BMS-5


Catalog No. size PriceQuantity
M6692-2 2mg solid $103
M6692-10 10mg solid $391

Description

Cas:1338247-35-0

Product Information

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

 

Synonym: 

 

LIMKI-3

LIMKI 3

LIMKI3

BMS-5

BMS 5

BMS5

 

Chemical Name:

N-[5-[1-(2,6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl]-2-thiazolyl]-2-methylpropanamide

 

InChi Key:

IVUGBSGLHRJSSP-UHFFFAOYSA-N

 

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)

 

Smiles Code:

CC(C)C(NC1=NC=C(C2=CC(C(F)F)=NN2C3=C(Cl)C=CC=C3Cl)S1)=O

 

 

Technical Data:

 

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

 

In Vitro

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.

 

In Vivo

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).

 

 

References

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

Products are for research use only. Not for human use.

 

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