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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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L288407-5mg | 5mg | In stock | $93.90 | |
L288407-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $151.90 | |
L288407-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $291.90 | |
L288407-50mg | 50mg | In stock | $489.90 | |
L288407-100mg | 100mg | In stock | $815.90 |
Potent LIM kinase inhibitor; antitumor
Synonyms | BMS-5|1338247-35-0|LIMKi 3|N-(5-(1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)thiazol-2-yl)isobutyramide|BMS 5|LIMKI-3 (BMS-5)|N-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]-2-methylpropanamide|BMS5|CHEMBL21418 |
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Specifications & Purity | Moligand™, ≥98%(HPLC) |
Biochemical and Physiological Mechanisms | Potent LIM kinase inhibitor (IC50values 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. |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of LIM domain kinase 1;Inhibitor of LIM domain kinase 2 |
Product Description | General description: 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. |
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IUPAC Name | N-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]-2-methylpropanamide |
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INCHI | 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 Key | IVUGBSGLHRJSSP-UHFFFAOYSA-N |
Canonical SMILES | CC(C)C(=O)NC1=NC=C(S1)C2=CC(=NN2C3=C(C=CC=C3Cl)Cl)C(F)F |
Isomeric SMILES | CC(C)C(=O)NC1=NC=C(S1)C2=CC(=NN2C3=C(C=CC=C3Cl)Cl)C(F)F |
Alternate CAS | 1338247-35-0 |
PubChem CID | 56965901 |
MeSH Entry Terms | LIMKi3;N-(5-(1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl)-2-thiazolyl)-2-methylpropanamide |
Molecular Weight | 431.29 |
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Lot Number | Certificate Type | Date | Item |
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J2119120 | Certificate of Analysis | Aug 14, 2024 | L288407 |
J2119117 | Certificate of Analysis | Aug 09, 2024 | L288407 |
J2119176 | Certificate of Analysis | Aug 09, 2024 | L288407 |
J2119312 | Certificate of Analysis | Aug 09, 2024 | L288407 |
J2119313 | Certificate of Analysis | Aug 09, 2024 | L288407 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 43.13, Max Conc. mM: 100 |
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