MS8535 | SPIN1 inhibitor | Probechem Biochemicals

Chemical Structure : MS8535

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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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.

MS8535 (MS-8535, MS 8535)

Biological Activity

Physicochemical Properties

References

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