ERK5 Inhibitor

BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC₅₀ of 59 nM.

XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with K_ds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with K_ds of 190, 600 and 890 nM, respectively. Anti-cancer activity.

AX-15836 is a potent and selective ERK5 inhibitor with an IC₅₀ of 8 nM.

JWG-071 is the kinase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC₅₀ values of 88nM and 109 nM, respectively.

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC₅₀ of 162 nM.

JWG-045 is a selective ERK5 inhibitor. JWG-045 exhibits unique ferroptosis-resistant activity independent of ERK5 inhibition. JWG-045 can be used in breast cancer research.

BAY-693 is a highly potent and highly selective ERK5 inhibitor with an IC₅₀ of 6.40 μM. BAY-693 reduces the transcriptional activity of MEF2. BAY-693 is applicable for cancer research.

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC₅₀s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.

ERK5-IN-1 is a potent ERK5 inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.

BAY885, a chemical probe, is a highly potent and selective ERK5 inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases.

BIX02188 is a potent MEK5-selective inhibitor with an IC₅₀ of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC₅₀ of 810 nM.

SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC₅₀ of 38.69 nM and a K_d of 126.9 nM against human ERK1, an IC₅₀ of 40.12 nM and a K_d of 209.8 nM against ERK2, and an IC₅₀ of 59.72 nM and a K_d of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer.

ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC₅₀ value of 6.23 µg/mL for A549 cells.

ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC₅₀ of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC₅₀ of 31 nM.

MHJ-627 is a potent ERK5 (MAPK7) inhibitor (IC₅₀: 0.91 μM). MHJ-627 promotes the mRNA expression of tumor suppressors and anti-metastatic genes, and promotes cancer cell death.

ERK5-IN-7 is an orally active ERK5 inhibitor with an IC₅₀ of 403.4 nM. ERK5-IN-7 directly inhibits ERK5 kinase activity, and downregulates the phosphorylation level and total protein expression of ERK5. ERK5-IN-7 induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer.

ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC₅₀ of 77 nM and 300 nM, respectively.