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Chemical Structure : XYD129
Catalog No.: PC-22486Not For Human Use, Lab Use Only.
XYD129 is a highly potent and selective CBP/p300 degrader with IC50 of 21/30 nM, effectively degrades CBP/p300 proteins and exhibits potent inhibition of growth in acute leukemia cell lines (MOLM-16, IC50=7.4 nM).
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XYD129 is a highly potent and selective CBP/p300 degrader with IC50 of 21/30 nM, effectively degrades CBP/p300 proteins and exhibits potent inhibition of growth in acute leukemia cell lines (MOLM-16, IC50=7.4 nM).
XYD129 can effectively induce the formation of CBP/p300-PROTAC-CRBN.
XYD129 at 1000 nM for 24 h is almost completely depletion of CBP and p300 proteins in MOLM-16 cells.
XYD129 is dependent on the ubiquitin-proteasome system (UPS) and involves the binding of the degraders to CBP/p300 and CRBN.
XYD129 (30 mg/kg) once daily via intraperitoneal injection for 2 weeks suppresses the tumor growth in vivo in MOLM-16 xenograft NOD-SCID mouse model.
| M.Wt | 806.81 | |
| Formula | C41H39FN8O9 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Tianbang Wu, et al. J Med Chem. 2024 Jun 13;67(11):9194-9213.
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