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PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM. While not directly inhibiting tumor cell growth, PPM-3 affects tumor progression through influencing macrophage differentiation [1].
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| Description | PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM. While not directly inhibiting tumor cell growth, PPM-3 affects tumor progression through influencing macrophage differentiation [1]. |
| Targets&IC50 | ERK5:62.4 nM |
| In vitro | PPM-3, applied at a concentration of 200 nM for 0-72 hours to A375 cells, initiates ERK5 degradation within 2-4 hours, with peak degradation observed at 12 hours and sustained for at least 72 hours [1]. Additionally, PPM-3, ranging from 0-1 μM for 12 hours, exhibits ERK5 degradation activity in various cancer cell lines—H1975, HepG2, MDA-MB-231, PC-3, HCT116, and A375—with respective DC50 values of 11.5±2.5, 13.7±8.2, 22.7±13.3, 23.5±10.3, 5.6±1.9, and 41.4±22.3 nM [1]. |
| Molecular Weight | 1000.26 |
| Formula | C54H69N11O6S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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