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TGF-beta&Smad

SB431542 (301836-41-9)

SB-431542 is a novel small molecule inhibitor of the type I TGF-beta receptor, on a panel of human malignant glioma cell lines….

Not Intended for Therapeutic Use. For research use only.

CAS: 301836-41-9 Category

SB431542 (301836-41-9) Description:

SB-431542 is a novel small molecule inhibitor of the type I TGF-beta receptor, on a panel of human malignant glioma cell lines. SB-431542 blocked the phosphorylation and nuclear translocation of the SMADs, intracellular mediators of TGF-beta signaling, with decreased TGF-beta-mediated transcription. Furthermore, SB-431542 inhibited the expression of two critical effectors of TGF-beta-vascular endothelial growth factor and plasminogen activator inhibitor-1.

SB 431542 is 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. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a member of benzamides, a member of imidazoles, a member of pyridines and a member of benzodioxoles.

Renal carcinoma studies have demonstrated that SB 431542 is a selective inhibitor of Smad3 phosphorylation (IC50= 94nM) and TGF-β-1 collagen induced lα1 (col Iα1). It has been reported that SB 431542 does not affect the JNK, ERK, or p38 MAP kinase pathways. SB 431542 has been shown to suppress TGF-β induced growth stimulation in MG63 cells, inhibit the motility and proliferation of glioma cells, and block the phosphorylation and translocation of SMADs.

SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC50 = 94 nM)1. It is a less potent antagonist of ALK4 (IC50 = 140 nM)2 and ALK7.3 It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested.3 SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer.3 Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.

SB431542 (301836-41-9) Specifications:

Product Name SB431542
Synonyms SB-431542; SB 431542
Chemical Name 4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1~{H}-imidazol-2-yl]benzamide
Purity >98%
CAS Number 301836-41-9
Molecular Formula C22H16N4O3
Molecular Weight 384.395 g/mol
Monoisotopic Mass 384.122 g/mol
MDL number MFCD05865244
InChIKey FHYUGAJXYORMHI-UHFFFAOYSA-N
InChi Code InChI=1S/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26)
SMILES C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5
Form powder
Color white
Solubility  Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A specific and selective inhibitor of TGF-β type I ALK receptors and Smad3; TGF-beta/Smad inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • TGF-β Small Molecule Inhibitor SB431542 Reduces Rotator Cuff Muscle Fibrosis and Fatty Infiltration By Promoting Fibro/Adipogenic Progenitor Apoptosis. Davies MR et al. PLoS One. (2016)
  • Radiosensitization of Non-Small Cell Lung Cancer Cells by Inhibition of TGF-β1 Signaling With SB431542 Is Dependent on p53 Status. Zhao Y et al. Oncol Res. (2016)
  • SB431542 treatment promotes the hypertrophy of skeletal muscle fibers but decreases specific force. Watt KI et al. Muscle Nerve. (2010)

1 review for SB431542 (301836-41-9)

  1. Cofttek

    Never had such good experience before,The SB431542 (301836-41-9) is high purity,also customer service is pretty nice !gotta try!!

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