TAPI-1 (Synonyms: TAPI) |
Catalog No.GC12344
One-Click Copy Product Info
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TAPI-1은 TACE (종양 괴사 인자-α 전환 효소) 억제제로 TACE의 단백질 분해 활성을 억제해서 세포막 단백질 (암피레귤린(AREG))의 세포외 영역 전이를 차단한다. 게다가 TAPI-1은 메탈로프로테이나제(MMP) 억제제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 163847-77-6
Sample solution is provided at 25 µL, 10mM.
TAPI-1은 TACE (종양 괴사 인자-α 전환 효소) 억제제로 TACE의 단백질 분해 활성을 억제해서 세포막 단백질 (암피레귤린(AREG))의 세포외 영역 전이를 차단한다. 게다가 TAPI-1은 메탈로프로테이나제(MMP) 억제제이다. TAPI-1은 세포 산화 스트레스와 염증 인자의 생성을 감소시킬 수 있다[4].
체외 실험에서 TAPI-1(0-20µM)으로 TE-1 및 Eca109 세포를 24시간 처리하면 용량 의존적으로 세포 생존율, 이동 및 침윤을 억제하고 시스플라틴 유도 세포 사멸을 촉진하였다[5]. TAPI-1(20µM)으로 A549 세포를 24시간 처리하면 세포 증식을 감소시키고 EGFR 및 Notch1 mRNA 발현을 억제하였다[6]. TAPI-1(5, 10µM)으로 NCI-H292 세포를 6시간 및 24시간 처리하면 다이아세틸에 의해 자극된 암피레귤린(AREG)의 세포막으로부터의 전이를 차단하였다[7].
체내 실험에서 황색 포도상구균 유도 관절염 쥐에게 복강 내 주사로 TAPI-1(10mg/kg)을 투여하면 발 부종을 현저하게 감소시키고 관절 조직 내 과산화물, 산화질소 및 과산화수소의 농도를 감소시켰다[8].
References:
[1] Slack B E, Ma L K, Seah C C. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme[J]. Biochemical Journal, 2001, 357(3): 787-794.
[2] Liu C, Xu P, Lamouille S, et al. TACE-mediated ectodomain shedding of the type I TGF-β receptor downregulates TGF-β signaling[J]. Molecular cell, 2009, 35(1): 26-36.
[3] Koon H W, Zhao D, Na X, et al. Metalloproteinases and transforming growth factor-α mediate substance P-induced mitogen-activated protein kinase activation and proliferation in human colonocytes[J]. Journal of Biological Chemistry, 2004, 279(44): 45519-45527.
[4] Bae E H, Kim I J, Choi H S, et al. Tumor necrosis factor α-converting enzyme inhibitor attenuates lipopolysaccharide-induced reactive oxygen species and mitogen-activated protein kinase expression in human renal proximal tubule epithelial cells[J]. The Korean Journal of Physiology & Pharmacology, 2018, 22(2): 135-143.
[5] Gao L, Li L, Zhang D, et al. TAPI-1 exhibits Anti-tumor efficacy in human esophageal squamous cell carcinoma cells via suppression of NF-κB signaling pathway[J]. Digestive Diseases and Sciences, 2024, 69(1): 81-94.
[6] Pancewicz J, Golec P. The effect of TAPI-1 treatment in non-small cell lung cancer cells[J].
[7] Kelly F L, Sun J, Fischer B M, et al. Diacetyl induces amphiregulin shedding in pulmonary epithelial cells and in experimental bronchiolitis obliterans[J]. American journal of respiratory cell and molecular biology, 2014, 51(4): 568-574.
[8] Sultana S, Bishayi B. Potential anti-arthritic and anti-inflammatory effects of TNF-α processing inhibitor-1 (TAPI-1): A new approach to the treatment of S. aureus arthritis[J]. Immunobiology, 2020, 225(2): 151887.
| 세포 실험 [1]: | |
세포 라인 | TE-1、Eca109 세포 |
제조 방법 | TE-1 및 Eca109 세포를 다양한 농도의 TAPI-1(0, 1.25, 2.5, 5, 10 및 20μM)에 24시간 노출시킨 후 CCK-8 분석법을 사용해서 세포 생존율을 측정하였습니다. |
반응 조건 | 0, 1.25, 2.5, 5, 10, 20μM; 24 시간 동안 |
응용 분야 | TAPI-1 노출 후 TE-1 및 Eca109 세포의 생존율이 용량 의존적으로 억제되었습니다. |
| 동물 실험 [2]: | |
동물 모형 | 성체 스위스 알비노 수컷 쥐 |
제조 방법 | TAPI-1은 멸균 생리 식염수에 5% DMSO를 혼합해서 희석하였습니다. 최종 사용 농도는 체종의 10mg/kg 이었습니다. 첫 번째 TAPI-1 용량은 황색 포도상구균 감염 후 24시간에 각 쥐에게 복강 내 투여되었고 감염 후 4일, 7일, 10일 및 13일에 반복 투여되었습니다. 대조 그룹 쥐는 희생 이틀 전에 TAPI-1 단일 용량을 투여받았습니다. |
제형 | 10mg/kg; i.p. |
응용 분야 | TAPI-1 투여는 황색 포도상구균 유도 관절염을 쥐의 발 부종을 현저하게 감소시켰습니다. TAPI-1 처리 후 관절염 관절 내 과산화물, 산화질소 및 과산화수소의 농도가 모두 감소하였습니다. |
References: | |
| Cas No. | 163847-77-6 | SDF | |
| Synonyms | TAPI | ||
| Chemical Name | N1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide | ||
| Canonical SMILES | NCCNC([C@@H](C)NC([C@H](NC(C(CC(C)C)CC(NO)=O)=O)CC1=CC2=CC=CC=C2C=C1)=O)=O | ||
| Formula | C26H37N5O5 | M.Wt | 499.6 |
| Solubility | ≥ 24.98mg/mL 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 | 2.0016 mL | 10.008 mL | 20.016 mL |
| 5 mM | 400.3 μL | 2.0016 mL | 4.0032 mL |
| 10 mM | 200.2 μL | 1.0008 mL | 2.0016 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 39 reference(s) in Google Scholar.)