NG25 |
Catalog No.GC13514
One-Click Copy Product Info
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NG25는 강력하고 세포 투과성이 있는 전환성 성장 인자-β 활성효소 1 (TAK1) 및 미토겐 활성화 단백질 키나제 2 (MAP4K2) 억제제이고 각각의 IC50 값은 149nM 및 21.7nM이다.
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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NG25는 강력하고 세포 투과성이 있는 전환성 성장 인자-β 활성효소 1 (TAK1) 및 미토겐 활성화 단백질 키나제 2 (MAP4K2) 억제제이고 각각의 IC50 값은 149nM 및 21.7nM이다. NG25는 종양학(예: KRAS 돌연변이 대장암), 면역 회피, 종양 미세환경 재구성 등과 관련된 연구에 일반적으로 사용된다[2,3,4].
체외 실험에서 NG25 (1, 2, 5, 10, 20μM)를 5종의 유방암 세포 라인 (T-47D, MCF7, HCC1954, MDA-MB-231, BT-549)에 72시간 처리한 후 모든 시험 세포 라인에서 세포 생존율이 용량 의존적으로 감소하였다[4]. 인간 대동맥 혈관 평활근 세포(HA-VSMCs)를 NG25 (0.1, 0.3, 1μM)로 30분간 전처리한 후 지방다당류 (LPS, 100ng/mL)로 2시간 처리하면LPS에 의해 유도된 Smad2 링커 영역의 Thr220 및 Ser245/250/255 부위의 인산화가 용량 의존적으로 억제되었고 1μM 농도에서 완전한 억제가 관찰되었다[5].
체내 실험에서 mdx 쥐에게 NG25 (6mg/kg/day)를 2주간 복강 내 투여한 후 TAK1 인산화 수준이 현저하게 감소하고 전경골근과 횡격막 근육의 염증 세포 침윤이 감소하였다[6]. Hop62-shCLU (CLU 녹다운 Hop62 세포) 이종 이식 종양을 이식한 누드 쥐에게 NG25 (4mg/kg/day)를 15일간 정맥 투여한 후 종양 성장이 느려졌다[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.
| 세포 실험 [1]: | |
세포 라인 | T-47D、MCF7、HCC1954、MDA-MB-231 및 BT-549 세포 (인간 유방암 세포 라인) |
제조 방법 | 5종의 인간 유방암 세포 라인 T-47D, MCF7, HCC1954, MDA-MB-231, BT-549를 NG25 0, 1μM, 2μM, 5μM, 10μM, 20μM으로 72시간 처리한 후 CCK-8 분석법으로 세포 생존율을 평가하였습니다. |
반응 조건 | 1, 2, 5, 10 및 20μM; 72 시간 동안 |
응용 분야 | NG25 처리는 모든 시험 세포의 생존율을 용량 의존적으로 감소시켰습니다. |
| 동물 실험 [2]: | |
동물 모형 | Mdx 쥐 |
제조 방법 | Mdx 쥐에게 NG25 (6mg/kg/day)를 2주간 복강 내 주사로 투여하였습니다. 그 후 쥐를 안락사시키고 전경골근과 횡격막 근육 절편을 조직학 및 단백질 자극법으로 사용하였다. |
제형 | 6mg/kg/일; 2 주 동안; i.p. |
응용 분야 | NG25 처리는 전경골근과 횡격막 근육에서 TAK1 인산화 수준을 현저하게 감소시키고 염증 세포 침윤을 감소시켰습니다. |
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)
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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
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- 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.)