SB505124


Catalog No. size PriceQuantity
M6691-2 2mg solid $78
M6691-10 10mg solid $316

Description

Cas:694433-59-5

Product Information

SB505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5, ALK4 and ALK7) with potential anticancer activity. SB505124 selectively inhibits signaling from TGF-β and activin; does not inhibit other ALK family members. SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK 7-dependent activation of downstream cytoplasmic signal transducers, Smad2 and Smad3, and of TGF-beta-induced mitogen-activated protein kinase pathway components but does not alter ALK1, ALK2, ALK3 or ALK6-induced Smad signaling.

 

Chemical Formula: C20H21N3O2

 

Exact Mass: 335.16338

 

Molecular Weight: 335.4 

 

Elemental Analysis: C, 71.62; H, 6.31; N, 12.53; O, 9.54

 

Synonym: 

 

SB505124

SB-505124

SB 505124

 

Chemical Name:

2-(4-(benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl)-6-methylpyridine

 

InChi Key:

WGZOTBUYUFBEPZ-UHFFFAOYSA-N

 

InChi Code:    InChI=1S/C20H21N3O2/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15/h5-10H,11H2,1-4H3,(H,22,23)

 

Smiles Code:

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1

 

 

Technical Data:

 

Appearance: Light peach to pale pink 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: >5 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

SB505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells. SB505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro. SB505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC.

 

In Vivo

SB505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals.

 

 

References

 

  1. Onai T, Takai A, Setiamarga DH, Holland LZ. Essential role of Dkk3 for head formation by inhibiting Wnt/β-catenin and Nodal/Vg1 signaling pathways in the basal chordate amphioxus. Evol Dev. 2012 Jul;14(4):338-50. doi: 10.1111/j.1525-142X.2012.00552.x. PubMed PMID: 22765205.

 

  1. Joseph C, Hunter MG, Sinclair KD, Robinson RS. The expression, regulation and function of secreted protein, acidic, cysteine-rich in the follicle-luteal transition. Reproduction. 2012 Sep;144(3):361-72. doi: 10.1530/REP-12-0099. Epub 2012 Jun 25. PubMed PMID: 22733805.

 

  1. Kocic J, Bugarski D, Santibanez JF. SMAD3 is essential for transforming growth factor-β1-induced urokinase type plasminogen activator expression and migration in transformed keratinocytes. Eur J Cancer. 2012 Jul;48(10):1550-7. doi: 10.1016/j.ejca.2011.06.043. Epub 2011 Jul 26. PubMed PMID: 21798735.

 

  1. Fang LP, Lin Q, Tang CS, Liu XM. Hydrogen sulfide attenuates epithelial-mesenchymal transition of human alveolar epithelial cells. Pharmacol Res. 2010 Apr;61(4):298-305. doi: 10.1016/j.phrs.2009.10.008. Epub 2009 Nov 11. PubMed PMID: 19913099.

 

  1. Sinpitaksakul SN, Pimkhaokham A, Sanchavanakit N, Pavasant P. TGF-beta1 induced MMP-9 expression in HNSCC cell lines via Smad/MLCK pathway. Biochem Biophys Res Commun. 2008 Jul 11;371(4):713-8. doi: 10.1016/j.bbrc.2008.04.128. Epub 2008 May 5. PubMed PMID: 18457660.

 

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

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