Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2.
説明 | SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2. |
In vitro | SHP2 protein degrader-1 (compound SP4), at concentrations ranging from 0-200 μM over 24 hours, significantly inhibits Hela cell growth, demonstrating an IC50 of 5.77 and 4.30 nM, respectively. These values imply an efficacy about 100 times greater than that of SHP099 (SHP2 inhibitor). When applied at 0-200 μM for 96 hours, this compound leads to a marked induction of apoptotic death (54.01%) at 100 nM, which starkly contrasts with the 0.13% baseline observed in the control group. Additionally, the same concentration and exposure time result in arrest of the cell cycle at the G1 phase and a significant reduction in the phosphorylation of JNK, Erk, and p38, crucial components in cell signaling pathways. These effects are attributed to the inhibition of RAS/MAPK signaling through a mechanism that involves blocking SHP2's catalytic activity, underscoring compound SP4's potential as a potent inhibitor of cellular growth and pro-apoptotic agent in Hela cells. |
別名 | SHP2 protein degrader-1 |
分子量 | 908.84 |
分子式 | C42H51Cl2N11O8 |
CAS No. | 2624181-69-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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