T56-LIMKi


Catalog No. size PriceQuantity
M6513-2 2mg solid $126
M6513-10 10mg solid $527

Description

Cas:924473-59-6

Product Information:

T-5601640 is a selective LIM kinase 2 (LIMK2) inhibitor.

 

Chemical Formula: C19H14F3N3O3

 

Exact Mass: 389.0987

 

Molecular Weight: 389.33

 

Elemental Analysis: C, 58.62; H, 3.62; F, 14.64; N, 10.79; O, 12.33

 

Synonym:

 

T-5601640

T 5601640

T5601640

T56LIMKi

T56 LIMKi

T56-LIMKi

 

Chemical Name: 

3-Methyl-N-[3-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]phenyl]-5-isoxazolecarboxamide

 

InChi Key: 

XVOKFRPKSAWELK-UHFFFAOYSA-N

 

InChi Code: 

InChI=1S/C19H14F3N3O3/c1-11-8-16(28-25-11)18(27)24-14-6-2-4-12(9-14)17(26)23-15-7-3-5-13(10-15)19(20,21)22/h2-10H,1H3,(H,23,26)(H,24,27)

 

Smiles Code:

O=C(C1=CC(C)=NO1)NC2=CC=CC(C(NC3=CC=CC(C(F)(F)F)=C3)=O)=C2

 

 

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

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:

T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition of tumor cell migration, tumor cell growth, and anchorage-independent colony formation in soft agar. T56-LIMKi (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1−/−MEFs with an IC50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50μM T56-LIMKi causes a statistically significant reduction in the number of cells exhibiting stress fibers.

 

In Vivo:

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control.

 

References

 

  1. Rak R, Haklai R, Elad-Tzfadia G, Wolfson HJ, Carmeli S, Kloog Y. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. eCollection 2014. PubMed PMID: 25593987; PubMed Central PMCID: PMC4295757.

 

  1. Rak R, Kloog Y. Targeting LIM kinase in cancer and neurofibromatosis. Cell Cycle. 2014;13(9):1360-1. doi: 10.4161/cc.28748. Epub 2014 Apr 3. PubMed PMID: 24698779; PubMed Central PMCID: PMC4050127.

 

  1. Mashiach-Farkash E, Rak R, Elad-Sfadia G, Haklai R, Carmeli S, Kloog Y, Wolfson HJ. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39. PubMed PMID: 22776759; PubMed Central PMCID: PMC3442289.

 

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

 

 

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