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SHP2-IN-8 是一种可逆、非竞争性、选择性、高效性的变构SHP2抑制剂(IC50= 23 nM,Ki= 22 nM),在细胞中也有效果。SHP2-IN-8 能引起显著的热位移(ΔTm = 7.01 ℃)。SHP2-IN-8 可抑制AKT 的磷酸化,诱导 Hela 细胞凋亡 (apoptosis)。
SHP2-IN-8 是一种可逆、非竞争性、选择性、高效性的变构SHP2抑制剂(IC50= 23 nM,Ki= 22 nM),在细胞中也有效果。SHP2-IN-8 能引起显著的热位移(ΔTm = 7.01 ℃)。SHP2-IN-8 可抑制AKT 的磷酸化,诱导 Hela 细胞凋亡 (apoptosis)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | SHP2-IN-8 is a reversible, noncompetitive, selective and efficient allosteric SHP2 inhibitor (IC50=23 nM, Ki=22 nM), which also has effects in cells. SHP2-IN-8 can cause significant thermal displacement( Δ Tm = 7.01 ℃)。 SHP2-IN-8 can inhibit the phosphorylation of AKT and induce apoptosis of Hela cells. |
体外活性 | SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells [1]. SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner [1]. SHP2-IN-8 (0-30 μM; 0-2 hour)concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines [1]. Cell Proliferation Assay Cell Line: Hela, KYSE-70, THP-1 [1] Concentration: 0, 1, 3, 10, 30 and 100 μM Incubation Time: 48 hours Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM. Apoptosis Analysis Cell Line: Hela [1] Concentration: 0, 10 and 30 μM Incubation Time: 24 hours Result: Induced the apoptosis of Hela cells in a concentration-dependent manner. Western Blot Analysis Cell Line: Hela and KYSE-70 [1] Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines. |
分子量 | 398.35 |
分子式 | C17H21Cl2N5S |
CAS No. | 1801692-60-3 |
存储 | Shipping with blue ice. |
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