SKLB-D18 | ERK1/2/5 inhibitor

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5 mg$90.00
25 mg$325.00
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SKLB-D18 is a first-in-class potent dual ERK1/2 and ERK 5 inhibitor (IC50’s: ERK1 = 39 nM, ERK2 = 40 NM, ERK5 = 60 nM) and is highly selective against a panel of 380 kinases.  It exhibited good activity against MDA-MB-231 (IC50 = 0.93 µM) and MDA-MB-468 (IC50 = 1.05 µM) cells.  SKLB-D18 inhibited activation of ERK1/2/5 downstream components p-ERK5, p-RSK90, p-c-Myc, and c-MYC.  It was also able to induce autophagy-dependent cell death and ferroptosis in triple negative breast cancer cells. Active in mouse triple negative breast cancer xenografts.

References/Citations:

  1. Xiao et al. (2025) A first-in-class selective inhibitor of ERK1/2 and ERK5 overcomes drug resistance with a single-molecule strategy; Sig. Transduct. Target. Ther., 10 70
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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

SKLB-D18 is a first-in-class potent dual ERK1/2 and ERK 5 inhibitor (IC50’s: ERK1 = 39 nM, ERK2 = 40 NM, ERK5 = 60 nM) and is highly selective against a panel of 380 kinases.  It exhibited good activity against MDA-MB-231 (IC50 = 0.93 µM) and MDA-MB-468 (IC50 = 1.05 µM) cells.  SKLB-D18 inhibited activation of ERK1/2/5 downstream components p-ERK5, p-RSK90, p-c-Myc, and c-MYC.  It was also able to induce autophagy-dependent cell death and ferroptosis in triple negative breast cancer cells. Active in mouse triple negative breast cancer xenografts.

References/Citations:

  1. Xiao et al. (2025) A first-in-class selective inhibitor of ERK1/2 and ERK5 overcomes drug resistance with a single-molecule strategy; Sig. Transduct. Target. Ther., 10 70