MAPK

H-Ile-Lys-Val-Ala-Val-OH is a potent activator of the MAPK/ERK1/2 and PI3K/Akt signaling pathways. This compound enhances cell adhesion, promotes neurite outgrowth, and supports tumor growth. It is particularly effective in stimulating the proliferation of bone marrow-derived mesenchymal stem cells (BMMSCs), making it valuable for research applications in cell biology and regenerative medicine.

AS1940477 is an orally active inhibitor of the p38 MAPK pathway, targeting both the p38α and p38β isoforms. It effectively reduces the production of pro-inflammatory cytokines, such as TNFα, IL-1β, and IL-6, in human synovial interstitial cells and relevant animal models of inflammation. This compound is a valuable tool for research aimed at understanding and treating inflammatory diseases.

PF-06745013 is a selective inhibitor of MAP4K4, exhibiting an IC50 of 0.4 nM. This compound is distinguished by its lack of time-dependent inhibition risk for CYP3A4 and demonstrates non-ATP competitive activity. PF-06745013 has potential applications in the study of inflammatory diseases, including diabetes and cancer, making it a valuable tool in related research.

rel-Talmapimod hydrochloride is a selective inhibitor of p38α MAPK, exhibiting an IC50 of 9 nM. By targeting the p38α MAPK pathway, rel-Talmapimod hydrochloride effectively inhibits the secretion of pro-inflammatory factors, including TNFα, IL-1β, IL-6, and VEGF, while also blocking angiogenesis and osteoclast activation. This compound has demonstrated the ability to inhibit the proliferation of multiple myeloma cells and induce apoptosis. It is suitable for research applications involving various hematological malignancies, such as multiple myeloma and myelodysplastic syndrome.

R-03201195 is a highly selective inhibitor of p38 MAP kinase, demonstrating an IC50 of 0.7 nM for p38α. It effectively inhibits TNF-α production in THP-1 cells and IL-1β in human whole blood, with IC50 values of 0.25 nM and 0.57 nM, respectively. This reagent is valuable for research applications in inflammatory diseases, particularly rheumatoid arthritis.

PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma.

BMS-751324 is a selective inhibitor of p38α MAPK, a key regulator in the inflammatory response pathway. This compound demonstrates significant anti-inflammatory effects, as evidenced by its ability to reduce foot swelling and inhibit LPS-induced TNFα production in an arthritic rat model. BMS-751324 is suitable for research applications focused on inflammation, arthritis, and related pathways.

P38α-IN-10 is a selective inhibitor of p38α with an IC₅₀ of 230 nM. It effectively suppresses TNF production induced by lipopolysaccharide (LPS), making it a valuable tool for research into inflammatory responses. This compound is particularly relevant for studying conditions such as rheumatoid arthritis and septic shock, contributing to a deeper understanding of their underlying mechanisms.

Talmapimod hydrochloride is a selective inhibitor of p38α MAPK, exhibiting an IC50 of 9 nM. This compound effectively suppresses the secretion of pro-inflammatory cytokines, including TNFα, IL-1β, IL-6, and VEGF, while also inhibiting angiogenesis and osteoclast activation. Talmapimod hydrochloride demonstrates efficacy in inhibiting the growth of multiple myeloma cells and promoting apoptosis, making it a valuable tool for investigating various hematological malignancies, such as multiple myeloma and myelodysplastic syndromes.

L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is an ERK/BACE1/PSEN1 inhibitor known for its anti-allergic and neuroprotective properties. This compound effectively inhibits mast cell activation and subsequent release of inflammatory mediators by targeting the ERK pathway. Additionally, L-Citronellol decreases the activity of BACE1, PSEN1, and acetylcholinesterase (AChE), while reducing TNF-α expression and lipid peroxidation, indicating its potential utility in multi-target approaches for Alzheimer's disease research.

SR-318 is a selective inhibitor of p38 MAPK, exhibiting potent activity with IC50 values of 5 nM, 32 nM, and 6.11 µM for p38α, p38β, and p38α/β, respectively. This compound effectively reduces TNF-α release in whole blood, showing an IC50 of 283 nM. SR-318 is utilized in research focusing on anti-cancer and anti-inflammatory pathways, making it valuable for investigating therapeutic strategies in related diseases.

TAT-MKK3b is a peptide inhibitor targeted at p38 mitogen-activated protein kinase (MAPK). It effectively inhibits p38 phosphorylation, contributing to its role in modulating cellular stress responses. TAT-MKK3b exhibits renal targeting, reactive oxygen species (ROS) scavenging, and the ability to mitigate ferroptosis. This compound has demonstrated potential in the improvement of acute kidney injury and may help prevent its progression to chronic kidney disease.

RO5068760 is a potent non-ATP-competitive inhibitor of MEK1/2, demonstrating an IC50 of 0.025 μM for MEK1. This compound effectively inhibits MAPK pathway activity, leading to G1 cell cycle arrest and apoptosis, thereby reducing cancer cell proliferation. RO5068760 is applicable in research on various tumors characterized by dysregulation of the MAPK pathway, including melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer.

Ophiopogonin B primarily activates the JNK/c-Jun signaling pathway. This saponin compound, derived from Radix Ophiopogonjaponicus, demonstrates significant biological activity by inducing autophagy and apoptosis in colon cancer cells. It serves as a valuable reagent for researchers investigating mechanisms of cancer cell death and the therapeutic potential of autophagy modulation.

(+)-Columbianetin targets JNK and ERK signaling pathways while acting as a TGFβ signaling activator. This compound effectively inhibits UVA-induced phosphorylation of JNK and ERK, decreases MMP-1 production, and reverses collagen degradation. In addition, it mitigates UVA-mediated suppression of Smad2/3 phosphorylation and translocation, providing protective effects against UV-induced cellular damage. (+)-Columbianetin is an essential tool for research focused on skin aging and oxidative stress responses in keratinocytes.

Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation.

EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development.

SOS1/EGFR-IN-1 is a dual-target inhibitor that specifically targets SOS1 and EGFR, demonstrating IC50 values of 42.13±1.55 nM and 1.01±0.04 nM, respectively. This compound effectively induces apoptosis and G1 phase cell cycle arrest, while reducing angiogenesis and cell migration. SOS1/EGFR-IN-1 exhibits significant antitumor activity in prostate cancer cells, with an IC50 of 0.45±0.03 μM, making it a valuable tool for research in cancer therapies.

Astragaloside VI is an activator of the EGFR/ERK signaling pathway, primarily influencing cell proliferation and survival. It demonstrates significant biological activity in promoting wound healing processes through enhanced cellular responses. This compound serves as a valuable tool for research applications focused on tissue regeneration and repair mechanisms.

CCT241161 is a potent pan-RAF inhibitor that effectively targets multiple RAF family members with IC50 values of 3 nM for LCK, 6 nM for CRAF, 10 nM for SRC, 15 nM for V600E-BRAF, and 30 nM for BRAF. This compound demonstrates significant antiproliferative activity in BRAF and NRAS mutant melanoma cell lines, making it a valuable tool for cancer research. CCT241161 is relevant for studies focused on targeted therapies in oncogenic signaling pathways.

LL-Z1640-4 is a selective inhibitor of p38 and JNK signaling pathways, demonstrating significant efficacy in attenuating their activation in hepatocellular carcinoma (HCC) cells following MLK4 siRNA transfection. This compound effectively reduces reactive oxygen species (ROS) production associated with MLK4 knockdown and subsequently decreases apoptosis in these HCC cells. LL-Z1640-4 serves as a valuable tool for investigating the roles of p38 and JNK in cancer biology and therapeutic interventions.

ERK-MYD88 Interaction Inhibitor 1 specifically targets the interaction between ERK and MYD88. This compound promotes an integrated stress response mediated by HRI, resulting in immunogenic apoptosis within cancer cells. In preclinical studies, ERK-MYD88 Interaction Inhibitor 1 has demonstrated the ability to stimulate anti-tumor T cell responses in Lewis lung cancer mouse models, showcasing its potential as an anti-tumor agent.

OTS964 is a selective inhibitor of T-cell orientation protein kinase (TOPK), demonstrating a high affinity with an IC50 of 28 nM. Additionally, OTS964 effectively inhibits cyclin-dependent kinase 11 (CDK11), with a binding affinity (Kd) of 40 nM for CDK11B. This compound is utilized in research exploring cancer therapeutic strategies and cell cycle regulation.

MEK-IN-5 is a potent inhibitor of the MEK pathway, functioning by significantly decreasing the phosphorylation levels of MEK and ERK in a dose-dependent and time-dependent manner. In addition to its inhibitory effects on MEK signaling, MEK-IN-5 acts as a nitric oxide donor, contributing to its biological activity. This compound has been shown to induce apoptosis in MDA-MB-231 breast cancer cells, making it a valuable tool for research in cancer therapeutics and signaling pathways.

SB 202190 hydrochloride is a selective inhibitor of the p38 MAP kinase with IC50 values of 50 nM and 100 nM for p38α and p38β, respectively. By binding to the ATP pocket of active recombinant human p38 kinase with a Kd of 38 nM, it demonstrates significant anti-cancer activity. Furthermore, SB 202190 hydrochloride has been shown to induce autophagy, making it a valuable tool for research in cancer biology and signaling pathways related to stress response.