(S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1 C311A or SARM1 C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy [1].
References:
[1]. Feldman HC, et al. Selective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain. Proc Natl Acad Sci U S A. 2022;119(35):e2208457119.
References:
[1]. Feldman HC, et al. Selective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain. Proc Natl Acad Sci U S A. 2022;119(35):e2208457119.