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GK921

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Purity:97.44%

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COA HNMR HPLC

GK921

Catalog No. T3968Cas No. 1025015-40-0

GK921 is an inhibitor of transglutaminase 2 (TGase).

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Pack Size	Price	Availability
2 mg	$84	In Stock
5 mg	$126	In Stock
10 mg	$207	In Stock
25 mg	$331	In Stock
50 mg	$531	In Stock
100 mg	$725	In Stock
1 mL x 10 mM (in DMSO)	$137	In Stock

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Product Introduction

Bioactivity

Description	GK921 is an inhibitor of transglutaminase 2 (TGase).
Targets&IC50	TGase 2:8.93 μM
In vitro	GK921 inhibits TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from a GI50 of 10^-10 to 10^-4 M with an average GI50 of 9.05×10^-7 M. GK921 rescues p53 levels and consequently induces apoptosis, increasing c-PARP and p53 levels in a concentration-dependent manner[1].'
In vivo	A single treatment with GK921 significantly stabilizes p53 and nearly completely reduces tumor growth in the ACHN and CAKI-1 preclinical xenograft tumor models, suggesting a potential new therapeutic approach to RCC[1].
Kinase Assay	TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2
Cell Research	Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1].

Chemical Properties

Molecular Weight	344.41
Formula	C21H20N4O
Cas No.	1025015-40-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 55 mg/mL (159.69 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9035 mL	14.5176 mL	29.0352 mL	145.1758 mL
5 mM	0.5807 mL	2.9035 mL	5.8070 mL	29.0352 mL
10 mM	0.2904 mL	1.4518 mL	2.9035 mL	14.5176 mL
20 mM	0.1452 mL	0.7259 mL	1.4518 mL	7.2588 mL
50 mM	0.0581 mL	0.2904 mL	0.5807 mL	2.9035 mL
100 mM	0.0290 mL	0.1452 mL	0.2904 mL	1.4518 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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