SML3678
ML-SI3
≥98% (HPLC), TRPML1/2 channel inhibitor, powder
别名:
N-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]cyclohexyl]benzenesulfonamide
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关于此项目
经验公式（希尔记法）:
C23H31N3O3S
化学文摘社编号:
分子量:
429.58
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
ML-SI3, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Four-diastereomer racemate with a cation channel TRPML1-blocking and TRPML2-activating activity, while exhibiting much weaker TRPML3 potency
ML-SI3 is a 4-diastereomer racemate (2 cis and 2 trans isomers) with a cation channel TRPML1-blocking (IC50 = 3.1 μM/trans, 18.5 μM/cis against 5 μM ML-SA1-induced cellular calcium response) and TRPML2-activating activity (EC50 = 3.3 μM/trans, 9.4 μM/cis), while exhibiting much weaker TRPML3 potency (EC50 = 28.5 μM/trans, IC50 = 29.0 μM/cis). ML-SI3 is shown to compete against ML-SA1 for binding the same TRPML1 hydrophobic cavity. Comparing with ML-SI1 (GW405833), ML-SI3 is more potent and not agonist-dependent, effectively antagonizing against TRPML1 activation by both MK6-83 and ML-SA1.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Mohammad Samie et al.
Developmental cell, 26(5), 511-524 (2013-09-03)
Phagocytosis of large extracellular particles such as apoptotic bodies requires delivery of the intracellular endosomal and lysosomal membranes to form plasmalemmal pseudopods. Here, we identified mucolipin TRP channel 1 (TRPML1) as the key lysosomal Ca2+ channel regulating focal exocytosis and
Charlotte Leser et al.
European journal of medicinal chemistry, 210, 112966-112966 (2020-11-15)
The members of the TRPML subfamily of non-selective cation channels (TRPML1-3) are involved in the regulation of important lysosomal and endosomal functions, and mutations in TRPML1 are associated with the neurodegenerative lysosomal storage disorder mucolipidosis type IV. For in-depth investigation
Philip Schmiege et al.
Structure (London, England : 1993), 29(11), 1295-1302 (2021-06-26)
Transient receptor potential mucolipin 1 (TRPML1) regulates lysosomal calcium signaling, lipid trafficking, and autophagy-related processes. This channel is regulated by phosphoinositides and the low pH environment of the lysosome, maintaining calcium levels essential for proper lysosomal function. Recently, several small
Wuyang Wang et al.
Proceedings of the National Academy of Sciences of the United States of America, 112(11), E1373-E1381 (2015-03-04)
Upon nutrient starvation, autophagy digests unwanted cellular components to generate catabolites that are required for housekeeping biosynthesis processes. A complete execution of autophagy demands an enhancement in lysosome function and biogenesis to match the increase in autophagosome formation. Here, we
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