Chemical Structure : Linker-free PROTAC Pro-DA
CAS No.:
2468065-01-0
Linker-free PROTAC Pro-DA
(Proline-Dasatinib analog)
Catalog No.: PC-24675Not For Human Use, Lab Use Only.
Linker-free PROTAC Pro-DA is a linker-free PROTAC degarder of BCR-ABL protein with DC50 of 8 nM in K562 cells, achieving a 93% reduction at 20 nM, shows cell growth IC50 of 0.9 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Linker-free PROTAC Pro-DA is a linker-free PROTAC degarder of BCR-ABL protein with DC50 of 8 nM in K562 cells, achieving a 93% reduction at 20 nM, shows cell growth IC50 of 0.9 nM.
Pro-DA-mediated decrease of BCR-ABL protein levels was largely blunted in GID4 knockout K562 cells.
ro-DA induces interaction between EML4-ALK and GID4 and subsequently promoted BCR-ABL ubiquitylation.
GID4, serving as the substrate receptor for the CTLH E3 ligase complex, is responsible for recognizing substrates featuring an N-terminal proline.
Physicochemical Properties
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M.Wt
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541.07
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Formula
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C25H29ClN8O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-N-(2-chloro-6-methylphenyl)-2-((2-methyl-6-(4-prolylpiperazin-1-yl)pyrimidin-4-yl)amino)thiazole-5-carboxamide
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References
1. Jianchao Zhang, et al. Nature Communications volume 16, Article number: 4794 (2025).
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