MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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p38 MAPK Inhibitor
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. -
p38 Inhibitor
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. -
MEK1/2 Inhibitor
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. -
JNK/c-Jun Activator
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. -
EGFR/BRAF Inhibitor
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 Inhibitor
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. -
EGFR/ERK Activator
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. -
JNK Inhibitor, ERK Inhibitor, TGFβ signaling Activator
(+)-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. -
Raf/EGFR Inhibitor
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. -
Insulin/IGF-1/p38 MAPK Regulator
2-Hydroxyisobutyric acid (2-HIBA) is a selective modulator of the Insulin/IGF-1 signaling pathway and p38 MAPK pathway, known for its ability to decrease reactive oxygen species and fat accumulation in Caenorhabditis elegans. This compound enhances β-oxidation while suppressing fatty acid synthesis via upregulation of SKN-1/NRF2 and downregulation of SREBP-1c transcription factors. 2-HIBA exhibits notable anti-aging and lipid-lowering properties, making it valuable for investigating metabolic diseases, including obesity and diabetes. Additionally, it serves as a renewable precursor for methacrylate production through 2-HIB-CoA mutase-mediated biosynthesis. -
MNK1/MNK2 Inhibitor
HD202A is a selective dual inhibitor of MNK1 and MNK2, exhibiting IC50 values of 6.09 nM and 8.06 nM, respectively. This compound effectively inhibits the MNK-eIF4E signaling pathway, leading to downregulation of perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α. HD202A enhances mitochondrial fatty acid oxidation, redox homeostasis, and demonstrates significant effects on metabolic health, including suppression of body weight gain, reduction in hepatic lipid accumulation, and improvement in glucose tolerance and insulin sensitivity. These properties make HD202A a valuable tool for researching metabolic dysfunction-associated steatotic liver disease. -
MNK1/2 Inhibitor
MNK1/2-IN-7 is a selective inhibitor of MNK1 and MNK2, primarily targeting the MNK/eIF4E signaling pathway. This compound exhibits potent anticancer activity by effectively inhibiting the phosphorylation of eIF4E, which contributes to reduced cancer cell proliferation. Additionally, MNK1/2-IN-7 demonstrates favorable hERG safety profiles, making it a valuable tool for research applications in oncology, particularly in combination therapies with agents like Ibrutinib. -
BAY-293 Negative Control
(S)-BAY-293 serves as a negative control for the potent KRAS-SOS1 interaction inhibitor, BAY 293. This compound is utilized in experimental settings to validate the specificity and efficacy of BAY 293 in studying KRAS signaling pathways. Researchers can use (S)-BAY-293 to ensure experimental results are due to the intended inhibition and not off-target effects. -
HPK1 Inhibitor
HPK1-IN-69 is a potent inhibitor of HPK1 with an IC50 of 1.7 nM. This compound disrupts the HPK1-mediated T cell receptor signaling pathway, decreasing SLP76 phosphorylation and enhancing IL-2 release. In vivo studies demonstrate its anti-tumor efficacy in mouse models, making it a valuable reagent for investigating colorectal cancer and MC38 syngeneic tumors. -
SOS1 Inhibitor
SOS1-IN-8 is a selective inhibitor of the SOS1 protein, exhibiting IC50 values of 11.6 nM for the SOS1-G12D variant and 40.7 nM for the SOS1-G12V variant. This compound serves as a valuable tool in the study of SOS1-mediated signaling pathways and their implications in various cancers. Its potent inhibitory activity makes it suitable for investigating therapeutic strategies targeting oncogenic mutations associated with SOS1. -
SOS1 Inhibitor
SOS1-IN-16 is a selective inhibitor of the SOS1 protein with an IC50 of 7.2 nM, making it a potent tool for studying SOS1-mediated signaling pathways. This compound exhibits inhibitory activity towards CYP3A4 when testosterone is utilized as a substrate, with an IC50 of 8.9 μM. SOS1-IN-16 is primarily applied in cancer research, facilitating the investigation of therapeutic strategies targeting SOS1-related oncogenic processes. -
SOS1 Inhibitor
SOS1-IN-7 is a selective inhibitor targeting SOS1, demonstrating potent activity with IC50 values of 20 nM for the SOS1-G12D mutant and 67 nM for the SOS1-G12V variant. This compound effectively disrupts SOS1-mediated signaling pathways, making it a valuable tool for investigating the roles of SOS1 in cancer biology. Its application in research may facilitate the development of therapeutic strategies against tumors driven by mutant RAS signaling. -
SOS1 Inhibitor
SOS1-IN-25 is a selective inhibitor of the SOS1 protein, effectively disrupting the formation of the KRASG12C/SOS1 complex with an IC50 of 11.11 nM. This compound demonstrates a dose-dependent reduction in phosphorylated ERK levels, indicating its potential to modulate downstream signaling pathways. SOS1-IN-25 is suitable for research focused on leukemia and other cancers associated with aberrant KRAS signaling. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-5 is a potent PROTAC compound that targets SOS1 for ubiquitin-proteasome mediated degradation. It exhibits strong biological activity, demonstrated by a DC50 value of 13 nM and an IC50 of 5 nM in inhibiting the proliferation of NCI-H358 cells. This reagent is valuable for research applications investigating the role of SOS1 in cancer biology and provides insights into targeted protein degradation strategies. -
SOS1 Ligand
SOS1 Ligand intermediate-4 is a key ligand for SOS1, playing a crucial role in the development of PROTAC-based degradation systems targeting SOS1. This compound facilitates the synthesis of SOS1 degraders, which can be employed in research related to targeted protein degradation and the modulation of oncogenic signaling pathways. Its ability to selectively interact with SOS1 makes it a valuable tool for investigating cellular mechanisms and therapeutic strategies in cancer biology. -
SOS1 Inhibitor
SOS1-IN-3 is a potent inhibitor of SOS1 (son of sevenless homolog 1) with an IC50 value of 5 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research in cancer biology. Its specificity for SOS1 allows for potential applications in studying the molecular mechanisms of cancer signaling pathways. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-7 is a targeted degradation compound designed to selectively degrade SOS1, a critical regulator in tumorigenesis. This PROTAC exhibits anti-tumor activity by promoting the ubiquitination and subsequent proteasomal degradation of SOS1. It is useful for researchers investigating the effects of SOS1 inhibition in cancer models and exploring potential therapeutic strategies for malignancies involving aberrant SOS1 signaling pathways. -
SOS1 Inhibitor
SOS1-IN-12 is a highly potent inhibitor of son of sevenless homolog 1 (SOS1), exhibiting a Ki value of 0.11 nM for SOS1 and an IC50 of 47 nM for phosphorylated ERK (pERK). This compound serves as a valuable tool for investigating the role of SOS1 in signaling pathways associated with cancer biology, enabling researchers to explore its potential in anticancer studies and therapeutic applications. -
SOS1 Inhibitor
SOS1-IN-10 is a selective inhibitor of SOS1, exhibiting a potent inhibitory effect with an IC50 value of 13 nM specifically targeting the KRAS G12C-SOS1 interaction. This compound is valuable for research studying the role of SOS1 in oncogenic signaling pathways, particularly in cancer models driven by KRAS mutations. Its use can facilitate investigations into therapeutic strategies aimed at modulating RAS-dependent pathways. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-6 is a targeted degradative compound designed to selectively degrade the SOS1 protein through a PROTAC mechanism. By utilizing a ligand for SOS1, an E3 ubiquitin ligase ligand, and an effective linker, this reagent enhances the efficacy of KRASG12C inhibitors. Its application is primarily in the study of KRAS-driven cancers and the exploration of protein homeostasis through targeted protein degradation pathways. -
SOS1 Inhibitor
HH0043 is a potent SOS1 inhibitor with an IC50 value of 5.8 nM. This orally active compound exhibits significant inhibition of the SOS1 protein, which plays a critical role in Ras signaling pathways. HH0043 is utilized in cancer research to explore therapeutic strategies targeting oncogenic signaling mechanisms. -
SOS1 Inhibitor
NSC-658497 is a potent inhibitor of the Ras guanine nucleotide exchange factor SOS1. It competitively binds to SOS1, thereby effectively inhibiting the SOS1-Ras interaction and reducing SOS1's guanine nucleotide exchange factor activity in a dose-dependent manner. This compound has demonstrated significant efficacy in suppressing Ras signaling pathways, ultimately leading to a reduction in associated cell proliferation. NSC-658497 is valuable for research in cancer biology and signaling modulation. -
SOS1 Inhibitor
SOS1-IN-4 is a potent inhibitor of SOS1, exhibiting an IC50 of 56 nM for the KRAS-C12C/SOS1 interaction. This compound is instrumental in studies investigating the role of SOS1 in RAS signaling pathways. Its application is significant in cancer research, particularly in models where KRAS mutations contribute to tumorigenesis. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-9 is a PROTAC (Proteolysis Targeting Chimeras) compound designed for targeted degradation of the SOS1 protein. It employs a specific ligand to bind SOS1, linking it to an E3 ligase for ubiquitination and subsequent proteasomal degradation. This compound is useful in research applications focused on elucidating SOS1's role in cellular signaling pathways and its implications in disease contexts such as cancer. -
SOS1 Inhibitor
SOS1-IN-2 is a potent inhibitor of SOS1, demonstrating an IC50 value of 5 nM. Its primary mechanism involves the inhibition of SOS1-mediated signaling pathways, making it a valuable tool in cancer research. This compound is suitable for studies focused on tumor biology and the exploration of therapeutic strategies targeting the SOS1 pathway. -
PROTAC SOS1 Degrader
(4S)-PROTAC SOS1 degrader-1 is a selective degrader targeting SOS1 through the PROTAC mechanism. This compound effectively reduces the expression of phosphorylated ERK (pERK) and levels of RAS-GTP in a dose-dependent manner, making it a valuable tool for studying RAS signaling. Its ability to significantly inhibit tumor growth in vivo underscores its potential applications in cancer research and therapy. -
SOS1 Inhibitor
SOS1-IN-5 is a potent inhibitor of SOS1, a critical component in RAS signaling pathways. This pyrimidobicyclic derivative disrupts the interaction between RAS and SOS1, effectively blocking KRAS activation and offering broad-spectrum inhibition of KRAS activity. SOS1-IN-5 is intended for use in cancer research, providing valuable insights into therapeutic strategies targeting KRAS-driven malignancies. -
SOS1/KRAS Inhibitor
SOS1/KRAS-IN-1 is a potent inhibitor targeting the SOS1/KRAS signaling pathway, critical in various cancers. This compound effectively disrupts SOS1-mediated activation of KRAS, providing valuable insights into SOS1/KRAS-mediated diseases. It is suitable for research applications investigating oncogenic signaling and potential therapeutic strategies against KRAS-driven malignancies. -
KRAS Inhibitor
SOF-436 is a selective KRAS inhibitor that targets SOS1-mediated nucleotide exchange, exhibiting an IC50 of 60 μM. Additionally, it effectively disrupts the interaction between KRAS and the effector protein RAF. This compound is primarily utilized in cancer research, providing insights into KRAS-driven oncogenic pathways. -
PROTAC SOS1 Degrader
PROTAC SOS1 Degrader-10 is a novel PROTAC compound designed to target and degrade the son of sevenless 1 (SOS1) protein via a cereblon (CRBN) and proteasome-dependent pathway. It effectively reduces SOS1 levels in KRAS mutant cancer cell lines, including SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. In addition to inducing degradation, PROTAC SOS1 Degrader-10 also inhibits cell proliferation in these models, displaying IC50 values of 36.7, 52.2, and 107 nM. Furthermore, it inhibits ERK phosphorylation, highlighting its potential role in cancer research and therapeutic applications targeting the RAS signaling pathway. -
SOS1 Inhibitor
SOS1-IN-9 is a selective inhibitor of SOS1, demonstrating an IC50 of 116.5 nM for the SOS1-KRAS G12C complex. This compound plays a crucial role in inhibiting SOS1-mediated signaling pathways, making it a valuable tool for research into KRAS-driven cancers. Its application extends to studies aimed at elucidating the mechanisms of oncogenic signaling and developing targeted therapeutic strategies. -
SOS1 Inhibitor
SOS1-IN-6 is a selective inhibitor of SOS1, demonstrating potent activity with IC50 values of 14.9 nM for the SOS1-G12D variant and 73.3 nM for SOS1-G12V. This compound is primarily utilized in research focused on RAS signaling pathways and cancer biology, offering potential insights into therapeutic strategies targeting oncogenic mutations. Its effectiveness makes SOS1-IN-6 a valuable tool for investigating the modulation of SOS1-related cellular processes. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-3 is a targeted protein degradation compound that selectively promotes the degradation of SOS1 via the ubiquitin-proteasome pathway. This degrader exhibits potent activity in downregulating SOS1, a key player in RAS signaling pathways. It is useful for researchers studying the roles of SOS1 in cancer biology and therapeutic interventions that disrupt aberrant signaling associated with this target. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-8 is a PROTAC-based molecule designed to target and degrade the SOS1 protein. By utilizing a specific SOS1 ligand, a linker, and an E3 ligase ligand, this compound promotes the ubiquitination and subsequent proteasomal degradation of SOS1. Its primary biological activity involves the modulation of downstream signaling pathways associated with oncogenic processes. This reagent is suitable for research applications focused on elucidating the role of SOS1 in cancer biology and exploring novel therapeutic strategies. -
PROTAC SOS1 degrader
PROTAC SOS1 degrader-1 is a targeted degrader that effectively induces the degradation of SOS1, with an observed DC50 value of 98.4 nM. This compound exhibits significant antiproliferative activity against cancer cells harboring various KRAS mutations. Additionally, PROTAC SOS1 degrader-1 demonstrates notable antitumor effects while maintaining low toxicity, making it a valuable tool for research in cancer therapeutics. -
SOS1/KRAS Inhibitor
SAH-SOS1A is a peptide-based inhibitor targeting the SOS1/KRAS protein interaction. It binds with nanomolar affinity (EC50 = 106-175 nM) to both wild-type and various mutant forms of KRAS, including G12D, G12V, G12C, G12S, and Q61H. By directly obstructing nucleotide association, SAH-SOS1A interferes with KRAS-driven cancer cell viability and inhibits the ERK-MAPK phosphosignaling cascade downstream of KRAS, making it a valuable tool for cancer research and therapeutic exploration. -
PROTAC SOS1 Degrader
SIAIS562055 is a cereblon-based PROTAC targeting the SOS1 protein, exhibiting a dissociation constant (Kd) of 95.9 nM. This compound effectively induces degradation of SOS1, leading to downstream inhibition of ERK signaling pathways. Notably, SIAIS562055 blocks the interaction of KRASG12C and KRASG12D with SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. Its potent anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
SOS1 Inhibitor
SOS1-IN-13 is a potent inhibitor of son of sevenless homolog 1 (SOS1), exhibiting IC50 values of 6.5 nM for SOS1 and 327 nM for phosphorylated extracellular signal-regulated kinase (pERK). This compound is valuable in anticancer research, providing insights into the role of SOS1 in tumorigenesis and signaling pathways associated with cell proliferation and survival. Its high selectivity allows for targeted studies of SOS1-mediated mechanisms in various cancer models. -
SOS1 Inhibitor
KRAS G12C inhibitor 56 is a selective SOS1 inhibitor that exhibits potent inhibitory activity with an IC50 of 1.6 nM. This compound is relevant for cancer research, particularly in studies targeting KRAS-driven malignancies, and may provide insights into therapeutic strategies for tumors harboring KRAS G12C mutations. Researchers can leverage this inhibitor to explore the biochemical mechanisms of cell signaling and proliferation linked to KRAS activation. -
p38 MAPK inhibitor
Losmapimod, also know as GW856553 or GW856553X, is a drug developed by GlaxoSmithKline which acts as a selective inhibitor of the enzyme family known as p38 mitogen-activated protein kinases. -
RAF inhibitor
PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively. -
p38 MAPK inhibitor
Talmapimod (SCIO-469) is a selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro).
