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| 25mg |
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| 100mg |
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ITD-1 is a selective inhibitor of TGF-β signaling (IC50 = 0.85 μM); exhibits little or no inhibition of activin, Wnt or BMP signaling pathways. ITD-1 selectively enhanced the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 is a highly selective TGF-β inhibitor and reveals an unexpected role for TGF-β signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors. References:
| ln Vitro |
To find out if ITD-1 blocks Activin A/Nodal and/or TGFβ signaling, which use the same intracellular signaling cascade through Smad4, HEK293T cells were transfected with a Smad4 response element driving luciferase (SBE4-Luc). ITD-1 effectively blocks the phosphorylation of effector SMAD2/3 proteins induced by TGFβ2, with only a minimal response to Activin A. ITD-1 is an activin A weakening of the signal and partial adapters that suppresses TGFβ2 signaling with a similar efficacy (92% vs. 99%, respectively), however less potent than the ACVR1B/TGFBR1 alternative SB-431542 (IC50= 850 nM vs. 70 nM). ITD-1 preferentially increases secretion to cardiomyocytes from undefinable mesoderm, but not to endothelial cells or vascular smooth muscle. The function of TGFβ signaling in regulating the production of cardiomyocytes from multipotent cardiovascular progenitor cells is revealed by ITD-1 [1].
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| References |
[1]. Willems E, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012 Aug 3;11(2):242-52
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| Molecular Formula |
C27H29NO3
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|---|---|
| Molecular Weight |
415.52
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| Exact Mass |
415.21474
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| CAS # |
1099644-42-4
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| Related CAS # |
1099644-42-4
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| SMILES |
O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C(C4=CC=CC=C4)C=C3)OCC
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| InChi Key |
ULFUJLFTRWWLPO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29NO3/c1-5-31-26(30)23-17(2)28-21-15-27(3,4)16-22(29)25(21)24(23)20-13-11-19(12-14-20)18-9-7-6-8-10-18/h6-14,24,28H,5,15-16H2,1-4H3
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| Chemical Name |
ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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| Synonyms |
ITD1 ITD 1 ITD-1.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~28 mg/mL (~67.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4066 mL | 12.0331 mL | 24.0662 mL | |
| 5 mM | 0.4813 mL | 2.4066 mL | 4.8132 mL | |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4066 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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