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Merck
CN

SML3321

GK921

≥98% (HPLC)

别名:

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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关于此项目

经验公式(希尔记法):
C21H20N4O
化学文摘社编号:
分子量:
344.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

assay

≥98% (HPLC)

form

powder

color

, Faint yellow to very dark orange

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

Quality Level

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).

存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Tracy J Berg et al.
Cancer research, 81(8), 2101-2115 (2021-01-24)
The tumor microenvironment plays an essential role in supporting glioma stemness and radioresistance. Following radiotherapy, recurrent gliomas form in an irradiated microenvironment. Here we report that astrocytes, when pre-irradiated, increase stemness and survival of cocultured glioma cells. Tumor-naïve brains increased
Yuanyuan Hou et al.
Journal of immunology research, 2021, 4754454-4754454 (2021-09-07)
Propofol is a known intravenous hypnotic drug used for induction and maintenance of sedation and general anesthesia. Emerging studies also reveal a neuroprotective effect of propofol in diverse diseases of neuronal injuries via modulating microglia activation. In this study, we
Bo Mi Ku et al.
Journal of cancer research and clinical oncology, 140(5), 757-767 (2014-03-13)
To test whether transglutaminase 2 (TGase 2) inhibitor GK921 alone reverses renal cell carcinoma (RCC) tumor growth. RCC is resistant to both radiation and chemotherapy, and the prognosis remains poor. Despite the recent therapeutic success of vascular endothelial growth factor

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