Skip to Content
Merck
All Photos(1)

Key Documents

View All Documentation

SML3321

Sigma-Aldrich

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

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C21H20N4O
CAS Number:
1025015-40-0
Molecular Weight:
344.41
MDL number:
MFCD28167818
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

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

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service