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GNF-2

CAS No. : 778270-11-4

MCE 国际站：GNF-2

产品活性：GNF-2 是一种具有高度选择性、变构的、非 ATP 竞争性 Bcr-Abl 抑制剂。 GNF-2 抑制 Ba/F3.p210 增殖， IC₅₀ 为 138 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Anti-infection

作用靶点：Bcr-Abl  |  SARS-CoV

In Vitro: GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC₅₀ of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC₅₀ values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC₅₀ values of 268 and 194 nM, respectively).
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells.
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC₅₀ of 267 nM.

In Vivo: GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice.
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS.

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