ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.
LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50s of 38.69, 40.12 and 59.72 nM, respectively. SKLB-D18 is also an autophagy agonist, plays a role in mTOR/p70S6K and NCOA4-mediated ferroptosis, which may mitigate multidrug resistance. SKLB-D18 exhibits significantly superior efficacy in vitro and in vivo against triple-negative breast cancer (TNBC).
ASN007(ERAS 007, ERK-IN-3) is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with 2 nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer.
SF-3-030 is a novel ATP-dependent/catalytic site inhibitor of ERK1/2, inhibits A375 cell viability with IC50 of 4.9 uM.SF-3-030 showed selective inhibition of cancer cell lines with activating mutations in the ERK1/2 pathway.SF-3-030 inhibited viability of four melanoma cell lines containing either BRAF or NRas mutations with IC50 of 5-10 uM.SF-3-030 selectively regulates ERK-dependent immediate early gene expression, causes differential changes in AP-1 protein levels characterized by inhibition of Fra-1, FosB, and the alternative splice variant FosB2 but no effect on c-Fos levels, and induces ROS mediates inhibition of A375 cell proliferation.
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
Get Quote
X
We have received your inquiry regarding and will respond to you as soon as possible.