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首页-抗体药物偶连体和PROTACs-PROTAC-LD5095
LD5095

Chemical Structure : LD5095

CAS No.:

LD5095 (LD-5095)

货号: PC-26648Not For Human Use, Lab Use Only.

LD5095 is a potent, selective cereblon (CRBN)-recruiting RIPK1 degrader with DC50 of 1.4, 1.2, and 2.3 nM and Dmax>90% for endogenous RIPK1 in WT Jurkat, MOLM14, and U937 cell lines.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LD5095 is a potent, selective cereblon (CRBN)-recruiting RIPK1 degrader with DC50 of 1.4, 1.2, and 2.3 nM and Dmax>90% for endogenous RIPK1 in WT Jurkat, MOLM14, and U937 cell lines.
LD5095 achieves maximal RIPK1 degradation at 200 nM, reaching Dmax values of 94% in Jurkat cells, 95% in MOLM14 cells, and 91% in U937 cells.
LD5095 induces RIPK1 degradation which is strictly dependent on the specific recruitment of the CRBN E3 ligase and the subsequent activation of the entire ubiquitin-proteasome system (UPS) cascade in Jurkat cells.
LD5095 sensitizes Jurkat cells to TNFα-mediated apoptosis.
LD5095 exhibits negligible activity in murine B16F10 cells.

物理化学性质&存储条件

分子量 1165.29
分子式 C65H63F3N12O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((4-(1-(2-(6-(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)-2,6-diazaspiro[3.3]heptan-2-yl)-2-oxoethyl)piperidin-4-yl)phenyl)amino)piperidine-2,6-dione

参考文献

1. Lu D, et al. bioRxiv [Preprint]. 2026 Apr 14:2026.04.10.717852.

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