GK921
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.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1025015-40-0
- Formula: C21H20N4O
- Molecular Weight:344.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
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HY-L146
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HY-L181
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HY-L001V
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HY-L205
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Alkyne Compound Library
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Publications Citing Use of MedChemExpress (MCE) GK921
More- Cancer Res. 2017 Sep 15;77(18):4973-4984. [Abstract]
- J Adv Res. 2025 Jul 4:S2090-1232(25)00500-4. [Abstract]
- Cancer Lett. 2026 May 1:645:218396. [Abstract]
- Cancer Lett. 2024 Aug 1:217150. [Abstract]
- Cell Death Discov. 2026 May 28. [Abstract]
- Biochem Pharmacol. 2025 Apr 9:116926. [Abstract]
- Mol Cancer Res. 2026 Mar 31:10.1158/1541-7786.MCR-25-0743. [Abstract]
- J Dent Sci. 2025 Jul;20(3):1885-1889. [Abstract]
- J Dent Sci. 2025 Oct;20(4):2363-2374. [Abstract]
- Discov Oncol. 2025 May 30;16(1):952. [Abstract]
- Am J Cancer Res. 2020 Sep 1;10(9):2878-2894. [Abstract]
- Respir Physiol Neurobiol. 2020 May;276:103402. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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WB
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IF
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RT-PCR
Biological Activity
IC50: 7.71 μM (TGase)[1]
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
0.72 μM
Compound: 921
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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
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[PMID: 21855350] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1025015-40-0
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Appearance Solid
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Molecular Weight 344.41
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Formula C21H20N4O
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Color Off-white to brown
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SMILES
C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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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).
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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.
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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
2026 May 28. PMID: 42209463 -
Biochem Pharmacol
2025 Apr 9:116926. PMID: 40216264 -
Mol Cancer Res
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.
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Discov Oncol
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.
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Respir Physiol Neurobiol
Blocking TG2 attenuates bleomycin-induced pulmonary fibrosis in mice through inhibiting EMT. [Abstract]2020 May;276:103402. PMID: 32006666
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 90% PBS
Solubility: ≥ 2.5 mg/mL (7.26 mM); Suspended solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
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