SB505124 - Moligand™, 10mM in DMSO , Inhibitor of transforming growth factor beta receptor 1, CAS No.694433-59-5, Inhibitor of transforming growth factor beta receptor 1

CAS: 694433-59-5 Cat. No.: S408748 Peso molecular: 335.4 PubChem CID: 9858940

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

SB505124 is a selective inhibitor ofTGFβRforALK4,ALK5withIC50of 129 nM and 47 nM in cell-free assays, respectively, also inhibitsALK7, but does not inhibit ALK1, 2, 3, or 6.
In vitro

SB505124 is identified as a reversible ATP competitive and selective ALK inhibitor of ALK4 and ALK5. SB505124 shows no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 hours, and blocks TGF-β–induced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner. In human umbilical vein endothelial cells (HUVEC), SB505124 (500 nM) blocks the changes of TGF-β1 on F-actin assembly and prevents ROS production induced by TGF-β. By inhibiting TGF-beta1 signaling, SB505124 leads to decreased deferoxamine (DFO)-induced neurogenesis. A recent study shows that SB505124 suppresses the migration and invasion of breast cancer MCF-7-M5 cells.

In vivo

In a rabbit GFS model, SB505124 decreased the intraocular pressure (IOP) levels and reduces subconjunctival cell infiltration and scarring at the surgical site in the GFS. In tacrolimus (TAC)-treated mice and FK12EC KO mice, SB505124 prevents the activation of endothelial TGF-β receptors and induction of renal arteriolar hyalinosis.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：48 hours

Powder Purity:≥98%

Specifications

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of transforming growth factor beta receptor 1

Nombres e identificadores

• Isómeros SMILES: CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4
• PubChem CID: 9858940
• Peso molecular: 335.4

Objetivos asociados (humanos)

TGFBR1 Tchem TGF-beta receptor type-1 (1 Activities)

Discover Target: TGFBR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 48 mg/mL (201.46 mM); Ethanol: 25 mg/mL (104.92 mM); Water: Insoluble
• Punto de fusión (°C): 168 °C