SB 431542A specific and selective inhibitor of TGF-β type I ALK receptors and Smad3

SB 431542 (CAS 301836-41-9)

SB 431542 | CAS 301836-41-9 is rated 5.0 out of 5 by 1.
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Synonym: 4-[4-(1,3-Benzodioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide
Application: A specific and selective inhibitor of TGF-β type I ALK receptors and Smad3
CAS Number: 301836-41-9
Purity: ≥98%
Molecular Weight: 384.39
Molecular Formula: C22H16N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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SB 431542 is a small molecule that acts as a specific and selective inhibitor of TGFβ RI, ACTR-IB and ACTR-IC (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.


References

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

Physical State :
Solid
Solubility :
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).
Storage :
Store at -20° C
Melting Point :
315.72° C (Predicted)
Boiling Point :
~662.36° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
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)
pK Values :
pKa: 10.14 (Predicted), pKb: 2.24 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
4521392
MDL Number :
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

Download SDS (MSDS)

Certificate of Analysis

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SB 431542  Product Citations

See how others have used SB 431542. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 31 total

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

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

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

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

PMID: # 26819576  Zhang, X. et al. 2015. PPAR Res. 2015: 489314.

PMID: # 26060017  Li, XQ. et al. 2015. Cancer research. 75: 3302-13.

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

PMID: # 26626025  Shimojo, D. et al. 2015. Molecular brain. 8: 79.

PMID: # 25909165  Zhao, L. et al. 2015. Oncotarget. 6: 9781-93.

PMID: # 26197043  Laudanski, K. et al. 2015. Anesthesiology. 123: 628-41.

Citations 1 to 10 of 31 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. The compound, sc-204265, is provided as a light yellow to off-white powder. If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-12

What is the&nbsp;re-test date for lot G0116 of sc-204265?

Asked by: two2igm05
Thank you for your question. For any lot, we recommend re-testing the chemical every year to make sure it is maintaining its original quality. Contact technical service to ask about your specific lot.
Answered by: Tech Service 9
Date published: 2016-12-15
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Rated 5 out of 5 by from Dogar Dogar, AM. et al. (PubMed 21402698) used SB 431542, a selective inhibitor of the TGF- superfamily, in HeLa cells to inhibit T RI and suppressing latent TGF- 1. -SCBT Publication Review
Date published: 2015-02-15
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