| Identification | Back Directory | [Name]
2-(3-(6-METHYLPYRIDIN-2-YL)-1H-PYRAZOL-4-YL)-1,5-NAPHTHYRIDINE | [CAS]
446859-33-2 | [Synonyms]
RepSox
CS-204
E616452
E-616452
SJN 2511
E 616452
RepSox, >=98%
RepSox(E-616452
ALK5 INHIBITOR I
ALK5 Inhibitor II
RepSox (SJN 2511)
RepSox(ALK5 Inhibitor II)
TGF-β RI Kinase Inhibitor II
TGF-BETA RI KINASE INHIBITOR II
E-616452; SJN 2511; E616452; SJN2511; E 616452; SJN-2511
TGF-β RI Kinase Inhibitor II - CAS 446859-33-2 - Calbiochem
2-(3-(6-METHYLPYRIDIN-2-YL)-1H-PYRAZOL-4-YL)-1,5-NAPHTHYRIDINE
2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine
2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-
TRANSFORMING GROWTH FACTOR-BETA TYPE I RECEPTOR KINASE INHIBITOR I
E-616452;SJN 2511;ALK5 INHIBITOR II;TGF-&BETA RI KINASE INHIBITOR II
InSolution TGF-β RI Kinase Inhibitor II, RepSox - CAS 446859-33-2 - Calbiochem
RepSox 2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine | [Molecular Formula]
C17H13N5 | [MDL Number]
MFCD09037561 | [MOL File]
446859-33-2.mol | [Molecular Weight]
287.319 |
| Chemical Properties | Back Directory | [Melting point ]
195 °C | [Boiling point ]
501.9±50.0 °C(Predicted) | [density ]
1.296±0.06 g/cm3(Predicted) | [storage temp. ]
Store at +4°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. | [InChIKey]
LBPKYPYHDKKRFS-UHFFFAOYSA-N |
| Hazard Information | Back Directory | [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. | [Definition]
ChEBI: 1,5-naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]- is a pyrazolopyridine. | [Biological Activity]
Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=23nM, 4nM and 18nM for binding, auto-phosphorylation and cellular assay in HepG2 cells of TGF-β RI kinase, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK (IC50>16μM). | [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]
Store at -20°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 |
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