SMS2-IN-1 |
رقم الكتالوجGC65364 |
SMS2-IN-1 هو مثبط قوي وانتقائي للغاية sphingomyelin synthase 2 (SMS2) مع IC 50 من 6.5 نانومتر و Kd من 37 نانومتر
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Cas No.: 2098890-15-2
Sample solution is provided at 25 µL, 10mM.
SMS2-IN-1 is a potent and highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM and a Kd of 37 nM. SMS2-IN-1 shows 150-fold selectivity for SMS2 over SMS1 (IC50 of 1000 nM)[1].
AS/MS binding experiments are conducted using these SMS2-mutant membrane fractions, SMS2-IN-1 (compound 2) binds to the S217A, H272A, and D276A mutants. S227 and H229 are pivotal amino acid residues for the binding of SMS2-IN-1 to SMS2[1].
[1]. Adachi R, et al. Discovery and characterization of selective human sphingomyelin synthase 2 inhibitors. Eur J Med Chem. 2017 Aug 18;136:283-293.
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