GK921

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.

Product information

CAS Number: 1025015-40-0

Molecular Weight: 344.41

Formula: C21H20N4O

Synonym:

GK 921

GK-921

Chemical Name: 1-(2-{[3-(2-phenylethynyl)pyrido[2,3-b]pyrazin-2-yl]oxy}ethyl)pyrrolidine

Smiles: C(CN1CCCC1)OC1=NC2=CC=CN=C2N=C1C#CC1C=CC=CC=1

InChiKey: MNYJJHBAEYKXEG-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.