GK921

This product is for research use only, not for human use. We do not sell to patients.

GK921
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1450Check With Us
500mg$2150Check With Us
1g$3225Check With Us

Cat #: V4158 CAS #: 1025015-40-0 Purity ≥ 98%

Description: GK921 is a novel and potent inhibitor of transglutaminase 2 (TGase) with an IC50 of 7.71 μM for human recombinant TGase 2.

References: 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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Product Promise

Promise
Molecular Weight (MW)344.41
Molecular FormulaC21H20N4O
CAS No.1025015-40-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeC12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2
SynonymsGK921; GK-921; GK 921
ProtocolIn VitroGK921 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 VivoA single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.9035 mL14.5176 mL29.0352 mL58.0703 mL
5mM0.5807 mL2.9035 mL5.8070 mL11.6141 mL
10mM0.2904 mL1.4518 mL2.9035 mL5.8070 mL
20mM0.1452 mL0.7259 mL1.4518 mL2.9035 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.