Art. -Nr.: HY-18758

IN-1130

2 Cited Publications

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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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Reinheit: 99.93%
CAS. Nr.: 868612-83-3
Formel: C₂₅H₂₀N₆O
Molecular Weight:420.47

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

IN-1130 Chemical Structure

CAS. Nr.: 868612-83-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ALK5

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.0442 μM Compound: 6, IN-1130	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	[PMID: 24786585]
HaCaT	IC₅₀	0.0196 μM Compound: 6, IN-1130	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	[PMID: 24786585]
Sf9	IC₅₀	0.017 μM Compound: 5, IN-1130	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	[PMID: 24704197]
Sf9	IC₅₀	0.017 μM Compound: 6, IN-1130	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	[PMID: 21696866]
Sf9	IC₅₀	0.017 μM Compound: 6, IN-1130	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	[PMID: 24786585]
Sf9	IC₅₀	0.017 μM Compound: 6, IN-1130	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	[PMID: 21435890]
Sf9	IC₅₀	0.036 μM Compound: 8, IN-1130	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	[PMID: 20472445]
Sf9	IC₅₀	17.2 nM Compound: 5, IN-1130	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	[PMID: 23047226]
Sf9	IC₅₀	17.2 nM Compound: 6, IN-1130	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	[PMID: 21911290]
Sf9	IC₅₀	36 nM Compound: IN-1130	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	[PMID: 18571921]

In Vitro

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].
? 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].
? 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.

Western Blot Analysis^[2]

Cell Line:

HepG2 and 4T1 cells
Concentration:

0.5, 1 μM
Incubation Time:

For 2 hours
Result:

Inhibited TGF-β-stimulated Smad2 phosphorylation.

RT-PCR^[2]

Cell Line:

MCF10A cells
Concentration:

1 μM
Incubation Time:

For 72 hours
Result:

Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.

In Vivo

IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats^[1].
? 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.

Animal Model:

Six-week-old male Sprague–Dawley rats weighing 180-200 g^[1]
Dosage:

10 and 20 mg/kg
Administration:

IP; daily; for 7 and 14 days
Result:

Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

Chemical Information

CAS. Nr. 868612-83-3
Appearance Solid
Molecular Weight 420.47
Formel C₂₅H₂₀N₆O
Color White to light yellow
SMILES

O=C(N)C1=CC=CC(CC2=NC(C3=NC(C)=CC=C3)=C(C4=CC=C5N=CC=NC5=C4)N2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3783 mL

11.8915 mL

23.7829 mL

5 mM

0.4757 mL

2.3783 mL

4.7566 mL

10 mM

0.2378 mL

1.1891 mL

2.3783 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

IN-1130

2 Cited Publications

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IN-1130

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) IN-1130

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IN-1130

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) IN-1130

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IN-1130 Related Classifications

HY-18758 Related Classifications