Art. -Nr.: HY-12337

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GK921

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC₅₀ of 7.71 μM for human recombinant TGase 2.

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Reinheit: 99.91%
CAS. Nr.: 1025015-40-0
Formel: C₂₁H₂₀N₄O
Molecular Weight:344.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GK921 Chemical Structure

CAS. Nr.: 1025015-40-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC₅₀ of 7.71 μM for human recombinant TGase 2.

IC₅₀ & Target

IC50: 7.71 μM (TGase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.72 μM Compound: 921	Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay	[PMID: 21855350]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1025015-40-0
Appearance Solid
Molecular Weight 344.41
Formel C₂₁H₂₀N₄O
Color Off-white to brown
SMILES

C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All In Vivo Efficacy StudyRT-PCRHistological Imaging/StainingIFWB

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Journal Impact Factor

Cancer Res

Transglutaminase 2 Inhibition Reverses Mesenchymal Transdifferentiation of Glioma Stem Cells by Regulating C/EBPβ Signaling. [Abstract]

2017 Sep 15;77(18):4973-4984. PMID: 28754668

GK921 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2017 Sep 15;77(18):4973-4984. [Abstract]

Immunoblot analysis of TGM2, CD44, TAZ, C/EBPβ, pSTAT3, and STAT3 in MES GSC treated with GK921 (24 hours).
J Adv Res

Transglutaminase 2 modulates inflammatory angiogenesis via vascular endothelial growth factor receptor 2 pathway in inflammatory bowel disease. [Abstract]

2025 Jul 4:S2090-1232(25)00500-4. PMID: 40619121

GK921 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 4:S2090-1232(25)00500-4. [Abstract]

The cohort that received GK921 (10 mg/kg, i.p.) treatment exhibited significant improvements in weight loss and colon shortening.

GK921 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 4:S2090-1232(25)00500-4. [Abstract]

Representative HE staining and TGM2, CD31 immunohistochemical images of GK921 (10 mg/kg, i.p.) treatment group and solvent treatment group after DSS colitis model establishment show decreased MVD in DSS mice after GK921 treatment.

GK921 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 4:S2090-1232(25)00500-4. [Abstract]

WB result display that GK921 (10 mg/kg, i.p.) treatment significantly reduce the phosphorylation of VEGFR2 at Tyr1059 and Tyr1214 after DSS treatment.

GK921 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 4:S2090-1232(25)00500-4. [Abstract]

GK921 (10 mg/kg, i.p.) treatment exhibit decrease in the number of CD31 (green), TGM2 (red), Ki-67 (cyan) positive proliferative vascular endothelial cells comparing to controls.
Cancer Lett

TGM2-mediated serotonylation in tumor endothelial cells promotes angiogenesis and tumor growth in colorectal cancer. [Abstract]

2026 May 1:645:218396. PMID: 41780842
Cancer Lett

Serotonylation in tumor-associated fibroblasts contributes to the tumor-promoting roles of serotonin in colorectal cancer. [Abstract]

2024 Aug 1:217150. PMID: 39097134
Cell Death Discov

Inhibition of TGM2 enhances cisplatin sensitivity in MSH2-deficient bladder cancer. [Abstract]

2026 May 28. PMID: 42209463
Biochem Pharmacol

Transglutaminase 2 promotes breast cancer cell autophagy by targeting p53/ mTOR axis. [Abstract]

2025 Apr 9:116926. PMID: 40216264
Mol Cancer Res

Interaction of NDRG1 and TGM2 modulates DNA replication and repair. [Abstract]

2026 Mar 31:10.1158/1541-7786.MCR-25-0743. PMID: 41914984
J Dent Sci

Fatostatin delayed lip sensory recovery after inferior alveolar nerve transection by inhibiting sterol regulatory element-binding protein 1. [Abstract]

2025 Jul;20(3):1885-1889. PMID: 40654464
J Dent Sci

Serotonin promotes lip sensory recovery after inferior alveolar nerve transection via histone serotonylation. [Abstract]

2025 Oct;20(4):2363-2374. PMID: 41040553

GK921 purchased from MedChemExpress. Usage Cited in: J Dent Sci. 2025 Oct;20(4):2363-2374. [Abstract]

GK921 significantly downregulated the mRNA expression of NGF, ATF3, NTF3, NTF5, GDNF, FASN, SREBF1, and APOD by RT-PCR.
Discov Oncol

Transglutaminase 2 nuclear localization enhances glioblastoma radiation resistance. [Abstract]

2025 May 30;16(1):952. PMID: 40445445
Am J Cancer Res

Blockade of CCL2 expression overcomes intrinsic PD-1/PD-L1 inhibitor-resistance in transglutaminase 2-induced PD-L1 positive triple negative breast cancer. [Abstract]

2020 Sep 1;10(9):2878-2894. PMID: 33042623

GK921 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2020 Sep 1;10(9):2878-2894. [Abstract]

Western blot analysis to assess the expressions of TG2, PD-L1, PTEN, pAKT, IκBα, and β-actin in MCF7/TG2 and MDA-MB-231 cells after GK921 (TG2 inhibitor) treatment for 24 h in a dose-dependent manner.
Respir Physiol Neurobiol

Blocking TG2 attenuates bleomycin-induced pulmonary fibrosis in mice through inhibiting EMT. [Abstract]

2020 May;276:103402. PMID: 32006666

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 30 mg/mL (87.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9035 mL

14.5176 mL

29.0352 mL

5 mM

0.5807 mL

2.9035 mL

5.8070 mL

10 mM

0.2904 mL

1.4518 mL

2.9035 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% PBS

Solubility: ≥ 2.5 mg/mL (7.26 mM); Suspended solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: GK921 is dissolved in DMSO. Vehicle alone and GK921 (8 mg/kg) are administered orally once per day, 5 days/week, for 64 days. The size of the primary tumors is measured every 2-3 days using calipers. Tumor volume is calculated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9035 mL	14.5176 mL	29.0352 mL	72.5879 mL
	5 mM	0.5807 mL	2.9035 mL	5.8070 mL	14.5176 mL
	10 mM	0.2904 mL	1.4518 mL	2.9035 mL	7.2588 mL
	15 mM	0.1936 mL	0.9678 mL	1.9357 mL	4.8392 mL
	20 mM	0.1452 mL	0.7259 mL	1.4518 mL	3.6294 mL
	25 mM	0.1161 mL	0.5807 mL	1.1614 mL	2.9035 mL
	30 mM	0.0968 mL	0.4839 mL	0.9678 mL	2.4196 mL
	40 mM	0.0726 mL	0.3629 mL	0.7259 mL	1.8147 mL
	50 mM	0.0581 mL	0.2904 mL	0.5807 mL	1.4518 mL
	60 mM	0.0484 mL	0.2420 mL	0.4839 mL	1.2098 mL
	80 mM	0.0363 mL	0.1815 mL	0.3629 mL	0.9073 mL

Keywords

GK921

12 Cited Publications

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GK921

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glutamine Metabolism Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Cuproptosis Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) GK921

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GK921

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glutamine Metabolism Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Cuproptosis Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) GK921

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GK921 Related Classifications

HY-12337 Related Classifications