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Chemical Structure : GK921
CAS No.: 1025015-40-0
Catalog No.: PC-42986Not For Human Use, Lab Use Only.
GK921 is a specific, orally active Transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 7.71 uM against recombinant hTGase 2.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 25 mg | $368 | In stock | |
| 100 mg | $988 | In stock | |
| 500 mg | Get quote | ||
| 1 g | Get quote |
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GK921 is a specific, orally active Transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 7.71 uM against recombinant hTGase 2.
GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner, induces cell death of eight RCC lines with average GI50 of 0.9 uM.
GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
GK921 blocks MES transdifferentiation and showed significant therapeutic efficacy in mouse models of glioma stem cells (GSC)
| M.Wt | 344.4097 | |
| Formula | C21H20N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 30 mg/mL |
|
| Chemical Name/SMILES |
Pyrido[2,3-b]pyrazine, 3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]- |
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1. Yin J, et al. Cancer Res. 2017 Sep 15;77(18):4973-4984.
2. Kang JH, et al. Cell Death Dis. 2016 Apr 21;7:e2200.
3. Ku BM, et al. J Cancer Res Clin Oncol. 2014 May;140(5):757-67.
4. Kang JH, et al. Cell Death Dis. 2016 Mar 31;7:e2163.
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