erk1/2

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 10 (Compound 36c) is a potent inhibitor of ERK1 and ERK2, with IC50 values of 0.11 nM and 0.08 nM, respectively. It effectively hinders the phosphorylation of downstream substrates p90RSK and c-Myc. Additionally, ERK1/2 inhibitor 10 induces apoptosis and incomplete autophagy-related cell death. This compound demonstrates significant antitumor efficacy in models of triple-negative breast cancer and colorectal cancer harboring BRAF and RAS mutations.

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.

p44/42 MAPK (Erk1/2) (137F5) Rabbit mAb #4695R is a useful organic compound for research related to life sciences and the catalog number is T64587.

Phospho-p44/42 MAPK (Erk1/2) (Thr202/Tyr204) (20G11) Rabbit mAb #4376R is a useful organic compound for research related to life sciences and the catalog number is T64608.

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 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].

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.

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).

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

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

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

PHPS1 is an inhibitor of Shp2. PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.

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.

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS/mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1/2.

BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with an IC50 of 188 nM and a Kd of 1.5 nM.