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EUK‑134 CAS 81065‑76‑1 High‑Purity Powder SOD & Catalase Mimetic Antioxidant Raw Material

High‑purity EUK‑134 powder CAS 81065‑76‑1, also named Ethylbisiminomethylguaiacol Manganese Chloride, is a premium self‑regenerating antioxidant small‑molecule compound that mimics superoxide dismutase and catalase activity. This dark‑brown powder efficiently scavenges reactive‑oxygen‑species, decomposes hydrogen‑peroxide and resists UV‑induced photodamage. Widely used for cosmetic anti‑aging raw‑material formulation, skin‑inflammation relief, photoprotection and oxidative‑stress‑related cell‑mechanism laboratory research. Every batch undergoes strict purity inspection, bulk supply and customized‑packaging are available for global skincare‑material suppliers and biochemistry researchers.

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LY364947 CAS 396129-53-6 | Selective TGF-β Type I (ALK5) Inhibitor | Nutrabiotech Chem

LY364947 CAS 396129-53-6
Selective TGF-β Type I (ALK5) Inhibitor for EMT & Fibrosis Research

LY364947 (CAS 396129-53-6) is a potent, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with an IC50 of 51 nM. By blocking Smad2 phosphorylation it suppresses epithelial-mesenchymal transition (EMT), reduces fibronectin and vimentin, and restores E-cadherin — a clean tool for fibrosis, cancer-metastasis and retinal-degeneration research. Formula C17H12N4, MW 272.30. Research grade with COA.

LY364947CAS 396129-53-6ALK5TGF-beta RITGF-beta inhibitorEMT inhibitorFibrosisSmad2Cancer metastasisKinase inhibitor
Request a Quote Technical Specs
272.30
MW (C17H12N4)
ALK5
Primary target
51 nM
IC50

Molecular Information

Name: LY364947
CAS: 396129-53-6
Formula: C17H12N4
MW: 272.30 g/mol
IUPAC: 4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline
SMILES: C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4
Class: Quinoline-pyrazole ALK5 inhibitor
Core: Quinoline-linked pyrazole
Target: TGF-beta type I receptor (ALK5)
IC50: TGF-beta RI kinase ≈ 51 nM
Activity: Smad2 blockade; EMT suppression
Solubility: Soluble in DMSO; insol. in water/ethanol
Appearance: White to off-white powder
Storage: -20°C, dry, protect from light
396129-53-6
🧪
CAS Number
272.30
⚖️
Molecular Weight
ALK5 inhibitor
🎯
Primary Activity
≥98%
✅
Purity

Product Technical Specifications

Complete physicochemical properties and QC parameters for LY364947 (CAS 396129-53-6)

📋 Physicochemical Properties

  • Product NameLY364947
  • IUPAC Name4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline
  • CAS Number396129-53-6
  • Molecular FormulaC17H12N4
  • Molecular Weight272.30 g/mol
  • SourceSynthetic (small-molecule kinase inhibitor)
  • AppearanceWhite to off-white powder
  • Water SolubilityInsoluble
  • Organic SolubilityDMSO (>=24.4 mg/mL); ethanol-poor
  • Compound ClassQuinoline-pyrazole ALK5 inhibitor
  • HS Code2933.99

🔬 Quality Control & Handling

  • Purity (HPLC)>=98%
  • FormPowder (research grade)
  • Primary TargetTGF-beta type I receptor (ALK5)
  • Assay ReadoutSmad2 phosphorylation; EMT markers
  • SelectivitySelective ALK5; minimal off-target kinases
  • Storage Condition-20°C, sealed, dry, protect from light
  • Solution StabilityDMSO stock stable at -20°C; avoid freeze-thaw
  • ShippingCold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes5 mg / 25 mg / 100 mg / 500 mg / 1 g
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human therapeutic or veterinary use

Key Molecular Targets & Biology Nodes

LY364947 engages the canonical TGF-beta/Smad axis at its most upstream kinase node, making it a precise, pathway-specific probe for EMT, fibrosis and metastasis biology.

🧬 TGF-β type I receptor (ALK5)🧬 Smad2 / Smad3🧭 TGF-β/Smad pathway🔥 EMT markers (vimentin, fibronectin)🛡️ E-cadherin (restored)🧬 TGF-β1 ligand signaling🫁 Fibrosis (lung/kidney/liver)🦠 Cancer metastasis👁️ Retinal degeneration🔬 Anti-fibrotic screening

How LY364947 Works: Selective ALK5 Blockade of TGF-β/Smad Signaling

LY364947 targets the TGF-beta type I receptor (ALK5) kinase domain, shutting down the phosphorylation cascade that drives EMT and fibrosis.

1

Selective ALK5 (TGF-β RI) Inhibition

LY364947 is an ATP-competitive, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with a biochemical IC50 of ~51 nM and minimal off-target kinase activity.

2

Smad2 Phosphorylation Blocked

By occupying the ALK5 ATP pocket, LY364947 prevents phosphorylation of Smad2/3 — the canonical transducers of TGF-beta responses — halting downstream EMT transcription.

3

EMT Suppressed, E-cadherin Restored

With Smad signaling off, mesenchymal markers (fibronectin, vimentin) fall and epithelial E-cadherin is re-expressed, reducing cell migration and invasiveness in vitro and in vivo.

⚖️ LY364947 vs Comparators

  • LY364947 (this product)Selective ALK5; IC50 ~51 nM
  • SB431542 / SB525334Related ALK5 inhibitors
  • GalunisertibClinical ALK5 (LY2157299)
  • Selective EdgeClean ALK5; low off-target
  • Research NicheEMT / fibrosis / metastasis

♻️ Downstream Biological Consequences

  • EnzymeALK5 kinase down
  • PathwaySmad2/3 phosphorylation reduced
  • MesenchymalVimentin / fibronectin down
  • EpithelialE-cadherin restored
  • FunctionMigration / invasion reduced
  • ModelsFibrosis; EMT; retinal injury

Research & Application Areas

LY364947 is a core, pathway-selective reagent for EMT, fibrosis, cancer-metastasis and retinal-degeneration research.

🧬

EMT Research

Benchmark tool to suppress TGF-beta-induced EMT and quantify marker switching.

EMT
🫁

Fibrosis Studies

Anti-fibrotic screening in lung, kidney and liver disease models.

Fibrosis
🦠

Cancer Metastasis

Dissect TGF-beta-driven invasion and metastatic progression.

Metastasis
👁️

Retinal Degeneration

Validated in NMDA-induced retinal injury and neurovascular models.

Retina
🧪

TGF-β/Smad Mapping

Smad2 phosphorylation readouts and pathway dissection.

Signaling
💊

Anti-Fibrotic Screening

Reference inhibitor in phenotypic and compound screens.

Screening

Key Literature & Landmark Publications

Representative and landmark work on LY364947 as a selective ALK5/TGF-beta type I receptor inhibitor.

LY364947 as a selective TGF-beta type I receptor (ALK5) kinase inhibitor with IC50 = 51 nM. Biochemical characterization.
Landmark reference
LY364947 blocks Smad2 phosphorylation and reverses EMT markers in HOXB9-MCF10A cells. EMT model.
Representative study
LY364947 attenuates NMDA-induced retinal degeneration and vascular damage in rat models. Retinal injury model.
Representative study
LY364947 suppresses fibronectin/vimentin and restores E-cadherin in TGF-beta-stimulated epithelia. Fibrosis model.
Representative study
Selective ALK5 inhibition as a strategy in anti-fibrotic and anti-metastatic drug discovery. Review context.
Review

Available Sizes & Ordering

Research-grade LY364947 (CAS 396129-53-6) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard5 mgIn StockLab screening / assay calibrationSame/next-day ship
Medium25 mgIn StockDose-response / cell assaysSame/next-day ship
Large100 mgIn StockIn vivo / extended studiesSame/next-day ship
Bulk500 mgIn StockLead optimizationQuote to confirm
Industrial1 g+Made to orderProcess developmentBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is LY364947 and what is it used for?
LY364947 (CAS 396129-53-6) is a potent, highly selective inhibitor of the TGF-beta type I receptor kinase (ALK5), with an IC50 of 51 nM. It is used to study epithelial-mesenchymal transition (EMT), fibrosis (lung, kidney, liver), cancer metastasis and retinal degeneration by blocking TGF-beta/Smad signaling. Formula C17H12N4, MW 272.30. Supplied as research-grade material with COA.
How does LY364947 work (mechanism of action)?
LY364947 is an ATP-competitive, selective ALK5 inhibitor. It binds the TGF-beta type I receptor kinase domain, preventing phosphorylation of Smad2/3. This suppresses downstream EMT transcription — reducing mesenchymal markers (fibronectin, vimentin) and restoring epithelial E-cadherin — which lowers cell migration and invasiveness.
Is LY364947 selective for TGF-beta type I (ALK5)?
Yes. LY364947 is a benchmark selective ALK5/TGF-beta type I receptor inhibitor with minimal off-target kinase activity, making it ideal for isolating TGF-beta/Smad-specific effects without broadly disrupting other pathways. It does not inhibit TGF-beta type II receptors at relevant concentrations.
How soluble is LY364947 and how should it be prepared?
LY364947 is insoluble in water and ethanol but highly soluble in DMSO (>=24.4 mg/mL). Prepare a fresh DMSO stock, keep final culture DMSO <=0.1% to avoid cytotoxicity, and store both powder and solutions at -20°C. Research use only.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, structural confirmation (NMR) and identity data; MSDS/SDS is included and additional spectra (MS) are available on request.

Need LY364947 for Your Research?

Research-grade LY364947 (CAS 396129-53-6) — purity >=98% HPLC, COA included
Selective ALK5 / TGF-beta type I receptor inhibitor (IC50 51 nM) — request a quote today

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