M2I-1

A cell-permeable nitrobenzylidene-thiobarbiturate compound that directly targets the hydrophobic core of Mad2 and selectively disrupts Mad2-Cdc20 complex formation. Shown to dose-dependently inhibit the interaction of Mad2 to Mad2-binding-peptide (Mbp1; IC₅₀ ~ 10.0 µM & K_d = 200 nM). Suggested to covalently modify Mad2-Cys¹⁴⁹ via a reversible Michael adduct formation. Significantly reduces the mitotic duration in paclitaxel (0.5 µM; Cat. No. 580555)-treated HeLa cells (25 µM of M2I-1) and impairs mitotic spindle assembly checkpoint (SAC) function.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
Mad2

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Use only fresh DMSO for reconstitution.

Kastl, J., et al. 2015. ACS Chem. Biol.10, 1661.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)