ITD 1 |
カタログ番号GC12108
One-Click Copy Product Info
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ITD 1は選択性のTGFβ受容体阻害剤である(IC50 = 460nM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1099644-42-4
Sample solution is provided at 25 µL, 10mM.
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ITD 1は選択性のTGFβ受容体阻害剤である(IC50 = 460nM)[1]。ITD 1はWnt/β-cateninシグナル伝達経路を阻害することで、心筋細胞への幹細胞の分化を促進する[2]。ITD 1は、心臓再生などの基礎研究に使われている[3-4]。
U87とU251細胞で、細胞の増殖は、ITD 1 (5μM；24時間)の処理後、阻害された[5]。ヒト線維芽細胞で、低酸素の条件下で、ITD 1 (5μM；24時間)によるTβRIIの阻害は、p-Smad2/3のレベルとコラーゲンの沈澱を減らす[6]。ヒト角膜内皮細胞で、ITD 1 (10μM；48時間)は細胞の増殖を阻害し、老衰を促進し、内皮細胞マーカーの発見を減らす[7]。
C57BL/6Jマウス、ITD 1 (20μL；2000ng；im；4日間)は筋肉で、TGF-βの活性を減らした[8]。Lewis細胞皮下腫瘍マウスモデルで、ITD 1 (5mg/kg；ip；5日間)はSmad2/3シグナル伝達を阻害することで、SAHA誘発の抗腫瘍免疫とCD8+ T細胞の活性化を弱めた[9]。
References:
[1]. Willems E, Cabral-Teixeira J, Schade D, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells[J]. Cell stem cell, 2012, 11(2): 242-252.
[2]. Zhong Q, Laco F, Liao M C, et al. Influencing the fate of cardiac and neural stem cell differentiation using small molecule inhibitors of alk5[J]. Stem cells translational medicine, 2018, 7(10): 709-720.
[3]. Plowright A T, Engkvist O, Gill A, et al. Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents[J]. Angewandte Chemie International Edition, 2014, 53(16): 4056-4075.
[4]. Lin Y H, Kang L, Feng W H, et al. Effects of lipids and lipoproteins on mesenchymal stem cells used in cardiac tissue regeneration[J]. International journal of molecular sciences, 2020, 21(13): 4770.
[5]. Sun Z, Yan T, Jiang H, et al. Claudin-3 facilitates the progression and mediates the tumorigenic effects of TGF-β in glioblastoma multiforme[J]. Medical Oncology, 2023, 40(9): 268.
[6]. Mingyuan X, Qianqian P, Shengquan X, et al. Hypoxia-inducible factor-1α activates transforming growth factor-β1/Smad signaling and increases collagen deposition in dermal fibroblasts[J]. Oncotarget, 2017, 9(3): 3188.
[7]. Ozen E A, Toprak E K, Donmez A Ç, et al. Investigation of the Effects of TGF-β and TGF-β Inhibitors on Cell Proliferation and Senescence in Human Corneal Endothelial Cells[J]. Acta Physiologica, 2023, 237.
[8]. Mázala D A G, Novak J S, Hogarth M W, et al. TGF-β–driven muscle degeneration and failed regeneration underlie disease onset in a DMD mouse model[J]. Jci Insight, 2020, 5(6): e135703.
[9]. Dong W, He B, Cao Y, et al. Low-dose SAHA enhances CD8+ T cell-mediated antitumor immunity by boosting MHC I expression in non-small cell lung cancer[J]. Cellular Oncology, 2025, 48(1): 249-264.
| 細胞実験[1]: | |
細胞株 | U87とU251細胞 |
準備方法 | U87とU251細胞を、1ウェルあたり5000細胞の密度で、96ウェルのプレートに播種し、37℃で24時間培養し、その後はDMSO、TGF-β1 (10ng/mL)またはITD 1 (5μM)で処理した。その後、10μLのCCK-8試薬を各ウェルに添加し、24時間培養した。細胞の生存率を評価した。 |
反応条件 | 5μM；24時間 |
アプリケーション | ITD 1処理後、細胞の増殖は阻害された。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6Jマウス |
準備方法 | 24日齢のマウスをイソフルランで麻酔し、後肢の前部から剃毛した。その後、28ゲージのインスリン注射器で、40μLのNTX (10μg/mL) を前脛骨筋（TA）に注射した。損傷部位をマークするために、針を最初は緑色のタトゥー染料に浸した。ITD 1処理群について、2000 ngのITD 1を30μLのNTX (10μg/mL)に添加し、片側のTA筋肉に注射したが、対側TA筋には30μLのNTXのみを与えた。最初の注射後の2と4日目に、20μLのITD 1 (2000ng)を、ITD 1注射側のTA筋肉に注射し、対側TA筋には同量の生理食塩水を与えた。 |
投与形態 | 20μL；2000ng；im；4日間 |
アプリケーション | ITD 1は筋肉で、TGF-βの活性を減らした。 |
References: | |
| Cas No. | 1099644-42-4 | SDF | |
| Chemical Name | (Z)-1-(5-(tert-butyl)isoxazol-3(2H)-ylidene)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea | ||
| Canonical SMILES | CC(C)(C1=C/C(NO1)=N/C(NC2=CC=C(C3=CN(C4=N3)C5=C(S4)C=C(OCCN6CCOCC6)C=C5)C=C2)=O)C | ||
| Formula | C29H32N6O4S | M.Wt | 560.67 |
| 溶解度 | ≥ 28.05mg/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 | 1.7836 mL | 8.9179 mL | 17.8358 mL |
| 5 mM | 356.7 μL | 1.7836 mL | 3.5672 mL |
| 10 mM | 178.4 μL | 891.8 μL | 1.7836 mL |
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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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)