SB-431542 [301836-41-9]
Katalog-Nummer HY-10431-50mg
Size : 50mg
Marke : MedChemExpress
SB-431542 est un inhibiteur puissant et sélectif du récepteur ALK5 / TGF-β de type I avec une valeur IC50 de 94 nM.
SB-431542 ist ein wirksamer und selektiver Inhibitor des ALK5/TGF-β-Typ I-Rezeptors mit einem IC50 -Wert von 94 nM.
SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways.
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SB-431542 Chemische Struktur
CAS. Nr. : 301836-41-9
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- SB431542 (4.2 mg/kg; i.p.; single daily for 3 days) reduces the expression of α-SMA, collagen-I and p-Smad3 in SiO2-induced fibrosis lungs of mice.
- Western blot analyses show the repression of SMC specific markers in the sh-GPM6B TGF-β1 group are abolished by Alantolactone in the sh-GPM6B and the enrichment of SMC specific markers in the GPM6B-sgRNA cells is cancelled by treatment with SB431542.
- Western blot images show Smad2/3 phosphorylation is lower than baseline in the sh-GPM6B cells and higher than baseline in the GPM6B-sgRNA cells. The phosphorylation of Smad2/3 in the sh-GPM6B TGF-β1 group is elevated by Alantolactone and the phosphorylation is reduced by treatment with SB431542.
- Effects of the TGF‑β1 inhibitor SB (20 μM) on mechanical force‑induced COL‑1 and MMP‑1 mRNA expression.
- Western analysis of FN and α-SMA in cardiac fibroblasts or NIH3T3 with treatments of (+)‐isobicyclogermacrenal, spathulenol, oxymatrine (OMT), and SB431542 at indicated concentrations.
- Western blot analysis of EGFR, total and phosphorylated Smad3, total and phosphorylated ERK protein expression in cell lysates from two breast cancer cells pretreated with SB431542 and then stimulated with TGF-β for the indicated times.
- E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.
- p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.
- Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.
- Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.
- pSmad2/3 protein levels are down-regulated by the ALK5 inhibitor SB431542 (rGDF11 group vs. rGDF11+SB group, p=0.000).
- A549 cells are co cultured with 10.0 mM SB431542 for 48 h, the expression of TGF β1, Smad2 and caspase 3 are tested by western blot analysis and then analyzed.
- A549 cells are treated with 1.0% CSE with or without 10.0 mM SB431542 for 48 h, the levels of TGF β1, p Smad2, and MMP3 is assayed by western blot analysis.
- The protein level of Six2 and Ki67 after the treatment of phosphorylation Smad3 ( p-Smad3) inhibitor SB431542 (10 µM) for 48 h.
- To investigate the effect of SB431542 on the accumulation of TGFβ1 and MMP3 in MM cells, RPMI 8226 cells are treated with 10, 100 and 1,000 nmol/mL SB431542 for 48 h. Western blotting is performed. The results demonstrate that SB431542 significantly decreases the accumulation of TGFβ1 and MMP3 at 100 and 1,000 nmol/mL when compared with the control. Smad2, as a signaling molecule, can be initially activated by TGFβ1. Therefore, the effect of SB431542 on the expression of Smad2 and p-Smad2 in RPM
- 10-1000 nM of SB431542 are co-cultured with RLE-6TN cells for 48 h. Expressions of p-Smad2 and Smad are detected by Western blot.
- SB431542 is used to block the TGF-β1/Smad2 pathway and the expression of PLTP, p-Smad2 and cleaved caspase-3 is analyzed. (A) RLE-6TN cells are treated with 5–500 nM SB431542 for 72 h. Expression of PLTP and p-Smad2 is analyzed by Western blot. (B) CSE-treated rat lung epithelial cells are treated with 500 nM SB431542 to block the TGF-β1/Smad2 pathway.
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SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways. | |||||||||||||||||||||||||||||||||
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In Vitro | SB-431542 can inhibit the activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis
Apoptosis Analysis
Cell Invasion Assay
Cell Migration Assay
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In Vivo | SB-431542 (subconjunctival; 0.5 and 2 mM; on days 1, 2, 3, and 7) inhibits scar formation after glaucoma filtration surgery in New Zealand rabbits. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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384.39 | |||||||||||||||||||||||||||||||||
C22H16N4O3 | |||||||||||||||||||||||||||||||||
301836-41-9 | |||||||||||||||||||||||||||||||||
Solid | |||||||||||||||||||||||||||||||||
Off-white to yellow | |||||||||||||||||||||||||||||||||
O=C(C1=CC=C(C=C1)C2=NC(C3=CC=C4OCOC4=C3)=C(N2)C5=NC=CC=C5)N | |||||||||||||||||||||||||||||||||
Room temperature in continental US; may vary elsewhere. | |||||||||||||||||||||||||||||||||
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In Vitro: DMSO : ≥ 100 mg/mL (260.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Ethanol : 11.17 mg/mL (29.06 mM; Need ultrasonic and warming) *"≥" means soluble, but saturation unknown. Preparing Stock Solutions
View the Complete Stock Solution Preparation Table * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo: Select the appropriate dissolution method based on your experimental animal and administration route. For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Please enter your animal formula composition: % DMSO + % + % Tween-80 + % Saline The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE). Calculation results: Working solution concentration: mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL). The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE). Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline. If the continuous dosing period exceeds half a month, please choose this protocol carefully. Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution. | |||||||||||||||||||||||||||||||||
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[1]. Gareth J Inman, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2002 Jul;62(1):65-74.
[2]. Sunil K Halder, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21.
[3]. Yi-qin Xiao, et al. SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Invest Ophthalmol Vis Sci. 2009 Apr;50(4):1698-706.
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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Ethanol / DMSO | 1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL | 65.0381 mL |
5 mM | 0.5203 mL | 2.6015 mL | 5.2030 mL | 13.0076 mL | |
10 mM | 0.2602 mL | 1.3008 mL | 2.6015 mL | 6.5038 mL | |
15 mM | 0.1734 mL | 0.8672 mL | 1.7343 mL | 4.3359 mL | |
20 mM | 0.1301 mL | 0.6504 mL | 1.3008 mL | 3.2519 mL | |
25 mM | 0.1041 mL | 0.5203 mL | 1.0406 mL | 2.6015 mL | |
DMSO | 30 mM | 0.0867 mL | 0.4336 mL | 0.8672 mL | 2.1679 mL |
40 mM | 0.0650 mL | 0.3252 mL | 0.6504 mL | 1.6260 mL | |
50 mM | 0.0520 mL | 0.2602 mL | 0.5203 mL | 1.3008 mL | |
60 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0840 mL | |
80 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8130 mL | |
100 mM | 0.0260 mL | 0.1301 mL | 0.2602 mL | 0.6504 mL |
- Stem Cell/Wnt TGF-beta/Smad Apoptosis
- Organoid TGF-β Receptor Apoptosis
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
SB-431542301836-41-9SB431542SB 431542OrganoidTGF-β ReceptorApoptosisTransforming growth factor beta receptorsTGF-β receptor kinase inhibitor (TRKI)ALK4ALK5ALK7transcriptiongene expressionapoptosisgrowth suppressioncancersignal transduction pathwaysInhibitorinhibitorinhibit
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- SB-431542
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