| Bioactivity | ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy[1][5]. | ||||||||||||
| Invitro | ML-SI3 (10 μM) inhibits ML-SA1-evoked Ca2+ signals in HeLa cells[2].ML-SI3 (25-75 μM, 24h) disrupts tegumental integrity of adult schistosomes[3].ML-SI3 (10 μM) blocks Rapamycin (HY-10219)-evoked ITRPML1 in mimic of lysosomal lumen[4].ML-SI3 (3 µM, 6 h) abolishes the increase in both LC3II and p62 levels induced by hypoxia/reoxygenation (H/R) (4 h H/2 h R) in neonatal rat ventricular myocytes (NRVM)[5]. | ||||||||||||
| In Vivo | ML-SI3 (1.5 mg/kg, i.p., four times) attenuates I/R injury in mouse cardiomyocytes[5]. Animal Model: | ||||||||||||
| Name | ML-SI3 | ||||||||||||
| CAS | 891016-02-7 | ||||||||||||
| Formula | C23H31N3O3S | ||||||||||||
| Molar Mass | 429.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |