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
- CAS NO.:446859-33-2
- Empirical Formula: C17H13N5
- Molecular Weight: 287.32
- MDL number: MFCD09037561
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-17 16:00:36
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) |
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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