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TGF-beta&Smad

SB505124 (694433-59-5)

SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively)…

Not Intended for Therapeutic Use. For research use only.

CAS: 694433-59-5 Category

SB505124 (694433-59-5) Description:

SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.

SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.1 Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.1 In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.

SB505124 (694433-59-5) Specifications:

Product Name SB505124
Synonyms SB-505124;SB 505124
Chemical Name 2-[4-(1,3-benzodioxol-5-yl)-2-~{tert}-butyl-1~{H}-imidazol-5-yl]-6-methylpyridine
Purity >98%
CAS Number 694433-59-5
Molecular Formula C20H21N3O2
Molecular Weight 335.407 g/mol
Monoisotopic Mass 335.163 g/mol
MDL number MFCD20926329
InChIKey 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 CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4
Form powder
Color yellow
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >5 years if stored properly
Handling Protect from air and light
Application An inhibitor of Activin receptor-like kinase 5; ALK5 inhibitor

 


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RIDADR NONH for all modes of transport

References:

Age-Dependent Effects of ALK5 Inhibition and Mechanism of Neuroprotection in Neonatal Hypoxic-Ischemic Brain Injury. Kim BH et al. Dev Neurosci. (2017).

TGFβ1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity. van Caam A et al. Arthritis Res Ther. (2017).

Forward genetic screening identifies a small molecule that blocks Toxoplasma gondii growth by inhibiting both host- and parasite-encoded kinases. Brown KM et al. PLoS Pathog. (2014)

1 review for SB505124 (694433-59-5)

  1. Cofttek

    Never had such good experience before,The SB505124 (694433-59-5) is high purity,also customer service is pretty nice !gotta try!!

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