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HomeProduct name listALK5 inhibitor II

ALK5 inhibitor II

Synonym(s):ALK5 Inhibitor II, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine;E-616452; 2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine;InSolution TGF-β RI Kinase Inhibitor II, RepSox - CAS 446859-33-2 - Calbiochem;RepSox InSolution, E-616452 InSolution, ALK5 Inhibitor II, Transforming Growth Factor-β, Type I Receptor Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine;TGF-β RI Kinase Inhibitor II - CAS 446859-33-2 - Calbiochem

ALK5 inhibitor II Structural

What is ALK5 inhibitor II?

Description

RepSox (446859-33-2) is a potent (IC50?ALK5 auto-P= 4 nM; IC50?TGF-β cellular assay = 23 nM) inhibitor of the TGF-β type I receptor (ALK5).1?RepSox can replace Sox2 in reprogramming adult cells into pluripotent stem cells via induction of Nanog transcription.2?It was able to convert astrocytes into neuronal cells as part of a small molecule cocktail (along with valproic acid and CHIR99021).3,4

The Uses of ALK5 inhibitor II

Alk 5 Inhibitor II is a selective ATP competitive inhibitor of transforming growth factor-β (TGFβ). A potential drug for the treatment of fibrosis and cancer.

The Uses of ALK5 inhibitor II

RepSox has been used as an inhibitor of autophosphorylation of the transforming growth factor β type I receptor kinase (ALK5). It has also been used as a basal media component for culturing human Pluripotent stem cells.

What are the applications of Application

ALK5 Inhibitor II is an ATP-competitive inhibitor of TGF-β RI kinase and has been used as an to inhibit autophosphorylation of ALK5.

Definition

ChEBI: 1,5-naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]- is a pyrazolopyridine.

Biochem/physiol Actions

RepSox Inhibits TGF-beta receptor signaling. Retroviral transduction of Sox2, Oct4, and Klf4 genes results in direct reprogramming of somatic cells into induced pluripotent stem cells (iPSCs).

storage

+4°C

References

1) Gellibert?et al. (2004),?Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors; J. Med. Chem.?47?4494 2) Ichida?et al.?(2009),?A Small-molecule Inhibitor of TGF-β Signaling Replaces Sox2 in Reprogramming by Inducing Nanog; Cell Stem Cell?5?491 3) Cheng?et al.?(2015),?Direct Conversion of astrocytes into neuronal cells by a drug cocktail;?Cell Res.?25?1269 4) Cheng?et al.?(2014),?Generation of neural progenitor cells by chemical cocktails and hypoxia; Cell Res.?24?665

Properties of ALK5 inhibitor II

Melting point: 195 °C
Boiling point: 501.9±50.0 °C(Predicted)
Density  1.296±0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: >20mg/mL
form  Yellow solid
pka 10.05±0.50(Predicted)
color  Pale yellow
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Safety information for ALK5 inhibitor II

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for ALK5 inhibitor II

InChIKey LBPKYPYHDKKRFS-UHFFFAOYSA-N

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