IN-1130
Based on 2 publication(s) in Google Scholar
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
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- Pureza: 99.93%
- No. CAS: 868612-83-3
- Fòrmula: C25H20N6O
- Peso molecular:420.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) IN-1130
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Actividad biológica
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ALK5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
0.0442 μM
Compound: 6, IN-1130
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Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
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[PMID: 24786585] |
| HaCaT | IC50 |
0.0196 μM
Compound: 6, IN-1130
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Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
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[PMID: 24786585] |
| Sf9 | IC50 |
0.017 μM
Compound: 5, IN-1130
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Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay
Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay
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[PMID: 24704197] |
| Sf9 | IC50 |
0.017 μM
Compound: 6, IN-1130
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Inhibition of human recombinant GST-fused ALK5 expressed in insect Sf9 cells using casein as substrate by radiometric kinase assay
Inhibition of human recombinant GST-fused ALK5 expressed in insect Sf9 cells using casein as substrate by radiometric kinase assay
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[PMID: 21696866] |
| Sf9 | IC50 |
0.017 μM
Compound: 6, IN-1130
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Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay
Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay
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[PMID: 24786585] |
| Sf9 | IC50 |
0.017 μM
Compound: 6, IN-1130
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
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[PMID: 21435890] |
| Sf9 | IC50 |
0.036 μM
Compound: 8, IN-1130
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
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[PMID: 20472445] |
| Sf9 | IC50 |
17.2 nM
Compound: 5, IN-1130
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay
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[PMID: 23047226] |
| Sf9 | IC50 |
17.2 nM
Compound: 6, IN-1130
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay
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[PMID: 21911290] |
| Sf9 | IC50 |
36 nM
Compound: IN-1130
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Inhibition of GST fused human recombinant ALK5 expressed in Sf9 cells by radioisotopic protein kinase assay
Inhibition of GST fused human recombinant ALK5 expressed in Sf9 cells by radioisotopic protein kinase assay
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[PMID: 18571921] |
IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells[2].
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IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells[2].
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IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and 4T1 cells
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Concentration:0.5, 1 μM
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Incubation Time:For 2 hours
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Result:Inhibited TGF-β-stimulated Smad2 phosphorylation.
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Cell Line:MCF10A cells
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Concentration:1 μM
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Incubation Time:For 72 hours
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Result:Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.
? IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys[1].
? IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male Sprague–Dawley rats weighing 180-200 g[1]
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Dosage:10 and 20 mg/kg
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Administration:IP; daily; for 7 and 14 days
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Result:Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.
Chemical Information
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No. CAS 868612-83-3
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Appearance Solid
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Peso molecular 420.47
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Fòrmula C25H20N6O
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Color White to light yellow
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SMILES
O=C(N)C1=CC=CC(CC2=NC(C3=NC(C)=CC=C3)=C(C4=CC=C5N=CC=NC5=C4)N2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Oncogene
Olfactomedin 4 orchestrates TGF-β/CEACAM6 axis, promoting cell-autonomous epithelial to mesenchymal transition during gallbladder epithelium carcinogenesis. [Abstract]2026 Jul;45(24):2359-2374. PMID: 42050078 -
iScience
Organic phosphate but not inorganic phosphate regulates Fgf23 expression through MAPK and TGF-ꞵ signaling. [Abstract]2024 Mar 29;27(6):109625. PMID: 38883842
Solvente y solubilidad
DMSO : 100 mg/mL (237.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.43 mg/mL (3.40 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43. [Content Brief]
[2]. Park CY, et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80. [Content Brief]
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.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3783 mL | 11.8915 mL | 23.7829 mL | 59.4573 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL | 11.8915 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 mL | 5.9457 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5855 mL | 3.9638 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | 2.9729 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9819 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4864 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1891 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |
IN-1130 Related Classifications
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