ALK5 inhibitor II 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

ALK5 inhibitor II Usage And Synthesis

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

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

ALK5 inhibitor II(446859-33-2)Related Product Information

• TYRPHOSTIN AG 1296
• ZM 336372
• ZM 306416 hydrochloride
• SU 4312
• DADEPYLIPQQG
• PF 543
• Valspodar
• PF-543 (Citrate)
• Y27632 (hydrochloride)
• SB 431542
• LY2109761
• SB525334
• 3-Cyclopentene-1,2-diol, 5-(4-aMino-1H-iMidazo[4,5-c]pyridin-1-yl)-3-(hydroxyMethyl)-, (Hydrochloride) (1:1), (1S,2R,5R)-
• CHIR-99021