SB525334


Catalog No. size PriceQuantity
M6900-2 2mg solid $100
M6900-10 10mg solid $411

Description

Cas:356559-20-1

Product Information

SB525334 is a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 inhibited ALK5 kinase activity with an IC(50) of 14.3 nM and was approximately 4-fold less potent as an inhibitor of ALK4 (IC(50) = 58.5 nM). SB-525334 was inactive as an inhibitor of ALK2, ALK3, and ALK6 (IC(50) > 10,000 nM). In cell-based assays, SB-525334 (1 microM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells.

 

Chemical Formula: C21H21N5

 

Exact Mass: 343.1797

 

Molecular Weight: 343.42494

 

Elemental Analysis: C, 73.44; H, 6.16; N, 20.39

 

Chemical Name: 6-(2-(tert-butyl)-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline

 

InChi Key:

DKPQHFZUICCZHF-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)

 

Smiles Code:

CC1=CC=CC(C2=C(C3=CC=C4N=CC=NC4=C3)N=C(C(C)(C)C)N2)=N1

 

 

Technical Data:

 

Appearance: Yellow to orange solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM.

 

In Vivo:

SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH).

 

 

References

 

  1. Ramdas V, McBride M, Denby L, Baker AH. Canonical Transforming Growth Factor-β Signaling Regulates Disintegrin Metalloprotease Expression in Experimental Renal Fibrosis via miR-29. Am J Pathol. 2013 Dec;183(6):1885-96. doi: 10.1016/j.ajpath.2013.08.027. Epub 2013 Oct 6. PubMed PMID: 24103556.

 

  1. Ying WZ, Aaron KJ, Sanders PW. Transforming growth factor-β regulates endothelial function during high salt intake in rats. Hypertension. 2013 Nov;62(5):951-6. doi: 10.1161/HYPERTENSIONAHA.113.01835. Epub 2013 Sep 16. PubMed PMID: 24041947.

 

  1. Walshe TE, dela Paz NG, D'Amore PA. The role of shear-induced transforming growth factor-β signaling in the endothelium. Arterioscler Thromb Vasc Biol. 2013 Nov;33(11):2608-17. doi: 10.1161/ATVBAHA.113.302161. Epub 2013 Aug 22. PubMed PMID: 23968981.

 

  1. Peng R, Sridhar S, Tyagi G, Phillips JE, Garrido R, Harris P, Burns L, Renteria L, Woods J, Chen L, Allard J, Ravindran P, Bitter H, Liang Z, Hogaboam CM, Kitson C, Budd DC, Fine JS, Bauer CM, Stevenson CS. Bleomycin induces molecular changes directly relevant to idiopathic pulmonary fibrosis: a model for "active" disease. PLoS One. 2013;8(4):e59348. doi: 10.1371/journal.pone.0059348. Epub 2013 Apr 2. PubMed PMID: 23565148; PubMed Central PMCID: PMC3614979.

 

  1. Kim YJ, Hwang JS, Hong YB, Bae I, Seong YS. Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine. Anticancer Res. 2012 Mar;32(3):799-806. PubMed PMID: 22399597; PubMed Central PMCID: PMC3508670.

 

Products are for research use only. Not for human use.

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