ML-SI3

ML-SI3 is a mixture of cis/trans ML-SI3 (HY-139426A), which is a TRPML1/2 channel inhibitor with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy. The cis/trans ML-SI3 (HY-139426A) components of ML-SI3 are TRPML2 activators with EC50s of 3.3 μM and 9.4 μM, respectively[1][2].

Product Specifications

CAS Number

[891016-02-7]

Product Name Alternative

ML-SI3 (cis/trans mix)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Parasite; TRP Channel

Type

Reference compound

Related Pathways

Anti-infection; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/ml-si3.html

Purity

99.93

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=CC=C1)(NC2C(N3CCN(C4=CC=CC=C4OC)CC3)CCCC2)=O

Molecular Formula

C23H31N3O3S

Molecular Weight

429.58

Precautions

H302, H315, H319, H335

References & Citations

[1]Rühl P, et al. Estradiol analogs attenuate autophagy, cell migration and invasion by direct and selective inhibition of TRPML1, independent of estrogen receptors. Sci Rep. 2021 Apr 15;11 (1) :8313. |[2]Kilpatrick BS, et al. Endo-lysosomal TRP mucolipin-1 channels trigger global ER Ca2+ release and Ca2+ influx. J Cell Sci. 2016 Oct 15;129 (20) :3859-3867. |[3]Bais S, et al. Schistosome TRPML channels play a role in neuromuscular activity and tegumental integrity. Biochimie. 2022 Mar;194:108-117. |[4]Zhang X, et al. Rapamycin directly activates lysosomal mucolipin TRP channels independent of mTOR. PLoS Biol. 2019 May 21;17 (5) :e3000252. |[5]Xing Y, et al. Blunting TRPML1 channels protects myocardial ischemia/reperfusion injury by restoring impaired cardiomyocyte autophagy. Basic Res Cardiol. 2022 Apr 7;117 (1) :20. |[6]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.