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> SB-431542 [301836-41-9]

SB-431542 [301836-41-9]

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Cat# HY-10431-50mg

Size : 50mg

Brand : MedChemExpress

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Description

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[1][2][3].

IC50 & Target[1]

ALK4

1 μM (IC50)

ALK5

0.75 μM (IC50)

ALK7

2 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HaCaT EC50
172 nM
Compound: 1a, SB-431542
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
[PMID: 20919678]
HEK-293T IC50
0.066 μM
Compound: SB-431542, SB
Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay
Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay
[PMID: 23130626]
HepG2 IC50
250 nM
Compound: SB-431542
Inhibition of TGFR-1 in human HepG2 cells expressing PAI-luciferase by luciferase reporter gene assay
Inhibition of TGFR-1 in human HepG2 cells expressing PAI-luciferase by luciferase reporter gene assay
[PMID: 19914068]
NCI-H1299 IC50
0.5 μM
Compound: 3, SB-431542
Antimigratory activity against human H1299 cells assessed as inhibition of cell migration after 12 to 24 hrs by transwell migration assay
Antimigratory activity against human H1299 cells assessed as inhibition of cell migration after 12 to 24 hrs by transwell migration assay
[PMID: 24417479]
Sf9 IC50
67.1 nM
Compound: SB-431542
Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay
Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay
[PMID: 31408333]
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[1].
SB-431542 (0- 10 μM; 24 h) inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are very highly related to ALK5 in their kinase domains[1].
SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 min) efficiently inhibits Smad phosphorylation induced by TGF-β and activin but not BMP4[1].
SB-431542 (0-10 μM) inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-431542 Related Antibodies

Western Blot Analysis[1]

Cell Line: NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells
Concentration: 10 μM; 0.1, 0.5, 1, 5, or 10 μM
Incubation Time: 24 h; 30 min
Result: Inhibited efficiently phosphorylated Smad2.
Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1.

Apoptosis Analysis[2]

Cell Line: A549 and HT29 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Inhibited TGF-induced growth suppression and apoptosis.

Cell Invasion Assay[2]

Cell Line: A549 cells
Concentration: 2, 10 μM
Incubation Time: 21 h
Result: Blocked TGF- induced tumor cell invasion.

Cell Migration Assay [2]

Cell Line: A549 cells
Concentration: 2, 10 μM
Incubation Time: 5 h , 30 h
Result: Blocked TGF- induced tumor cell migration.
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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3]
Dosage: 0.5 and 2 mM
Administration: Subconjunctival injection, on days 1, 2, 3, and 7
Result: Showed wound healing and less severe scar formation.
Molecular Weight

384.39

Formula

C22H16N4O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CC=C(C=C1)C2=NC(C3=CC=C4OCOC4=C3)=C(N2)C5=NC=CC=C5)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6015 mL 13.0076 mL 26.0152 mL
5 mM 0.5203 mL 2.6015 mL 5.2030 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, 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.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
References

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