erk5

ERK5-IN-6 is a potent inhibitor of ERK5 kinase.ERK5-IN-6 exhibits antiproliferative activity, anticonvulsant activity, and antitumor activity, and can be used in the study of central nervous system-related disorders.

ERK5-IN-5 is a potent extracellular signal-regulated kinase 5 (ERK5) inhibitor with anticancer activity and potential anticonvulsant activity that inhibits A549 cell proliferation.

ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM).

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 values of 0.82 μM for ERK5 and 3 μM for ERK5 (MEF2D).

BAY885 is a new ERK5 inhibitor.

AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).

JWG-071, the first reported chemical probe for ERK5 kinase selectivity, is a BET-selective inhibitor with a 1 μM BRD4 IC that enhances both ERK5 activity and BRD4 selectivity.

XMD17-109 (ERK5-IN-1) is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).

(E/Z)-BIX 02189 is an isomer of BIX 02189 that can be employed in biochemical experiments.

BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.

PROTACERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. It induces the degradation of ERK5 in MOLT-4 cells via a VHL-mediated proteasome pathway. PROTACERK5 degrader-1 is useful for studying diseases or disorders characterized by abnormal ERK5 activity.

ERK5ligand-1 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). It is useful for designing PROTACs, such as PROTACERK5 degrader-1.

ERK5-IN-7 is an orally active ERK5 inhibitor with an IC50 of 403.4 nM. It directly suppresses ERK5 kinase activity, reduces phosphorylation levels, and decreases total protein expression of ERK5. Additionally, ERK5-IN-7 induces apoptosis [Apoptosis] by upregulating Bax, downregulating Bcl-2, and promoting Caspase-3 cleavage. It also leads to the accumulation of reactive oxygen species (ROS) and exhibits anticancer effects against Lewis lung carcinoma.

ERK5-IN-4 (compound 34b) is a potent and specific inhibitor of extracellular signal-related kinase 5 (ERK5) activity, effectively inhibiting both full-length ERK5 and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with IC50 values of 77 nM and 300 nM, respectively [1].

ERK5-IN-3 is a selective and potent inhibitor of ERK5 (extracellular signal-associated kinase 5) (IC50: 6 nM). ERK5-IN-3 exhibits anti-proliferative effects on Hela cells (IC50: 31 nM).

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).

PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM. While not directly inhibiting tumor cell growth, PPM-3 affects tumor progression through influencing macrophage differentiation [1].

L-797,591 hydrochloride is active for somatostatin receptor isoform 1 (SSTR1). L-797,591 hydrochloride is commonly used in combination with AG1478 to enhance p-ERK5 expression in SSTR1 cells. L-797,591 hydrochloride significantly enhanced p38 phosphorylation in cotransfected cells, and this effect was reversed in combination with AG1478.

XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50 values of 38.69, 40.12, and 59.72 nM, respectively. It also serves as an autophagy agonist, influencing mTOR/p70S6K and NCOA4-mediated ferroptosis, potentially mitigating multidrug resistance. SKLB-D18 demonstrates significantly superior efficacy against triple-negative breast cancer (TNBC) in both in vitro and in vivo studies.

JWG-045 is a selective ERK5 inhibitor that also exhibits unique ferroptosis activity independent of ERK5 inhibition. This compound can be utilized in breast cancer research.

AX15839 is an inhibitor of BRD4 and ERK5.

AX15892 is a potent and selective inhibitor of ERK5.