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Chemical Structure : DW0254
Catalog No.: PC-73367Not For Human Use, Lab Use Only.
DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.
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DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.
DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).
DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.
DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.
| M.Wt | 416.525 | |
| Formula | C25H28N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sara Canovas Nunes, et al. Blood Cancer J. 2022 Apr 14;12(4):64.
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