IN-1130

Name: IN-1130
Brand: MedChemExpress
SKU: HY-18758
Rating: 4.5 (1 reviews)

Cat. No.: HY-18758 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

IN-1130 Chemical Structure

CAS No. : 868612-83-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 94	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 94	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE IN-1130

•iScience. 2024 Mar 26.

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•Related Screening Libraries:

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View All TGF-β Receptor Isoform Specific Products:

View All Isoforms

ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ALK5

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: 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: 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	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.

Molecular Weight

420.47

Formula

C₂₅H₂₀N₆O

CAS No.

868612-83-3

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.
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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

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

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

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.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (253 KB) HNMR (289 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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

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

Help & FAQs

Do most proteins show cross-species activity?
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:

IN-1130868612-83-3IN1130IN 1130TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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IN-1130

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IN-1130 Related Antibodies

1 Publications Citing Use of MCE IN-1130

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•Related Screening Libraries:

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View All TGF-β Receptor Isoform Specific Products:

Biological Activity

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Customer Review

IN-1130 Related Antibodies

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Complete Stock Solution Preparation Table

IN-1130 Related Classifications

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