BIX02189

BIX02189

Biochem/physiol Actions

BIX02189 is an ATP site-targeting, potent and selective MEK5 inhibitor (IC50 =1.5 nM, [ATP] = 750 nM) with much reduced or no potency against 79 other kinases (CSF1R (FMS)/ERK5/Lck/Jak3/TGFβR1/RPS6KA6 (RSK4) IC50 = 46/59/250/440/580/990 nM, MEK1/MEK2/ERK2/JNK2/EGFR/STK16 IC50 >6.2 μM). BIX02189 blocks cellular ERK5, but not ERK1/2 or p38, phosphorylation induction (IC50 ﹤1 μM in sorbitol-stimulated HeLa), as well as downstream MEF2C transcriptional activation (IC50 = 0.53/0.26 μM, MEK5/ERK5/MEF2C HeLa/HEK293 reporter cells). BIX02189 in vivo efficacies are demonstrated in murine models of atherosclerosis, cancer, and diabetes (10-20 mg/kg i.p.).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576194 BIX02189 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£449.89 (exc VAT) per 25MG
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3576195 BIX02189 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear
£143.46 (exc VAT) per 5MG
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