GK921( GK921 | GK-921 | GK 921 )

Catalog No. M17119 CAS No. 1025015-40-0

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Datasheet

HNMR

HPLC

MSDS

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Product Name

GK921
Note

Research use only, not for human use.
Brief Description

GK921 is a transglutaminase 2 (TGase) inhibitor.
Description

GK921 is a transglutaminase 2 (TGase 2) inhibitor. GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. TGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models, suggesting the possibility of a new therapeutic approach to RCC.
In Vitro

GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.05×10-7 M. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.
In Vivo

A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
Synonyms

GK921 | GK-921 | GK 921
Pathway

Others
Target

Other Targets
Recptor

TGase
Research Area

Cancer
Indication

——

CAS Number

1025015-40-0
Formula Weight

344.42
Molecular Formula

C21H20N4O
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 30 mg/mL 87.11 mM
SMILES

C1CCN(C1)CCOc1c(nc2c(n1)cccn2)C#Cc1ccccc1
Chemical Name

3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[2,3-b]pyrazine

1. Ku BM,et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models.J Cancer Res Clin Oncol. 2014 May;140(5):757-67.

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