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MS8535

Chemical Structure : MS8535

CAS No.:

MS8535 (MS-8535, MS 8535)

Catalog No.: PC-22053Not For Human Use, Lab Use Only.

MS8535 is a potent, selective and cell-active inhibitor of methyl-lysine reader protein SPIN1 with biochemical IC50 of 202 nM and ITC binding Kd of 30 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MS8535 is a potent, selective and cell-active inhibitor of methyl-lysine reader protein SPIN1 with biochemical IC50 of 202 nM and ITC binding Kd of 30 nM.
MS8535 displays high selectivity for SPIN1 over 38 epigenetic targets, including G9a/GLP, and >18-fold selective for SPIN1 over several other SPIN family members, such as SPIN2B (Kd = 0.56 μM), SPIN3 (Kd = 1.4 μM), and SPIN4 (Kd = 0.71 μM).
MS8535 concentration dependently blocks the interactions between SPIN1 and histone H3 in U2OS cells with EC50 of 1.1 uM in NanoBRET assay.

Physicochemical Properties

M.Wt 490.65
Formula C28H38N6O2
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

N1-(7-(3-(Isoindolin-2-yl)propoxy)-6-methoxy-4-(pyrrolidin-1-yl)quinazolin-2-yl)-N2,N2-dimethylethane-1,2-diamine

References

1. Yan Xiong, et al. J Med Chem. 2024 Mar 27. doi: 10.1021/acs.jmedchem.4c00121.

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