ChemicalBook Product Catalog Biochemical Engineering Inhibitors TGF-beta / Smad TGF-beta / Smad inhibitors ALK5 inhibitor II

ALK5 inhibitor II

Product NameALK5 inhibitor II
CAS446859-33-2
MFC17H13N5
MW287.32
EINECS
MOL FileMol File

Chemical Properties

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.
InChI	InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
InChIKey	LBPKYPYHDKKRFS-UHFFFAOYSA-N
SMILES	N1C2C(=NC=CC=2)C=CC=1C1=CNN=C1C1=NC(C)=CC=C1

Safety Information

Hazard Codes	T
Risk Statements	25
Safety Statements	45
RIDADR	UN 2811
WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

RepSox (446859-33-2) is a potent (IC50ALK5 auto-P= 4 nM; IC50TGF-β cellular assay = 23 nM) inhibitor of the TGF-β type I receptor (ALK5).1RepSox can replace Sox2 in reprogramming adult cells into pluripotent stem cells via induction of Nanog transcription.2It was able to convert astrocytes into neuronal cells as part of a small molecule cocktail (along with valproic acid and CHIR99021).3,4

Uses

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.

Uses

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.

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] FRANÇOISE GELLIBERT. Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors[J]. Journal of Medicinal Chemistry, 2004, 47 18: 4494-4506. DOI:10.1021/jm0400247
[2] JUSTIN K ICHIDA. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog.[J]. Cell stem cell, 2009, 5 5: 491-503. DOI:10.1016/j.stem.2009.09.012
[3] LIN CHENG. Direct conversion of astrocytes into neuronal cells by drug cocktail[J]. Cell Research, 2015, 25 11: 1269-1272. DOI:10.1038/cr.2015.120
[4] LIN CHENG. Generation of neural progenitor cells by chemical cocktails and hypoxia[J]. Cell Research, 2014, 24 6: 665-679. DOI:10.1038/cr.2014.32

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