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TO-1187

Chemical Structure : TO-1187

CAS No.:

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TO-1187 (TO1187)

Catalog No.: PC-24278Not For Human Use, Lab Use Only.

TO-1187 is a potent, selective, cereblon (CRBN)-based HDAC6 PROTAC degrader with DC50 of 5.81 nM in MM.1S cells (6 h), Dmax of 94%.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TO-1187 is a potent, selective, cereblon (CRBN)-based HDAC6 PROTAC degrader with DC50 of 5.81 nM in MM.1S cells (6 h), Dmax of 94%.
TO-1187 exhibits no cellular degradation of other HDACs.
TO-1187 does not impact the abundance of well-known CRBN neosubstrates, like IKZF1, IKZF3, CK1α, SALL4, and GSPT1.
TO-1187 efficiently degrades HDAC6 in mouse tissues, measured 6 h after intravenous injection.

Physicochemical Properties

M.Wt 681.71
Formula C34H35N9O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-((((1-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)(pyridin-3-ylmethyl)amino)methyl)-N-hydroxybenzamide

References

1. Garcha HK, et al. J Med Chem. 2025 Mar 10. doi: 10.1021/acs.jmedchem.4c02021.

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