SB 431542 CAS: 301836-41-9
MF: C22H16N4O3
MW: 384.39

SB 431542 (CAS 301836-41-9)

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Noms alternatifs: SB 431542 is also known as TGF-β RI Kinase Inhibitor VI.
Application: SB 431542 is a Potent, selective inhibitor of TGF-βRI, specifically at ALK5 and its relatives ALK4 and ALK7.
Numéro CAS: 301836-41-9
Pureté: ≥98%
Masse Moléculaire: 384.39
Formule Moléculaire: C22H16N4O3
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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SB 431542 is a small molecule that acts as a specific and selective inhibitor of TGF-β (transforming growth factor-β) superfamily type I activin receptor-like kinase (ALK) receptors ALK4, 5, and 7. 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 also known as 4-[4-(1,3-Benzodioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide, TGF-β RI Kinase Inhibitor VI, and ALK inhibitor.


Références

1. Laping, N.J., et al. 2002. Mol. Pharmacol. 62: 58-64. PMID: 12065755

2. Inman, G.J., et al. 2002. Mol. Pharmacol. 62: 65-74. PMID: 12065756

3. Matsuyama, S., et al. 2003. Cancer Res. 63: 7791-7798. PMID: 14633705

4. Hjelmeland, M.D., et al. 2004. Mol. Cancer Ther. 3: 737-745. PMID: 15210860

État Physique :
Solid
Solubilité :
Soluble in DMSO (77 mg/ml at 25° C), ethanol (45 mg/ml at 25° C), DMF (~20 mg/ml), DMSO:PBS (pH 7.2) (1:1) (~ 0.5 mg/ml), and water (<1 mg/ml at 25° C).
STOCKAGE :
Store at -20° C
Point de fusion :
315.72° C (Predicted)
Point d'Ébullition :
~662.36° C at 760 mmHg (Predicted)
Densité :
~1.4 g/cm3 (Predicted)
Indice de Réfraction :
n20D 1.68 (Predicted)
IC50 :
TGFβ RII: IC50 = 66 nM (human); TGFβ RI: IC50 = 94 nM; ACTR-IB: IC50 = 140 nM
Ki Data :
TGFβ RI: Ki= 17 nM (human); casein kinase Iα: Ki= 100 nM (human); PKAα cat: Ki= >1.26 µM (human); CDK9: Ki= >1.58 µM (human); ARK-1: Ki= >1.58 µM (human)
Valeurs pK :
pKa: 10.14 (Predicted), pKb: 2.24 (Predicted)
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
PubChem CID :
Numéro MDL :
MFCD05865244
SMILES :
C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

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SB 431542 (CAS 301836-41-9)  Références bibliographiques

Consultez les publications faisant référence à l' utilisation de SB 431542 (CAS 301836-41-9). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 10 sur un total de 40

PMID: # 31313605  Lin, TC.|Lin, YY.|Hsu, CC.|Yang, YP.|Yang, CH.|Hwang, DK.|Wang, CY.|Liu, YY.|Lo, WL.|Chiou, SH.|Peng, CH.|Chen, SJ.|Chang, YL.| et al. 2019. Cell Transplant. 28: 1345-1357.

PMID: # 29337130  2018. Dev. Biol. 435: 26-40.

PMID: # 29886243  Fujita, M.|Tamano, R.|Yoneda, S.|Omachi, S.|Yogo, E.|Rokushima, M.|Shinohara, S.|Sakaguchi, G.|Hasegawa, M.|Asaki, T.| et al. 2018. Eur J Pharmacol. 833: 263-274.

PMID: # 28775339  Khan, FM. et al. 2017. Nat Commun. 8: 198.

PMID: # 29088702  Hangauer, MJ. et al. 2017. Nature. 551: 247-250.

PMID: # 25893292  Hwangbo, C. et al. 2016. Oncogene. 35: 389-401.

PMID: # 25754222  Caballé-Serrano, J. et al. 2016. Clin Oral Implants Res. 27: 226-32.

PMID: # 26279418  Wang, D. et al. 2015. Cell. Physiol. Biochem. 36: 2093-107.

PMID: # 26269769  Guo, Q. et al. 2015. Am J Cancer Res. 5: 2098-112.

PMID: # 25635683  Arshad, A. et al. 2015. PloS one. 10: e0115447.

Citations 1 à 10 sur un total de 40
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