, GK-921
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About This Item
Empirical Formula (Hill Notation):
C21H20N4O
CAS Number:
Molecular Weight:
344.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
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
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).
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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