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ALK5 inhibitor II

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ALK5 inhibitor II Basic information

Product Name:
ALK5 inhibitor II
Synonyms:
  • ALK5 INHIBITOR I
  • 2-(3-(6-METHYLPYRIDIN-2-YL)-1H-PYRAZOL-4-YL)-1,5-NAPHTHYRIDINE
  • 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
  • SJN 2511
  • 2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine
  • E 616452
  • E616452
  • E-616452
CAS:
446859-33-2
MF:
C17H13N5
MW:
287.32
Product Categories:
  • Selective inhibitor of the TGF-β type I receptor ALK5.
  • Smad
  • Inhibitors
  • TGF-beta
Mol File:
Mol File
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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
pka
10.05±0.50(Predicted)
form 
Yellow solid
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.
InChIKey
LBPKYPYHDKKRFS-UHFFFAOYSA-N
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Safety Information

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811
WGK Germany 
3
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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.

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).

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

ALK5 inhibitor IISupplier

Changzhou Fulangke Chemical Technology Co., Ltd. Gold
Tel
13776872728
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amwpl888@sina.cn
Abmole Bioscience Inc. Gold
Tel
021-50967598 02150967598
Email
sales@abmole.cn
Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
Email
jkinfo@jkchemical.com
3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
Email
3bsc@sina.com