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HomeProduct name listSB 431542

SB 431542

Synonym(s):4-(5-Benzol[1,3]dioxol-5-yl-4-pyrldin-2-yl-1H-imidazol-2-yl)-benzamide hydrate;4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-benzamide hydrate;4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]-benzamide hydrate;

SB 431542 Structural

What is SB 431542?

Description

SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC50 = 94 nM). It is a less potent antagonist of ALK4 (IC50 = 140 nM) and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer. Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.

The Uses of SB 431542

SB 431542 is a known Src family kinase inhibitor that effectively blocks the transforming growth factor-β1-induced cell migration and invasion in both established and primary carcinoma cells.

The Uses of SB 431542

SB 431542 is a known Src family kinase inhibitor that effectively blocks the transforming growth factor-β1-induced cell migration and invasion in both established and primary carcinoma cells. Potent TGF-beta inhibitor.

What are the applications of Application

SB 431542 is a Potent, selective inhibitor of TGF-βRI, specifically at ALK5 and its relatives ALK4 and ALK7.

Definition

ChEBI: A member of the class of benzamides that is 4-(imidazol-2-yl)benzamide carrying additional 1,3-benzodioxol-5-yl and pyridin-2-yl substituents at positions 4 and 5 respectively on the imidazole ring.

General Description

A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 μM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC50 = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC50 ≥10 μM in the presence of 10 μM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).

Biological Activity

Potent and selective inhibitor of the transforming growth factor- β (TGF- β ) type I receptor activin receptor-like kinase ALK5 (IC 50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF- β -induced proliferation of human osteosarcoma cells. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells.

Biochem/physiol Actions

SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.

storage

Room temperature

References

1) Laping et al. (2002), Inhibition of transforming growth factor (TGF-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I kinase activity: SB-431542; Mol. Pharmacol., 62 58 2) Inman et al. (2002), SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5 and ALK7; Mol. Pharmacol., 62 65 3) Matsuyama et al. (2003), SB-431542 and Gleevec inhibit transforming growth factor-beta-induced proliferation of human osteosarcoma cells; Cancer Res., 63 7791 4) Watabe et al. (2003), TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells; J. Cell Biol., 163 1303 5) Stanslowsky et al. (2014), Functional differentiation of midbrain neurons from human cord blood-derived induced pluripotent stem cells; Stem Cell Res. Ther., 5 35

Properties of SB 431542

Melting point: 214 °C(dec.)
Boiling point: 662.4±55.0 °C(Predicted)
Density  1.373
Flash point: 354.4℃
storage temp.  Sealed in dry,Store in freezer, under -20°C
solubility  DMSO: 10 mg/mL, soluble
form  powder
pka 10.14±0.10(Predicted)
color  Yellow
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Safety information for SB 431542

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for SB 431542

InChIKey FHYUGAJXYORMHI-UHFFFAOYSA-N

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