MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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Inhibitor of the Phosphorylation of c-jun
TAT-JIP is an effective inhibitor of the phosphorylation of endogenous c-jun, particularly following activation by PHA-PMA. This compound is useful for studying the role of c-jun in various signaling pathways and cellular processes. Its application in research may extend to investigating the regulatory mechanisms involved in cell proliferation, differentiation, and response to stress. -
JNK3 Inhibitor
JNK3 Inhibitor-7 is a selective inhibitor of the c-Jun N-terminal kinase 3 (JNK3) pathway, exhibiting potent activity with IC50 values of 53 nM for JNK3, while demonstrating lesser inhibition against JNK2 and JNK1 at 973 nM and 1039 nM, respectively. This compound effectively crosses the blood-brain barrier and exhibits significant neuroprotective properties. JNK3 Inhibitor-7 holds potential for research applications related to neurodegenerative disorders, particularly Alzheimer's disease. -
p38 MAPK Activator
OVA-E1 peptide is an activator of p38 MAPK, derived from the original SIINFEKL sequence (OVA 257-264). This peptide effectively stimulates both p38 and JNK signaling pathways in both mutant and wild-type thymocytes. It serves as a valuable tool for studying MAPK pathways and their roles in cellular responses such as inflammation and stress signaling in various research applications. -
JNK Inhibitor
JNK-IN-24 is a selective inhibitor of c-Jun N-terminal kinase (JNK), demonstrating significant anti-metastatic properties in cancer research. By downregulating JNK and matrix metalloproteinase 1 (MMP1) expression in Scrib knockdown-induced cancer models, JNK-IN-24 facilitates recovery from tumorous phenotypes. This compound is suitable for investigations into a range of epithelial cell-derived cancers, contributing to the understanding of JNK's role in tumor progression and metastasis. -
c-Jun N-terminal Kinase Inhibitor
JNK-IN-19 is a selective inhibitor of c-Jun N-terminal kinase (JNK), an important regulator in cellular stress responses. This compound demonstrates significant biological activity by modulating pathways associated with apoptosis, inflammation, and cell survival. JNK-IN-19 shows potential utility in research focused on surgical interventions, neuroprotection, and conditions characterized by oxidative stress. It provides a valuable tool for investigating the role of JNK in various physiological and pathological processes. -
p38 MAPK Inhibitor, JNK Inhibitor
HE4-1 leech peptide is a selective inhibitor of p38 MAPK and c-Jun N-terminal kinase (JNK). It effectively suppresses macrophage migration while maintaining normal macrophage immunological functions, such as phagocytosis, lysozyme activity, and the expression of various inflammatory factors. This peptide is primarily utilized in research focused on atherosclerosis and inflammation-related studies. -
JNK3 Inhibitor
JNK3 Inhibitor-8 is a selective, orally bioavailable inhibitor targeting the c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 21 nM. It demonstrates pronounced neuroprotective effects and effectively crosses the blood-brain barrier. This compound is relevant for research applications related to neurodegenerative disorders, particularly Alzheimer’s disease. -
JNK3 Inhibitor
JNK3 Inhibitor-3 is a selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) that effectively permeates the blood-brain barrier and exhibits oral bioavailability. With IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM for JNK1, JNK2, and JNK3 respectively, JNK3 Inhibitor-3 demonstrates significant inhibitory effects across these kinase targets. This compound has been shown to enhance memory performance in mouse models of dementia, making it a valuable tool for research in Alzheimer’s disease and related neurodegenerative disorders. -
JNK Inhibitor
JNK-1-IN-4 is a selective inhibitor of the c-Jun N-terminal kinase (JNK) family, targeting JNK-1, JNK-2, and JNK-3 with IC50 values of 2.7 nM, 19.0 nM, and 9.0 nM, respectively. This compound effectively inhibits the phosphorylation of c-Jun and decreases the expression of TGF-β1-induced epithelial-to-mesenchymal transition (EMT) marker proteins, including fibronectin and α-SMA. JNK-1-IN-4 demonstrates favorable pharmacokinetic properties, evidenced by a bioavailability of 69%, and has shown anti-fibrotic effects in bleomycin-induced models of idiopathic pulmonary fibrosis. -
TOPK-p38/JNK Inhibitor
TOPK-p38/JNK-IN-1 is an orally active inhibitor targeting the TOPK-p38/JNK signaling pathway, exhibiting an IC50 value of 2.14 µM for nitric oxide production. This compound demonstrates significant anti-inflammatory activity by inhibiting the phosphorylation of downstream proteins while preventing degradation of TOPK. Research applications include studies on inflammatory processes and cellular signaling mechanisms in various disease models. -
JNK Inhibitor
ZG-10 is a selective inhibitor of JNK (c-Jun N-terminal kinase), demonstrating IC50 values of 809 nM for JNK1, 1140 nM for JNK2, and 709 nM for JNK3. This compound exhibits potential therapeutic benefits in mitigating SARS-CoV-2 infection. Its biological activity positions it as a valuable tool for research into cellular signaling pathways and antiviral strategies. -
JNK3/p38 Inhibitor
SR-3737 is a potent inhibitor of JNK3 and p38 mitogen-activated protein kinases, with IC50 values of 12 nM and 3 nM, respectively. This compound exhibits significant biological activity by modulating pathways involved in stress responses and inflammation. SR-3737 is useful in research applications focusing on neuronal signaling, cytokine production, and the molecular mechanisms underlying various neurodegenerative diseases. -
JNK3 Inhibitor
JNK3 Inhibitor-2 is a selective inhibitor targeting c-Jun N-terminal kinase 3 (JNK3), demonstrating an IC50 of 0.25 µM for JNK3, with minimal activity against JNK1 and JNK2 (>100 µM). This compound exhibits additional inhibitory effects on DDR1 and EGFR variants (T790M, L858R). JNK3 Inhibitor-2 is valuable for research applications focusing on cellular stress response and cancer signaling pathways, particularly in studies investigating JNK3’s role in neurodegeneration and oncogenesis. -
JNK Inhibitor
JNK-IN-20 is a selective JNK inhibitor targeting the c-Jun N-terminal kinase pathway. This compound demonstrates significant anti-inflammatory properties and exhibits potential in cancer research by modulating cell signaling pathways involved in tumor progression. JNK-IN-20 is suitable for studies focusing on inflammatory diseases and tumorigenesis. -
JNK Inhibitor
JD118 is a selective JNK inhibitor that predominantly targets JNK1, effectively modulating its activity and downstream signaling pathways. This compound has been shown to inhibit the expression of cJun (1–135), making it a valuable tool for research in cellular stress responses and apoptosis. JD118 is suitable for studies investigating the role of JNK signaling in various disease models, including cancer and neurodegeneration. -
JNK Inhibitor
AS601245 TFA is a selective, ATP-competitive inhibitor of c-Jun NH2-terminal protein kinases (JNK), demonstrating IC50 values of 150 nM for hJNK1, 220 nM for hJNK2, and 70 nM for hJNK3. This compound exhibits significant selectivity, being 10- to 20-fold more selective for JNK over kinases such as c-src, CDK2, and c-Raf, and shows more than 50- to 100-fold selectivity against various Ser/Thr and Tyr-protein kinases. AS601245 TFA is suitable for applications involving neuroprotection and the study of cellular stress response pathways in research settings. -
p38 Inhibitor
p38 Kinase Inhibitor 8 is a selective inhibitor of p38β and JNK2α2, demonstrating IC50 values of 6.3 nM and 53.6 nM, respectively. This compound has shown significant anti-inflammatory properties in models of collagen-induced arthritis in rats, making it a valuable tool for research into inflammatory diseases and related signaling pathways. Its orally active nature enhances its practicality for in vivo studies. -
RAF Molecular Glue
NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis. -
pan-RAF Inhibitor
Exarafenib is a selective pan-RAF inhibitor that is available for oral administration. It is effective in targeting RAF-dependent cancers, specifically those with various BRAF alterations, by suppressing MAPK signaling pathways. Exarafenib has demonstrated significant anticancer activity in preclinical studies, making it a valuable tool for research in oncology and potential therapeutic applications in melanoma and other RAF-driven malignancies. -
BRAF Inhibitor
Claturafenib is a potent, orally active pan-mutant BRAF inhibitor. It effectively inhibits phosphorylated ERK (pERK) in cells, demonstrating an IC50 value of 1.6 nM in HT29 cell lines. Claturafenib exhibits significant antitumor activity against non-small cell lung cancer (NSCLC) harboring the BRAFG469A mutation and melanoma with the BRAFK601E mutation, making it a valuable tool for cancer research focused on BRAF mutant pathways. -
BRAF Inhibitor
Mosperafenib is a selective BRAF inhibitor designed to target BRAF V600 mutations. It exhibits significant biological activity against BRAF-mutant solid tumors, including colorectal cancer (CRC). This reagent is used in various research applications, particularly in the study of malignancies driven by BRAF mutations, enabling investigations into disease mechanisms and therapeutic strategies. -
RAF Inhibitor
TBAP-001 is a pan-RAF kinase inhibitor that targets the RAF signaling pathway. It exhibits potent inhibitory activity with an IC50 of 62 nM in the BRAF V600E kinase assay. This compound is utilized in research applications aimed at understanding the role of RAF kinases in cancer progression and therapeutic resistance, making it valuable for studies focused on targeted cancer therapies. -
B-Raf Inhibitor
B-Raf IN 11 is a selective inhibitor of the B-RafV600E mutant kinase, demonstrating an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. This compound effectively inhibits the kinase activities of both B-RafV600E mutant and wild-type B-Raf, making it a valuable tool for investigating pathways related to colorectal cancer. Its application in research provides insight into therapeutic strategies targeting B-Raf mutations in cancer treatment. -
Raf Inhibitor
Flezurafenibum is a Raf kinase inhibitor that demonstrates significant antineoplastic activity. By selectively targeting the Raf pathway, it interferes with tumor growth and proliferation. This compound is of particular interest in cancer research, especially for studies involving Raf-mediated signaling pathways and potential therapeutic applications in various malignancies. -
BRAF Inhibitor
Uplarafenib is a selective BRAF inhibitor with an IC50 ranging from 50 to 100 nM. This compound displays significant antitumor activity, making it a valuable tool in cancer research. Uplarafenib is primarily utilized in studies investigating BRAF mutations and their role in tumorigenesis. -
BRAF Inhibitor
Braftide is an allosteric inhibitor of BRAF kinase that targets the dimer interface, effectively preventing the formation of BRAF dimers. It exhibits inhibitory activity against both wild-type BRAF and the oncogenic variant BRAFG469A, with IC50 values of 364 nM and 172 nM, respectively. By inhibiting the MAPK signaling pathway, Braftide demonstrates the ability to suppress the proliferation of KRAS mutant tumor cells, with EC50 values of 7.1 µM and 6.6 µM for HCT116 and HCT-15 cell lines, respectively. This compound is applicable in various cancer research studies. -
BRAF Inhibitor
B-Raf IN 15 is a potent BRAF inhibitor that selectively targets both BRAF wild-type and BRAF V600E variants, exhibiting IC50 values of 2.0 μM and 0.8 μM, respectively. This compound is particularly valuable in cancer research, facilitating studies on the pathways involved in tumor growth and progression. B-Raf IN 15 serves as an effective tool for evaluating therapeutic strategies and understanding the mechanisms of BRAF-related malignancies. -
RAF Inhibitor
PLX7922 is a selective RAF inhibitor that targets BRAFV600E mutations. It effectively inhibits phosphorylated ERK (pERK) in BRAFV600E cell lines, while paradoxically activating pERK in NRAS mutant cell lines. This compound is valuable for studying the signaling pathways involved in cancer, particularly in the context of RAS/RAF/MEK/ERK pathway alterations. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
RAF Inhibitor
GNE-9815 is a highly selective pan-RAF inhibitor that targets both CRAF and BRAF with Ki values of 0.062 nM and 0.19 nM, respectively. It demonstrates good oral bioavailability and, when used in conjunction with MEK inhibitors such as Cobimetinib, leads to synergistic modulation of the MAPK pathway. GNE-9815 is particularly useful in research focused on KRAS mutant cancers, facilitating the exploration of therapeutic strategies in this context. -
BRAF Inhibitor
Vem-L-Cy5 is a BRAF inhibitor that incorporates the near-infrared fluorophore cyanine-5 (Cy5). This compound specifically targets the BRAFV600E mutation and effectively inhibits MEK phosphorylation. Vem-L-Cy5 demonstrates cell permeability and has been shown to inhibit the growth of various cancer cell types, making it a valuable tool for cancer research and therapeutic development. -
b/cRAF Inhibitor
SHR902275 is a selective and potent b/cRAF inhibitor, specifically designed to target RAS mutant cancers. It demonstrates impressive inhibitory activity with IC50 values of 1.6 nM for cRAF, 10 nM for bRAFwt, and 5.7 nM for the bRAFV600E mutation. In cellular assays, SHR902275 effectively inhibits growth with GI50 values of 1.5 nM and 0.17 nM for H358, as well as 0.4 nM and 0.32 nM for A375 and Calu6, and SK-MEL2 cells, respectively. This compound holds potential for research applications focused on targeted cancer therapies and understanding RAF signaling pathways. -
Raf Inhibitor
Belvarafenib TFA is a potent pan-RAF inhibitor that targets the rapidly accelerated fibrosarcoma (RAF) family of kinases. It demonstrates impressive inhibitory activity, with IC50 values of 56 nM for B-RAF, 7 nM for B-RAFV600E, and 5 nM for C-RAF. This compound is valuable for research focusing on cancer therapeutics, particularly for the treatment of tumors driven by aberrant RAF signaling pathways. -
Raf Inhibitor
Brimarafenib is a selective inhibitor of Raf kinase, primarily targeting the MAPK/ERK signaling pathway. It exhibits significant antineoplastic activity, making it valuable for cancer research, specifically in the study of tumors driven by aberrant Raf signaling. Brimarafenib is utilized in preclinical models to investigate its therapeutic potential and mechanisms of action in various malignancies. -
Ras-Raf Inhibitor
Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways. -
c-Raf Inhibitor
(Z)-GW 5074 is a selective c-Raf inhibitor that demonstrates unique interactions with mutant huntingtin protein (mHTT) and LC3, without affecting wild-type huntingtin protein. This compound effectively inhibits c-Raf signaling, playing a crucial role in cellular responses associated with neurodegenerative disorders. (Z)-GW 5074 is primarily utilized in research focused on neurodegeneration and related biochemical pathways, providing valuable insights into therapeutic strategies targeting these diseases. -
Pan-RAF Kinase Inhibitor
Pan-RAF kinase inhibitor 1 is a selective inhibitor targeting the Pan-RAF kinase family, modulating the MAPK signaling pathway. This compound effectively suppresses the proliferation of RAS-mutant tumor cells, making it a valuable tool for investigating cancer biology. Its applications include research focused on therapeutic strategies for cancer treatment, particularly in the context of RAS mutations. -
RAF Inhibitor
Anticancer Agent 124 is a potent and selective pan RAF inhibitor that acts primarily on the RAF family of kinases. It effectively suppresses MAPK signaling in tumor cells harboring BRAF V600E, NRAS, and KRAS mutations. This compound is suitable for research applications aimed at understanding the role of RAF-mediated pathways in cancer progression and therapeutic resistance. -
C-RAF Kinase Inhibitor
C-RAF kinase-IN-1 is a selective inhibitor of C-RAF kinase, demonstrating an IC50 value of 0.193 μM. As a quinoline derivative, it plays a significant role in inhibiting C-RAF-mediated signaling pathways. This compound is primarily utilized in cancer research, providing insights into therapeutic targeting and the underlying mechanisms of cancer progression. -
B-Raf Inhibitor
B-Raf IN 5 is a highly effective B-Raf inhibitor, demonstrating an IC50 of 2.0 nM. This compound selectively targets B-Raf without binding to the secondary target PXR and exhibits resistance to rapid metabolism. B-Raf IN 5 is ideal for research applications focused on cancer biology and therapeutic interventions targeting B-Raf-driven malignancies. -
BRAF Inhibitor
SB-699393 is a potent BRAF inhibitor with a dissociation constant (Kd) of 7.2 nM, demonstrating the ability to effectively cross the blood-brain barrier. This makes SB-699393 a valuable tool for investigating the role of BRAF in neurological conditions, including stroke. Its selective inhibition of BRAF can aid in the elucidation of signaling pathways and therapeutic strategies in related research applications. -
BRAF Inhibitor
B-Raf IN 13 is a potent BRAF inhibitor, demonstrating an IC50 of 3.55 nM in assays targeting the BRAF V600E mutant enzyme. This compound exhibits significant anti-cancer activity, making it a valuable tool for research into targeted therapies for cancers associated with BRAF mutations. Its application spans studies focused on the modulation of cellular signaling pathways linked to oncogenesis. -
RAF/MEK Inhibitor
Avutometinib potassium is a potent RAF/MEK inhibitor that effectively prevents MEK phosphorylation by ARAF, BRAF, and CRAF through the formation of dominant negative RAF-MEK complexes. This compound exhibits significant anti-proliferative activity across various tumor cell lines, particularly those with KRAS mutations, including pancreatic ductal adenocarcinoma (PDAC) cell lines. In vivo studies demonstrate that Avutometinib potassium inhibits tumor growth and enhances survival in mouse models of KRAS and p53 mutant pancreatic cancer. It holds potential for research in low-grade serous ovarian carcinoma and other oncogenic conditions involving the RAF/MEK pathway. -
RAF Inhibitor
LSN3074753 is a pan-RAF inhibitor targeting RAF monomers and dimers, particularly effective against tumor cells with activated MAPK pathways driven by BRAF or KRAS mutations. This reagent exhibits significant antitumor activity, making it a valuable tool for research applications involving colorectal cancer models. In combination with Cetuximab, LSN3074753 produces additive and synergistic effects, highlighting its potential for therapeutic strategies in tumors with specific genetic alterations such as KRAS or BRAF mutations. -
Raf
SB-682330A is a selective inhibitor of Raf kinase, a key component of the MAPK signaling pathway. This compound demonstrates potent inhibition of Raf, leading to decreased cellular proliferation and survival in cancer cells. SB-682330A is primarily used in research investigating the role of Raf in oncogenic signaling and as a potential therapeutic agent in targeted cancer therapies. -
BRAFV600E Inhibitor
BRAFV600E-IN-2 is a potent BRAFV600E inhibitor with an IC50 of less than 10 nM, demonstrating significant anti-tumor activity. This compound is valuable for research applications focused on targeted cancer therapies, particularly those involving BRAF-mutant tumors. Its efficacy underscores its potential utility in investigating mechanisms of resistance and sensitivity in cancer treatment. -
BRAF-V600E Degrader
CST905 is a highly effective PROTAC degrader specifically targeting the BRAF-V600E mutation, demonstrating a DC50 value of 18 nM. This compound facilitates the selective degradation of the BRAF-V600E protein, making it a valuable tool for cancer research aimed at understanding and addressing mutant BRAF-driven tumors. Its ability to modulate protein levels through targeted ubiquitination offers significant potential for therapeutic applications in oncology. -
B-Raf Inhibitor
B-Raf IN 7 is a potent inhibitor of the B-Raf kinase, demonstrating an IC50 value of 110.23 nM. This compound has shown significant antitumor activity in various cancer cell lines, including colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela), and human prostate cancer (PC-3), with IC50 values ranging from 7.50 to 12.83 µM. B-Raf IN 7 is a valuable tool for research in cancer biology and therapeutic development targeting the RAS/RAF/MEK/ERK signaling pathway. -
pan-Raf Inhibitor
Pan-Raf/RTK inhibitor 1 (compound I-16) is a highly selective pan-Raf inhibitor that targets the Raf kinases with IC50 values of 3.49 nM for BRafV600E, 8.86 nM for ARaf, 5.78 nM for BRafWT, and 1.65 nM for CRaf. This compound exhibits significant antiproliferative effects across a range of cancer cell lines, making it a valuable tool for cancer research. Its ability to inhibit multiple Raf isoforms facilitates studies investigating the role of the Raf signaling pathway in tumorigenesis and therapeutic resistance. -
Raf Inhibitor
ISIS 5132 is a phosphorothioate oligonucleotide consisting of 20 bases that specifically targets and down-regulates c-raf expression. By inhibiting the expression of c-raf, this compound modulates downstream signaling pathways involved in cell proliferation and survival. ISIS 5132 is valuable for research applications focused on cancer biology and therapeutic development associated with Raf signaling pathways.
