ITD 1
目录号 : GC12108
ITD 1是一种选择性TGFβ受体抑制剂（IC50 = 460nM）。
Cas No.:1099644-42-4
Sample solution is provided at 25 µL, 10mM.
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ITD 1 is a selective TGFβ receptor inhibitor (IC50 = 460nM) [1]. ITD 1 promotes the differentiation of stem cells into cardiomyocytes by inhibiting the Wnt/β-catenin signaling pathway [2]. ITD 1 is used in basic research such as cardiac regeneration [3-4].
In U87 and U251 cells, cell proliferation was inhibited after ITD 1 (5μM; 24h) treatment [5]. In human fibroblasts, inhibition of TβRII by ITD 1 (5μM; 24h) under hypoxic conditions reduces p-Smad2/3 levels and collagen deposition [6]. In human corneal endothelial cells, ITD 1 (10μM; 48h) inhibits cell proliferation, accelerates senescence, and reduces the expression of endothelial cell markers [7].
In C57BL/6J mice, ITD 1 (20μL; 2000ng; im; 4d) reduced TGF-β activity in muscle [8]. In Lewis cell subcutaneous tumor mouse model, ITD 1 (5mg/kg; ip; 5d) weakened SAHA-induced anti-tumor immunity and CD8+ T cell activation by inhibiting Smad2/3 signaling [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.
ITD 1是一种选择性TGFβ受体抑制剂（IC50 = 460nM） [1]。ITD 1通过抑制Wnt/β-catenin信号通路促进干细胞向心肌细胞分化 [2]。ITD 1已用于心脏再生等基础研究 [3-4]。
在U87和U251细胞中，ITD 1（5μM；24h）处理后细胞增殖受到抑制 [5]。在人成纤维细胞中，低氧条件下ITD 1（5μM；24h）抑制TβRII可降低p-Smad2/3水平和胶原沉积 [6]。在人角膜内皮细胞中，ITD 1（10μM；48h）可抑制细胞增殖，加速衰老，并降低内皮细胞标志物的表达 [7]。
在C57BL/6J小鼠中，ITD 1（20μL；2000ng；im；4d）降低了肌肉中TGF-β的活性 [8]。在Lewis细胞皮下肿瘤小鼠模型中，ITD 1（5mg/kg；ip；5d）通过抑制Smad2/3信号传导减弱了SAHA诱导的抗肿瘤免疫和CD8+T细胞活化 [9]。
| Cell experiment [1]: | |
Cell lines | U87 and U251 cells |
Preparation Method | U87 and U251 cells were seeded at a density of 5,000 cells per well in 96-well plates and incubated at 37℃ for 24 hours before being treated with DMSO, TGF-β1 (10ng/mL), or ITD 1 (5μM). Following treatment, 10μL of CCK-8 reagent was added to each well and incubated for 24h. Cell viability was then assessed. |
Reaction Conditions | 5μM; 24h |
Applications | After ITD 1 treatment, cell proliferation was inhibited. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | 24-day-old mice were anesthetized with isoflurane and shaved from the anterior hind limbs. Then, 40μL of NTX (10μg/mL) was injected into the tibialis anterior (TA) muscle using a 28-gauge insulin syringe. The needle was first dipped in green tattoo dye to mark the injury site. For the ITD 1 treatment group, 2000 ng of ITD 1 was added to 30μL of NTX (10μg/mL) and injected into one TA muscle, while the contralateral TA muscle received only 30μL of NTX. On days 2 and 4 after the initial injection, 20μL of ITD 1 (2000ng) was injected into the TA muscle of the ITD 1-injected side, and the contralateral TA muscle received an equal volume of saline. |
Dosage form | 20μL; 2000ng; im; 4d |
Applications | ITD 1 reduced TGF-β activity in muscle. |
References: | |
| Cas No. | 1099644-42-4 | SDF | |
| 化学名 | (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 | ||
| 分子式 | C29H32N6O4S | 分子量 | 560.67 |
| 溶解度 | ≥ 28.05mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7836 mL | 8.9179 mL | 17.8358 mL |
| 5 mM | 0.3567 mL | 1.7836 mL | 3.5672 mL |
| 10 mM | 0.1784 mL | 0.8918 mL | 1.7836 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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