GLPBio

ITD 1

Catalog No.: GC12108Purity:>99.50%
COASDSData Sheet
ITD 1 is a selective TGFβ receptor inhibitor (IC50 = 460nM).

Products are for research use only. Not for human use. We do not sell to patients.

ITD 1
Cas No.: 1099644-42-4
10mM (in 1mL DMSO)In Stock
$54.00
1
1mgIn Stock
$25.00
1
5mgIn Stock
$49.00
1
10mgIn Stock
$84.00
1
50mgIn Stock
$245.00
1
100mgIn Stock
$364.00
1
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Description

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.

Protocol

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:
[1]. 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.
[2]. 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1099644-42-4
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
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
Molecular Formula
C29H32N6O4S
Molecular Weight
560.67
Solubility
≥ 28.05mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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