XAV939

SKU: orb1225436

Description

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.(In Vitro):XAV-939 has activity against TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively.XAV-939 (0.3-30 μM; 3 or 10 days) enhances osteoblast differentiation of hBMSCs.XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2.XAV-939 (3 μM; 10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation.XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression.(In Vivo):XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo.

Key Properties

• CAS Number: 284028-89-3
• MW: 312.31
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₁F₃N₂OS
• SMILES: O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1
• Target: PPAR
• Solubility: DMSO: 12 mg/mL (38.42 mM)

Bioactivity

• In Vitro:
  XAV-939 (GMP) (5 μM; 2 μM for 3 days; 1 μM) induces human pluripotent stem cells (hPSCs) to post-mitotic cortical neurons differentiation. XAV939 (GMP) promotes anterior CNS identity. RT-PCR Cell line: Human pluripotent stem cells (hPSCs). Concentration: 5 μM, 2 μM, 1 μM. Incubation time: 3 days. Result: Showed downregulation of the pluripotency marker OCT4 and induction of neural and neuronal markers PAX6, FOXG1 and DCX, as well as markers of early born cortical neurons, including TBR1 (preplate, subplate and layer VI) and REELIN, in LSB+X/P/S/D conditions.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

XAV939 | XAV 939 | XAV-939

Quick Database Links

Gene Symbol

PPAR