A group 2 PAK inhibitor (IC50s = 7.5

GNE-2861 – 5 mg

Brand:
Cayman
CAS:
1394121-05-1
Storage:
-20
UN-No:
Non-Hazardous - /

GNE-2861 is an inhibitor of the group 2 p21-activated kinases (PAKs; IC50s = 7.5, 126, and 36 nM for PAK4, -5, and -6, respectively).{45666} It is selective for group 2 PAKs over group 1 PAKs (IC50s = 5.42, 0.97, and >10 μM for PAK1, -2, and -3, respectively), as well as JAK3, KHS1, MAP4K4, and MINK1 at 1 μM. GNE-2861 (0.1-50 μM) inhibits cell migration and reduces cell viability of MDA-MB-436 and MCF-10A PIK3CA cells in a concentration-dependent manner. It sensitizes drug-resistant MCF-7/LCC2 breast cancer cells to tamoxifen (Item No. 13258).{45667}  

 

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SKU: 29458 - 5 mg Category:

Description

A group 2 PAK inhibitor (IC50s = 7.5, 126, and 36 nM for PAK4, -5, and -6, respectively); selective for group 2 PAKs over group 1 PAKs (IC50s = 5.42, 0.97, and >10 μM for PAK1, -2, and -3, respectively), as well as JAK3, KHS1, MAP4K4, and MINK1 at 1 μM; inhibits cell migration and reduces cell viability of MDA-MB-436 and MCF-10A PIK3CA cells from 0.1-50 μM; sensitizes drug-resistant MCF-7/LCC2 breast cancer cells to tamoxifen

Formal name: 1-[2-[1-(2-amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]-cyclohexanol

Synonyms: 

Molecular weight: 406.5

CAS: 1394121-05-1

Purity: ≥98%

Formulation: A solid

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