(1S,2S)-ML-SI3

Names

[ Name ]:
(1S,2S)-ML-SI3

Biological Activity

[Description]:

(1S,2S)-ML-SI3 is the trans-isomer of ML-SI3, a TRPML inhibitor. The (-)-isomer is a potent inhibitor of TRPML1 and TRPML2 (IC50=1.6 μM/2.3 μM) and a weak inhibitor of TRPML3 (IC50=12.5 μM), whereas the (+)-enantiomer is an inhibitor on TRPML1 (IC50=5.9 μM), but an activator on TRPML 2 and 3[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Cancer

[Target]

IC50: 1.6 μM (TRPML1), 2.3 μM (TRPML2), 12.5 (TRPML3) for the (-)-isome of (1S,2S)-ML-SI3; 5.9 μM (TRPML1) for the (+)-enantiomer[1]

[References]

[1]. Leser C, et al. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3. Eur J Med Chem. 2021 Jan 15;210:112966.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₃₁N₃O₃S

[ Molecular Weight ]:
429.58

Related Compounds

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