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.

• 同義詞: LIM Kinase Inhibitor I, LIMKi 3, N-(5-(1-(2,6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide
• 經驗公式（希爾表示法）: C₁₇H₁₄Cl₂F₂N₄OS
• CAS號碼: 1338247-35-0
• 分子量：: 431.29
• MDL號碼: MFCD17019327
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: beige
• 溶解度: DMSO: 100 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• SMILES 字串: 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)
• InChI 密鑰: IVUGBSGLHRJSSP-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
LIMK1 and LIMK2

Reversible: yes

Secondary Target
AMPKA1, AMPKA2, DDR1, PAK3, DCAMKL2

Target IC₅₀: 7 and 8 nM against LIMK1 and LIMK2, respectively

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Scott, R.W., et al. 2010. J. Cell. Biol.191, 169.

Ross-Macdonald, P., et al. 2008. Mol. Cancer Ther.7, 3490.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 2
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable