1. TGF-beta/Smad
  2. TGF-β Receptor
  3. IN-1130

IN-1130 

Cat. No.: HY-18758 Purity: 99.79%
Handling Instructions

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

IN-1130 Chemical Structure

CAS No. : 868612-83-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 110 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
25 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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[1][2].

IC50 & Target[1]

ALK5

 

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].

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].

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.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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IN-1130
Cat. No.:
HY-18758
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