| Identification | Back Directory | [Name]
JW74 | [CAS]
863405-60-1 | [Synonyms]
JW74
JW74;JW 74
JW74 >=98% (HPLC)
4-[4-(4-Methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-pyridine
Pyridine, 4-[4-(4-methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]- | [Molecular Formula]
C24H20N6O2S | [MDL Number]
MFCD07048962 | [MOL File]
863405-60-1.mol | [Molecular Weight]
456.52 |
| Chemical Properties | Back Directory | [Boiling point ]
699.4±65.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [pka]
1.63±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
Tankyrases (TNKS) are poly(ADP-ribose) polymerases (PARPs) that cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in a process known as poly(ADP-ribosyl)ation. TNKS have key roles in the Wnt signaling pathway as part of the β-catenin destruction complex. JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC50 value of 790 nM. It increases the levels of Axin2 and decreases β-catenin levels in colorectal cancer (CRC) cells, leading to down-regulation of Wnt target genes. JW 74 inhibits the growth of CRC xenograft tumors in mice. JW 74 induces apoptosis and differentiation in osteosarcoma cell lines. | [Uses]
JW 74 is an inhibitor that affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. | [in vitro]
previous study found that jw74 at the molecular level induced stabilization of axin2, a key component of the β-catenin destruction complex, leading to reduced levels of nuclear β-catenin. in addition, jw74 could induce reduced cell growth in all tested cell lines, partially due to a delay in cell cycle progression and partially because of an induction of caspase-3-mediated apoptosis. moreover, jw74 was able to induce the differentiation in u2os cells and also enhance differentiation of os cell lines that did not harbor a differentiation block [1]. | [in vivo]
previous animal study found that the dose of 150 mg/kg of jw74 in apcmin model could reduce the small intestinal adenoma by 48% and was comparable with celecoxib or rofecoxib. furthermore, it was noteworthy that jw74 became rapidly cleared from the blood stream due to its poor in vivo stability [2]. | [IC 50]
790 nm for canonical wnt signaling | [storage]
Store at +4°C | [References]
1. e. w. stratford, j. daffinrud, e. munthe, et al. the tankyrase-specific inhibitor jw74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. cancer med. 3(1), 36-46 (2014).2. waaler j et al. novel synthetic antagonists of canonical wnt signaling inhibit colorectal cancer cell growth. cancer res. 2011 jan 1;71(1):197-205. |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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