BMS-5 is a Potent LIM kinase inhibitor (IC50 values are 7 and 8 nM for LIMK1 and LIMK2 respectively). Inhibits cofilin phosphorylation in MDA-MB-231 breast cancer cells. Reduces MDA-MB-231 tumor cell invasion in a 3D matrigel invasion assay.
Chemical Formula: C17H14Cl2F2N4OS
Exact Mass: 430.0233
Molecular Weight: 431.2828
Elemental Analysis: C, 47.34; H, 3.27; Cl, 16.44; F, 8.81; N, 12.99; O, 3.71; S, 7.43
InChi Code: InChI=1S/C17H14Cl2F2N4OS/c1-8(2)16(26)23-17-22-7-13(27-17)12-6-11(15(20)21)24-25(12)14-9(18)4-3-5-10(14)19/h3-8,15H,1-2H3,(H,22,23,26)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life:>2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
BMS-5 (LIMKi 3) inhibits cofilin-Ser3 phosphorylation in a dose-dependent manner in Nf2ΔEx2 mouse Schwann cells (MSCs) with an IC50 of ~2 µM. BMS-5 (LIMKi 3) reduces Nf2ΔEx2 MSC viability in a dose-dependent manner with an IC50 of 3.9 µM, but does not significantly reduce the viability of control Nf2flox2/flox2 MSCs at equivalent BMS-5 concentrations. At 10 µM BMS-5, Nf2ΔEx2 MSC viability is 40% compared to 83% for controls.
BMS-5 (LIMKi 3) (20 or 200 μM/side) is bilaterally infused into the hippocampus of rats immediately after contextual fear conditioning training. Rats are tested for memory consolidation 48 h after fear conditioning. Post hoc analysis shows that the group treated with 200 μM BMS-5 express lower freezing levels compared to the 20 μM and vehicle groups (P<0.01).
Wang W, Townes-Anderson E. LIM Kinase, a Newly Identified Regulator of Presynaptic Remodeling by Rod Photoreceptors After Injury. Invest Ophthalmol Vis Sci. 2015 Dec;56(13):7847-58. doi: 10.1167/iovs.15-17278. PubMed PMID: 26658506; PubMed Central PMCID: PMC4682489.
Bao Z, Han X, Chen F, Jia X, Zhao J, Zhang C, Yong C, Tian S, Zhou X, Han L. Evidence for the involvement of cofilin in Aspergillus fumigatus internalization into type II alveolar epithelial cells. BMC Microbiol. 2015 Aug 13;15:161. doi: 10.1186/s12866-015-0500-y. PubMed PMID: 26268695; PubMed Central PMCID: PMC4542120.
Park JB, Agnihotri S, Golbourn B, Bertrand KC, Luck A, Sabha N, Smith CA, Byron S, Zadeh G, Croul S, Berens M, Rutka JT. Transcriptional profiling of GBM invasion genes identifies effective inhibitors of the LIM kinase-Cofilin pathway. Oncotarget. 2014 Oct 15;5(19):9382-95. PubMed PMID: 25237832; PubMed Central PMCID: PMC4253441.
Petrilli A, Copik A, Posadas M, Chang LS, Welling DB, Giovannini M,Fernandez-Valle C. LIM domain kinases as potential therapeutic targets for neurofibromatosis type 2. Oncogene. 2014 Jul 3;33(27):3571-82. doi: 1038/onc.2013.320. Epub 2013 Aug 12. PubMed PMID: 23934191; PubMed Central PMCID: PMC4016185.
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