XAV-939XAV-939
MedChemExpress (MCE)
HY-15147
284028-89-3
99.80%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Room temperature in continental US
may vary elsewhere.
XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation.
XAV-939 has activity against TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively[1]. XAV-939 (0.3-30 μM
3 or 10 days) enhances osteoblast differentiation of hBMSCs[2]. XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2[2]. XAV-939 (3 μM
10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation[2]. XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression[3].
XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo[3].
TNKS2 2 nM (IC50) TNKS1 5 nM (IC50) ARTD2 479 nM (IC50) ARTD1 5500 nM (IC50)
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[1]. Mohit Narwal, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24
56(20):7880-9. [Content Brief]
[2]. Nuha Almasoud, et al. Tankyrase inhibitor XAV-939 enhances osteoblastogenesis and mineralization of human skeletal (mesenchymal) stem cells. Sci Rep. 2020 Oct 7
10(1):16746. [Content Brief]
[3]. Senxin Cai, et al. Mechanical stress reduces secreted frizzled-related protein expression and promotes temporomandibular joint osteoarthritis via Wnt/β-catenin signaling. Bone. 2022 Aug
161:116445. [Content Brief]