XAV-939_product_DataBase

Bioactivity

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[1][2][3].

Invitro

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]. Cell Viability Assay[2] Cell Line:

In Vivo

XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo[3].

Name

XAV-939

CAS

284028-89-3

Formula

C14H11F3N2OS

Molar Mass

312.31

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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. [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. [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.

PeptideDB

XAV-939

CAS: 284028-89-3 F: C14H11F3N2OS W: 312.31