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Merck
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Key Documents

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Safety Information

SML2819

Sigma-Aldrich

AZ12799734

≥98% (HPLC)

Synonym(s):

4-[[4-[(2,6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide, 4-[[4-[(2,6-Dimethylpyridin-3-yl)oxy]pyridin-2-yl]amino]benzenesulfonamide, AZ 12799734, AZ-12799734

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About This Item

Empirical Formula (Hill Notation):
C18H18N4O3S
CAS Number:
1117684-36-2
Molecular Weight:
370.43
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and availability is not currently available.

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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B18R Plasmid (human codon optimized) To supply B18R RNA that suppresses IFN responses to support Simplicon® RNA or normal mRNA expression

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B18R Plasmid (human codon optimized)

TagGFP2 Simplicon® Plasmid (E3L) To determine optimal transfection conditions to express the self-replicating RNA of your interest through using Simplicon Cloning Vector (E3L) (Part #:SCR724) in hard-to- transfect somatic or primary cells

SCR725

TagGFP2 Simplicon® Plasmid (E3L)

TagRFP Simplicon® Plasmid (E3L)

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TagRFP Simplicon® Plasmid (E3L)

technique(s)

nucleic acid detection: suitable (RNA)

technique(s)

nucleic acid detection: suitable (RNA)

technique(s)

nucleic acid detection: suitable (RNA)

technique(s)

nucleic acid detection: suitable (RNA)

Biochem/physiol Actions

AZ12799734 is an orally active TGF-β type I receptors active site inhibitor (ALK1/2/3/4/5/6 Kd = 7.1/6.2/40/1/0.74/0.017 μM) that inhibits ALK5-dependent Smad2 nuclear translocation upon TGF-β1 stimulation (IC50 = 17 nM; MDA-MB-468), as well as ALK1/2/3/6-mediated Smad1 and ALK4/5/7-mediated Smad2 phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12799734 oral administration in rats results in heart valve lesions (200 mg/kg/day for 5 days) and physeal dysplasia (400 mg/kg/day for 6 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
Orally active TGF-β type I receptors ALK1-7 active site inhibitor in vitro and in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Regulatory Information

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    Certificates of Analysis (COA)

    Lot/Batch Number
    0000098425
    0000098426
    0000095945

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    Frederick W Goldberg et al.
    Journal of medicinal chemistry, 52(23), 7901-7905 (2009-09-10)
    A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel
    Jason S L Yu et al.
    Stem cells (Dayton, Ohio), 37(7), 958-972 (2019-04-02)
    Direct in vivo reprogramming of cardiac fibroblasts into myocytes is an attractive therapeutic intervention in resolving myogenic deterioration. Current transgene-dependent approaches can restore cardiac function, but dependence on retroviral delivery and persistent retention of transgenic sequences are significant therapeutic hurdles.
    Mark J Anderton et al.
    Toxicologic pathology, 39(6), 916-924 (2011-08-24)
    Aberrant signaling by transforming growth factor-β (TGF-β) and its type I (ALK5) receptor has been implicated in a number of human diseases and this pathway is considered a potential target for therapeutic intervention. Transforming growth factor-β signaling via ALK5 plays
    Lindsay C Spender et al.
    Molecular pharmacology, 95(2), 222-234 (2018-11-22)
    The transforming growth factor β (TGFβ) superfamily includes TGFβ, activins, inhibins, and bone morphogenetic proteins (BMPs). These extracellular ligands have essential roles in normal tissue homeostasis by coordinately regulating cell proliferation, differentiation, and migration. Aberrant signaling of superfamily members, however

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