p-erk

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist.MSU-42011 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.MSU-42011 is an effective therapy for the treatment of preclinical krasdriven lung cancer and has immunomodulatory activity.

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].

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.

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

Febuxostat (TEI 6720) is a xanthine oxidase Inhibitor.

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values ranging from 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.

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.

PABA/NO is a novel glutathione-S-transferase-p-activated nitric oxide donor, inhibiting proliferation and inducing apoptosis by targeting PI3K/AKT/mTOR and MEK/ERK pathways in hepatocellular carcinoma cells.

Dosimertinib-d3 is a potent, orally active inhibitor of EGFR, known to reduce the expression of p-EGFR and p-ERK proteins, thereby exhibiting antiproliferative and anti-tumor effects. It holds promise for research into non-small-cell lung cancer (NSCLC).

KRAS inhibitor-18 (compound 3-10) is a potent inhibitor of KRAS G12C (IC50: 4.74 μM). KRAS inhibitor-18 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 66.4, 11.1 μM respectively. KRAS inhibitor-18 has potential for pancreatic, colorectal and lung cancer studies.

KRAS inhibitor-16 (compound 3-11) is a potent inhibitor of KRAS G12C (IC50: 0.457 μM). KRAS inhibitor-16 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 3.06, 11.1 μM respectively. KRAS inhibitor-16 has potential to be studied in pancreatic, colorectal and lung cancers.

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT) is 6 nM[1].ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].ASK120067 (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[1]. ASK120067 (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[1]. [1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90.

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

KRAS inhibitor-17 (compound 3-9) is a potent inhibitor of KRAS G12C (IC50: 3.37 μM). KRAS inhibitor-17 exhibits p-ERK inhibition with IC50 = 9.25 μM in MIA PaCA-2 cells and >33.3 μM in A549 cells. KRAS inhibitor-17 has the potential to be studied 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].

Asatone, an active component isolated from Radix et Rhizoma Asari, has an anti-inflammatory effect via activation of NF-κB and downregulation of p-MAPK (ERK, JNK, and p38) pathways.

SHP389 is an allosteric SHP2 inhibitor, with an IC 50 of 36 nM for both SHP2 and p-ERK.

KRAS inhibitor-15 (compound 3-19) is a potent inhibitor of KRAS G12C (IC50: 0.954 μM). KRAS inhibitor-15 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 2.03, >33.3 μM, respectively. KRAS inhibitor-15 has potential to be studied in pancreatic, colorectal and lung cancers.

KRAS inhibitor-13 (compound 5-6) is a potent inhibitor of KRAS G12C (IC50: 0.883 μM). KRAS inhibitor-13 has a p-ERK inhibitory effect in MIA PaCA-2, A549 cells with IC50 values of 5.9 and >100 μM respectively. KRAS inhibitor-13 has potential to be studied in pancreatic, colorectal and lung cancers.

KRAS G12C inhibitor 47 is a potent inhibitor of KRAS G12C (IC50: 0.172 μM). KRAS G12C inhibitor 47 exhibits p-ERK inhibition in MIA PaCA-2 cells, A549 cells with IC50 values of 0.046 μM and 69.8 μM respectively. KRAS G12C inhibitor 47 showed investigational potential against pancreatic, colorectal and lung cancers.