Chemical Structure : LD5097
CAS No.:
LD5097
(LD-5097)
Catalog No.: PC-25704Not For Human Use, Lab Use Only.
LD5097 is a potent, selective RIPK1 PROTAC degrader with DC50 of 0.7 nM in Jurkat cells, Dmax=96% (24h).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LD5097 is a potent, selective RIPK1 PROTAC degrader with DC50 of 0.7 nM in Jurkat cells, Dmax=96% (24h).
LD5097 induces dose-dependent degradation of endogenous RIPK1 after 24 h in Jurkat cells, with DC50 and Dmax values of 2.6 nM and 98%, respectively, in western blot assay.
LD5097 exhibited potent degradation of endogenous RIPK1, with DC50 values of 2.8 and 0.8 nM, respectively, in both MOLM14 and U937 cells.
LD5097 acts as a PROTAC dependent on the VHL E3 ligase and ubiquitin-proteasome system to degrade RIPK1 in the cells.
(100 nM) sensitizes Jurkat cells to TNFα-mediated apoptosis.
LD5097 (10-100 mg/kg, i.v.) induces a reduction of RIPK1 protein levels by more than 70% at both 6 and 24 h postadministration in Jurkat subcutaneous xenograft mouse model.
Physicochemical Properties
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M.Wt
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1382.55
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Formula
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C74H75F4N13O8S
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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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(2S,4R)-N-((S)-3-(4-(5-((4-(4-(4-Amino-5-(1-(2-(3-(trifluoromethoxy)phenyl)acetyl)indolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)piperidine-1-carbonyl)phenyl)ethynyl)pyridin-2-yl)piperazin-1-yl)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
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References
1. Dong Lu, et al. J Med Chem. 2025 Oct 24. doi: 10.1021/acs.jmedchem.5c00773.
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