p-erk

Neticonazole Hydrochloride is an imidazole antifungal for the treatment of fungal skin infections. Neticonazole is reported as a potent exosome inhibitor which can block the activity of exosomes.

DNL343 is a selective and potent eIF2B activator that crosses the blood-brain barrier and inhibits the assembly of stress granules (SGs) induced by the C9ORF72 dipeptide repeats. DNL343 may be useful in the study of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS).

SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

ISRIB is a potent and selective PERK inhibitor.

GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice.

HC-5404 is a novel, potent and highly selective PERK (Protein kinase RNA-like Endoplasmic Reticulum Kinase) inhibitor, blocking the activation of the PERK pathway, which in turn inhibits the endoplasmic reticulum stress response signaling pathway, thereby exerting anti-tumor effects, and can be used to treat advanced solid tumors and renal cell Cancer.

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.

KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.

ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

FLT3 VEGFR2-IN-1 (Compound 26) is a potent inhibitor of FLT3, VEGFR2, and HDAC, exhibiting IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM against FLT3, VEGFR2, and HDAC1, respectively. It effectively inhibits the phosphorylation of STAT3 and ERK1 2, as well as the proliferation of leukemia cells. FLT3 VEGFR2-IN-1 demonstrates antitumor activity and is applicable in research on acute myeloid leukemia.

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.

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1 ERK2.

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1 2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0 G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values of 1-10 μM against NEA-G12D, PPI-G12D, and p ERK-AGS, and is utilized in cancer research [1].

KRAS inhibitor-14 is a potent inhibitor of KRAS G12C (IC50: 0.249 μM). KRAS inhibitor-14 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 1.12, >33.3 μM, respectively. KRAS inhibitor-14 has potential to be investigated in pancreatic, colorectal and lung cancers.

CYP1B1-IN-3 is a potent, selective inhibitor of CYP1B1, exhibiting IC50 values of 6.6 nM for CYP1B1, 347.3 nM for CYP1A1, and >10000 nM for CYP1A2. It also impedes cell migration and invasion, and inhibits the P-gp, AKT ERK, FAK SRC, and EMT pathways [1].

KRAS inhibitor-12 (compound 6-1) is a potent inhibitor of KRAS G12C (IC50: 0.537 μM), exhibiting p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50 values of 1.3 and 3.7 μM, respectively. KRAS inhibitor-12 has potential for study in pancreatic, colorectal, and lung cancers.

KRAS inhibitor-17 (compound 3-9) is a potent inhibitor of KRAS G12C with an IC50 of 3.37 μM. It exhibits p-ERK inhibition with an IC50 of 9.25 μM in MIA PaCA-2 cells and greater than 33.3 μM in A549 cells. KRAS inhibitor-17 has potential applications in the study of pancreatic, colorectal, and lung cancers.