ERK

A metabolite of ellagic acid

JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology.

Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects.

2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.

A dual inhibitor of CK2 and ERK8

Cafestol, one of the major components of coffee, is a coffee-specific diterpene form and an inhibitor of ERK2.

Inflachromene is an inhibitor of HMGB1 and HMGB expression. Inflachromene can inhibit the release of HMGB1 and the NF-κB signaling pathway, exerting anti-inflammatory and neuroprotective effects. Inflachromene is mainly used to treat epilepsy.

Nε-(1-Carboxymethyl)-L-lysine is a unique post-translational modification (PTM) of proteins that is generated by the non-enzymatic glycation of lysine residues.

Theaflavin 3,3'-digallate (TF-3; ZP10) is a potent inhibitor of Zika virus (ZIKV) protease with an IC 50 value of 2.3μM.

Enniatins are cyclohexadepsipeptides commonly isolated from fungi that are known to have antibiotic properties and to induce apoptosis in several cancer lines.

Enniatins are cyclohexadepsipeptides commonly isolated from fungi and are known to have antibiotic properties.

A resorcylic acid lactone polyketide

L-Sulforaphene is a natural isothiocyanate with anti-inflammatory, anticancer, and antioxidant effects.

DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.

Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK.

ERK-IN-3 is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.

Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.

(E)-Osmundacetone is the isomer of Osmundacetone.

Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects.

EF24 is a novel synthetic curcumin analog.

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.

ACA-28 (compound 2a) is an effective ERK MAPK signaling regulator. ACA-28 induces apoptosis through excessive activation of ERK and selectively inhibits cancer cell growth. ACA-28 inhibits the growth of melanoma cells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively.