NG25 |
Catalog No.GC13514
One-Click Copy Product Info
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NG25 is a potent and cell-permeable inhibitor of transforming growth factor-β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), with IC50 values of 149nM and 21.7nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1315355-93-1
Sample solution is provided at 25 µL, 10mM.
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NG25 is a potent and cell-permeable inhibitor of transforming growth factor-β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), with IC50 values of 149nM and 21.7nM, respectively[1]. NG25 is commonly used in studies related to oncology (e.g., KRAS-mutant colorectal cancer), immune evasion, and tumor microenvironment remodeling[2,3,4].
In vitro, treatment with NG25 (1, 2, 5, 10, and 20μM) for 72h in five breast cancer cell lines (T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549) dose-dependently reduced cell viability in all tested cell lines[4]. Pre-incubation of human aortic vascular smooth muscle cells (HA-VSMCs) with NG25 (0.1, 0.3, 1μM) for 30min, followed by treatment with lipopolysaccharide (LPS, 100ng/mL) for 2h, dose-dependently inhibited LPS-induced phosphorylation of the Smad2 linker region at the Thr220 and Ser245/250/255 sites, with complete inhibition observed at a concentration of 1μM[5].
In vivo, intraperitoneal administration of NG25 (6mg/kg/day) for 2 weeks in mdx mice significantly reduced TAK1 phosphorylation levels and decreased inflammatory cell infiltration in the tibialis anterior and diaphragm muscles[6]. Intravenous administration of NG25 (4mg/kg/day) for 15 days in nude mice bearing Hop62-shCLU (CLU-knockdown Hop62 cell) xenograft tumors slowed tumor growth[7].
References:
[1] Basnet R, Khadka S, Basnet B B, et al. Xanthine oxidase and transforming growth factor beta-activated kinase 1: potential targets for gout intervention[J]. Current Rheumatology Reviews, 2021, 17(2): 153-161.
[2] Xiang Q, Mao Z, Ma Q, et al. NG25 enhances anti-tumor immunity in KRAS-mutant colorectal cancer[J]. OncoTargets and Therapy, 2026: 1-12.
[3] Ma Q, Gu L, Liao S, et al. NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivo[J]. Apoptosis, 2019, 24(1): 83-94.
[4] Wang Z, Zhang H, Shi M, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells[J]. Scientific Reports, 2016, 6(1): 32737.
[5] Afroz R, Zhou Y, Little P J, et al. Toll-like receptor 4 stimulates gene expression via Smad2 linker region phosphorylation in vascular smooth muscle cells[J]. ACS Pharmacology & Translational Science, 2020, 3(3): 524-534.
[6] Xu D, Li S, Wang L, et al. TAK1 inhibition improves myoblast differentiation and alleviates fibrosis in a mouse model of Duchenne muscular dystrophy[J]. Journal of Cachexia, Sarcopenia and Muscle, 2021, 12(1): 192-208.
[7] Chen Z, Fan Z, Dou X, et al. Inactivation of tumor suppressor gene Clusterin leads to hyperactivation of TAK1-NF-κB signaling axis in lung cancer cells and denotes a therapeutic opportunity[J]. Theranostics, 2020, 10(25): 11520.
| Cell experiment [1]: | |
Cell lines | T-47D、MCF7、HCC1954、MDA-MB-231 and BT-549 cells (human breast cancer cell lines) |
Preparation Method | Five human breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 were treated with NG25 at 0, 1μM, 2μM, 5μM, 10μM, and 20μM for 72h, then cell viability was assessed using the CCK-8 assay. |
Reaction Conditions | 1, 2, 5, 10, and 20μM; 72h |
Applications | Treatment with NG25 dose-dependently reduced the viability of all tested cells. |
| Animal experiment [2]: | |
Animal models | Mdx mice |
Preparation Method | Mdx mice were treated with NG25 (6mg/kg/day) via intraperitoneal injection for 2 weeks. Then the mice were euthanized, and the tibialis anterior and diaphragm muscle sections were subjected to histological and western blot analysis. |
Dosage form | 6mg/kg/day; 2 weeks; i.p. |
Applications | Treatment with NG25 significantly reduced TAK1 phosphorylation levels in the tibialis anterior and diaphragmatic muscles and decreased inflammatory cell infiltration. |
References: | |
| Cas No. | 1315355-93-1 | SDF | |
| Chemical Name | N-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide | ||
| Canonical SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)C3=CC(=C(C=C3)C)OC4=C5C=CNC5=NC=C4)C(F)(F)F | ||
| Formula | C29H30F3N5O2 | M.Wt | 537.58 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8602 mL | 9.3009 mL | 18.6019 mL |
| 5 mM | 372 μL | 1.8602 mL | 3.7204 mL |
| 10 mM | 186 μL | 930.1 μL | 1.8602 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)