SML3321

GK921

≥98% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₁H₂₀N₄O
• CAS-Nummer: 1025015-40-0
• Molekulargewicht: 344.41
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD28167818
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• 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

Beschreibung

Biochem/physiol Actions

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).

Orally active transglutaminase 2 (TG2, TGase 2) inhibitor in vitro and in vivo.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable