XAV939

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

XAV-939 通过抑制 tankyrase1/2 选择性抑制 Wnt/β-catenin 介导的转录，在无细胞测定中 IC50 为 11 nM/4 nM。

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.

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.

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XAV939 | XAV 939 | XAV-939

Metabolic Enzyme/Protease

PPAR

TNKS1| TNKS2

Cancer

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284028-89-3

312.31

C14H11F3N2OS

>98% (HPLC)

DMSO: 12 mg/mL (38.42 mM)

O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1

2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-3H-thiopyrano[4,3-d]pyrimidin-4(5H)-one

(-20℃)

With Ice Pack

≥ 2 years