ML-SI3

Last updated
ML-SI3
ML-SI3 structure.png
Identifiers
  • N-[(1S,2S)-2-[4-(2-methoxyphenyl)piperazin-1-yl]cyclohexyl]benzenesulfonamide
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
Formula C23H31N3O3S
Molar mass 429.58 g·mol−1
3D model (JSmol)
  • COC1=CC=CC=C1N2CCN(CC2)[C@H]3CCCC[C@@H]3NS(=O)(=O)C4=CC=CC=C4
  • InChI=1S/C23H31N3O3S/c1-29-23-14-8-7-13-22(23)26-17-15-25(16-18-26)21-12-6-5-11-20(21)24-30(27,28)19-9-3-2-4-10-19/h2-4,7-10,13-14,20-21,24H,5-6,11-12,15-18H2,1H3/t20-,21-/m0/s1
  • Key:OVTXOMMQHRIKGL-SFTDATJTSA-N

ML-SI3 is a chemical compound which acts as an "antagonist" (i.e. channel blocker) of the TRPML family of calcium channels, with greatest activity at the TRPML1 channel, although it also blocks the related TRPML2 and TRPML3 channels with lower affinity. It is used for research into the role of TRPML1 and its various functions in lysosomes and elsewhere in the body. [1] [2] [3] [4] [5] [6] [7]

See also

References

  1. ↑ Kilpatrick BS, Yates E, Grimm C, Schapira AH, Patel S (October 2016). "Endo-lysosomal TRP mucolipin-1 channels trigger global ER Ca2+ release and Ca2+ influx". Journal of Cell Science. 129 (20): 3859–3867. doi: 10.1242/jcs.190322 . PMC   5087663 . PMID   27577094.
  2. ↑ Li X, Rydzewski N, Hider A, Zhang X, Yang J, Wang W, et al. (April 2016). "A molecular mechanism to regulate lysosome motility for lysosome positioning and tubulation". Nature Cell Biology. 18 (4): 404–17. doi:10.1038/ncb3324. hdl: 2027.42/120892 . PMC   4871318 . PMID   26950892.
  3. ↑ Sahoo N, Gu M, Zhang X, Raval N, Yang J, Bekier M, et al. (May 2017). "2+ Efflux Channel in the Tubulovesicle". Developmental Cell. 41 (3): 262–273.e6. doi: 10.1016/j.devcel.2017.04.003 . PMC   5497767 . PMID   28486130.
  4. ↑ Scotto Rosato A, Montefusco S, Soldati C, Di Paola S, Capuozzo A, Monfregola J, Polishchuk E, Amabile A, Grimm C, Lombardo A, De Matteis MA, Ballabio A, Medina DL (December 2019). "TRPML1 links lysosomal calcium to autophagosome biogenesis through the activation of the CaMKKβ/VPS34 pathway". Nature Communications. 10 (1): 5630. Bibcode:2019NatCo..10.5630S. doi:10.1038/s41467-019-13572-w. PMC   6904751 . PMID   31822666.
  5. ↑ Zhang X, Chen W, Gao Q, Yang J, Yan X, Zhao H, et al. (May 2019). "Rapamycin directly activates lysosomal mucolipin TRP channels independent of mTOR". PLOS Biology. 17 (5) e3000252. doi: 10.1371/journal.pbio.3000252 . PMC   6528971 . PMID   31112550.
  6. ↑ Li D, Shao R, Wang N, Zhou N, Du K, Shi J, et al. (March 2020). "Sulforaphane Activates a lysosome-dependent transcriptional program to mitigate oxidative stress". Autophagy. 17 (4): 872–887. doi:10.1080/15548627.2020.1739442. PMC   8078734 . PMID   32138578.
  7. ↑ Leser C, Keller M, Gerndt S, Urban N, Chen CC, Schaefer M, Grimm C, Bracher F (October 2020). "Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3". European Journal of Medicinal Chemistry. 210 112966. doi:10.1016/j.ejmech.2020.112966. PMID   33187805.
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