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| Product Name: | JW74 | | Synonyms: | JW74;4-[4-(4-Methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-pyridine;JW74;JW 74;Pyridine, 4-[4-(4-methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-;JW74 >=98% (HPLC);Inhibitor,JW74,JW-74,JW 74,inhibit,Wnt;5-(((4-(4-Methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio)methyl)-3-(p-tolyl)-1,2,4-oxadiazole | | CAS: | 863405-60-1 | | MF: | C24H20N6O2S | | MW: | 456.52 | | EINECS: | | | Product Categories: | | | Mol File: | 863405-60-1.mol |  |
| 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 | | pka | 1.63±0.10(Predicted) | | form | powder | | color | white to beige |
| 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. |
| | JW74 Preparation Products And Raw materials |
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