435930
LIM Kinase Inhibitor I, LIMKi 3
The LIM Kinase Inhibitor I, LIMKi 3 controls the biological activity of LIM Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonyme(s) :
LIM Kinase Inhibitor I, LIMKi 3, N-(5-(1-(2,6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide
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About This Item
Formule empirique (notation de Hill):
C17H14Cl2F2N4OS
Numéro CAS:
Poids moléculaire :
431.29
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
powder
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
beige
Solubilité
DMSO: 100 mg/mL
Conditions d'expédition
ambient
Température de stockage
2-8°C
Chaîne SMILES
ClC1=CC=CC(Cl)=C1N2N=C(C=C2C3=CN=C(NC(C(C)C)=O)S3)C(F)F
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)
Clé InChI
IVUGBSGLHRJSSP-UHFFFAOYSA-N
Description générale
A cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50 = 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 µM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 µM in A549 proliferation & colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µM) with concomitant blockage of invasion (by 93% at 10 µM).
A cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50 = 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 µM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 µM in A549 proliferation and colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µM) with concomitant blockage of invadopedia-mediated ECM degradation (13% and 10% of control, respectively, by 3 and 10 µM inhibitor) and invasion (45% and 7% of control invasion rate, respectively, by 3 and 10 µM inhibitor). Although reported to exhibit affinity toward AMPKα1 and AMPKα2 in T7 phage-based competition binding studies, inhibitory activity of LIMKi 3 against AMPKα1/2 is not yet directly demonstrated.
Actions biochimiques/physiologiques
Cell permeable: yes
Primary Target
LIMK1 and LIMK2
LIMK1 and LIMK2
Reversible: yes
Secondary Target
AMPKA1, AMPKA2, DDR1, PAK3, DCAMKL2
AMPKA1, AMPKA2, DDR1, PAK3, DCAMKL2
Target IC50: 7 and 8 nM against LIMK1 and LIMK2, respectively
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Autres remarques
Scott, R.W., et al. 2010. J. Cell. Biol.191, 169.
Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther.7, 3490.
Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther.7, 3490.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 2
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
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Mariana Morales-Quinones et al.
Hypertension (Dallas, Tex. : 1979), 76(2), 393-403 (2020-07-01)
Increased arterial stiffness and vascular remodeling precede and are consequences of hypertension. They also contribute to the development and progression of life-threatening cardiovascular diseases. Yet, there are currently no agents specifically aimed at preventing or treating arterial stiffening and remodeling.
Thomas J Jurrissen et al.
American journal of physiology. Heart and circulatory physiology, 323(5), H879-H891 (2022-09-10)
Adropin is a peptide largely secreted by the liver and known to regulate energy homeostasis; however, it also exerts cardiovascular effects. Herein, we tested the hypothesis that low circulating levels of adropin in obesity and type 2 diabetes (T2D) contribute
Catarina Domingues et al.
Frontiers in cell and developmental biology, 8, 678-678 (2020-09-10)
The mechanical properties of the extracellular environment are interrogated by cells and integrated through mechanotransduction. Many cellular processes depend on actomyosin-dependent contractility, which is influenced by the microenvironment's stiffness. Here, we explored the influence of substrate stiffness on the proteome
Xing Duan et al.
Journal of cellular physiology, 233(8), 6088-6097 (2018-01-11)
LIM kinases (LIMK1/2) are LIM domain-containing serine/threonine/tyrosine kinases that mediate multiple cellular processes in mitosis. In the present study, we explored the functional roles and potential signaling pathway of LIMK1/2 during mouse oocyte meiosis. Disruption of LIMK1/2 activity and expression
Tobias Heib et al.
Cell reports, 35(6), 109102-109102 (2021-05-13)
Megakaryocytes (MKs), the precursors of blood platelets, are large, polyploid cells residing mainly in the bone marrow. We have previously shown that balanced signaling of the Rho GTPases RhoA and Cdc42 is critical for correct MK localization at bone marrow
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