SB 431542
SB 431542 (CAS 301836-41-9) is a selective ATP-competitive inhibitor targeting activin receptor-like kinase 5 (ALK5), a type I receptor within the transforming growth factor-β (TGF-β) signaling pathway. It inhibits ALK5 activity with an IC50 value of 94 nM, thereby preventing phosphorylation of Smad2 proteins and their subsequent nuclear accumulation. Additionally, SB 431542 inhibits closely related receptors ALK4 and ALK7, while showing minimal or no significant activity against ALK1, ALK2, ALK3, and ALK6 at relevant concentrations. Commonly utilized in cellular assays to investigate TGF-β signaling, this compound is valuable for studying associated cellular processes and diseases.
References:
[1] Callahan J F, Burgess J L, Fornwald J A, et al. Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5). Journal of medicinal chemistry, 2002, 45(5): 999-1001.
[2] Inman G J, Nicolás F J, Callahan J F, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Molecular pharmacology, 2002, 62(1): 65-74.
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| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 384.39 |
| Cas No. | 301836-41-9 |
| Formula | C22H16N4O3 |
| Solubility | insoluble in H2O; ≥10.06 mg/mL in EtOH with ultrasonic; ≥19.22 mg/mL in DMSO |
| Chemical Name | 4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide |
| SDF | Download SDF |
| Canonical SMILES | C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: [1] | |
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Cell lines |
D54MG, U87MG and U373MG cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
10 μM, 24 hours |
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Applications |
SB-431542 at both 0.1 and 1μmol/L had a modest effect on DNA synthesis, but at 10 μmol/L, there was a consistent 60% to 70% reduction of thymidine incorporation for D54MG, U87MG, and U373MG cells. No evidence of apoptotic cell death on SB-431542 treatment was detected either by direct observation or on propidium iodide flow cytometric analysis. Thus, SB-431542 acts to inhibit the proliferation of the tested malignant glioma lines. |
| Animal experiment: [2] | |
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Animal models |
BALB/c mice injected with colon-26 cells |
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Dosage form |
Intraperitoneal injection, 1 μM |
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Applications |
Intraperitoneal injection of SB-431542 resulted in triggering CTL activities against colon-26 targets compared with vehicle alone. Moreover, the CTL activity against colon-26 cells was more potent when treated with SB combined a ligand for toll-like receptor 4, OK-432, compared with OK-432 alone. Thus, SB-431542 is likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGFß. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Hjelmeland M D, Hjelmeland A B, Sathornsumetee S, et al. SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility. Molecular Cancer Therapeutics, 2004, 3(6): 737-745. [2] Tanaka H, Shinto O, Yashiro M, et al. Transforming growth factor b signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncology reports, 2010, 24: 1637-1643. |
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| Description | SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases. | |||||
| Targets | ALK5 | |||||
| IC50 | 94 nM | |||||
Quality Control & MSDS
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