RepSox (E-616452) - 10mM in DMSO , CAS No.446859-33-2

CAS: 446859-33-2 Cat. No.: R408431 Peso molecular: 287.32 Número EC: 663-924-9

GRADE & PURITY 10mM in DMSO

Synonyms

SJN 2511,ALK5 Inhibitor II | 1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of theTGFβR-1/ALK5withIC50of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.
In vitro

RepSox inhibits ATP binding to ALK5 and ALK5 autophosphorylation with IC50 of 23 nM and 4 nM, respectively. RepSox inhibits TGF-β induced cellular PAI-1 luciferase activity with IC50 of 18 nM. RepSox is able to successfully replace Sox2 in reprogramming by inhibiting transforming growth factor-β (Tgf-β) signaling, which in turn induces Nanog expression. Effect of RepSox inducing reprogramming does not require chromatin remodeling. RepSox is found to be efficient at generating iPSCs.

In vivo

RepSox is able to be contribute to forming chimeric embryos in vivo when injected into blastocysts. A one-day treatment with RepSox is sufficient to replace transgenic Sox2.
Cell Data

cell lines：MCF-7 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

SJN 2511, ALK5 Inhibitor II | 1, 5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Nombres e identificadores

• Isómeros SMILES: CC1=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4
• WGK Alemania: 3
• Peso molecular: 287.32

Objetivos asociados (humanos)

TGFBR1 Tchem TGF-beta receptor type-1 (4 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: 47 mg/mL (198.09 mM); Ethanol: 21 mg/mL (88.51 mM); Water: Insoluble
• Punto de fusión (°C): 195 °C