erk1/2 inhibitor 2

ERK1 2 inhibitor 2 (ASTX029) is a selective and orally bioavailable extracellular signal-regulated kinases 1 and 2 (ERK 1 2) inhibitor, with potential antineoplastic activity.

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

ERK1 2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1 2 that promotes the accumulation of DSBs and the degradation of ERK1 2 expression. This compound decreases BCL-2 levels and induces DNA damage by inhibiting PARP and ERK1 2. Additionally, ERK1 2 inhibitor 11 activates caspase 3 to induce apoptosis.

ERK1 2 inhibitor 12 (compound 76.3) is an ERK1 2 inhibitor that suppresses ERK-mediated phosphorylation of caspase-9 and p90Rsk-1 kinases. It exhibits anticancer properties and is applicable in cancer research.

ERK1 2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.

ERK1 2 inhibitor 7 is a potent inhibitor of ERK, with an IC50 of 0.94 nM for ERK2.

ERK1 2 inhibitor 8 is a potent ERK inhibitor, targeting ERK2 with an IC50 of 0.48 nM.

ERK1 2 inhibitor 6 is a potent inhibitor of ERK1 2, showing potential for studying or preventing cancer, inflammation, and other proliferative diseases.

ERK1 2 inhibitor 5 is a potent inhibitor of ERK1 2, with potential applications in investigating or preventing cancer, inflammation, and other proliferative diseases.

ERK1 2 Inhibitor 3, a potent inhibitor of ERK1 2, plays a crucial role in the signal transduction pathway by targeting the Mitogen-activated protein kinase (MAPK) family, specifically the extracellular signal-regulated kinase (ERK). Given its significant impact, this compound holds promise for research or prevention efforts related to cancer, inflammation, or other proliferative diseases[1].

ERK1 2 Inhibitor 5, a potent suppressant of the ERK1 2 pathway, is instrumental in the mitogen-activated protein kinase (MAPK) signal transduction pathway, where extracellular signal-regulated kinase (ERK) serves as a critical component of the MAPK family. This compound holds promise for the investigation or mitigation of cancer, inflammation, or various proliferative diseases[1].

ERK1 2 Inhibitor 9 (Probe 1), a covalent antagonist of ERK1 2, exhibits sub-micromolar efficacy in cellular assays (A375 GI50=0.47 μM) and facilitates the reduction of phospho-ERK1 2 levels. When conjugated with trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine-tagged Thalidomide), it forms the corresponding ERK-CLIPTAC, promoting targeted ERK1 2 degradation [1].

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

MK-8353 (SCH900353) is a potent, selective, and orally available inhibitor of ERK1/2 with IC50 values of 23.0 nM and 8.8 nM, respectively.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1 2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1 2 activating mutations in the MAPK pathway.

WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3 5, and ERK1 2, not JAK1 and JAK3. WP1066 has been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.

Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.

Theaflavin 3,3'-digallate, a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

Ravoxertinib (GDC-0994) is an efficacious, orally available ERK1 2 inhibitor with an IC50 of 1.1 0.3 nM.

SAX-187 (SAX-187) has high-affinity binding at the human 5-HT6 receptor.

AC-73 is an orally available Cluster of Differentiation 147 (CD147) inhibitor with high bioavailability that selectively disrupts the dimerization of CD147 (the binding site is in the N-terminal IgC2 domain of CD147 including Glu64 and Glu73), resulting in inhibition of the CD147 ERK1 2 STAT3 MMP-2 pathway and inhibition of liver cancer cell motility and invasion. AC-73 has antiproliferative activity and induces autophagy in leukemia cells.