MAPK
Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
BRAF Kinase Inhibitor
Tinlorafenib is a potent inhibitor of BRAF and CRAF kinases, exhibiting IC50 values of 5.8 nM and 4.1 nM, respectively. It specifically targets V600E and V600K mutations in BRAF with IC50s of 4.25 nM and 2.7 nM, making it valuable for studying BRAF-driven tumors. Notably, Tinlorafenib demonstrates effective penetration of the blood-brain barrier, facilitating research into both central nervous system tumors and extracranial malignancies associated with BRAF mutations. -
MEK Inhibitor
Polfurmetinib is a potent MEK inhibitor that selectively targets the MEK signaling pathway. It effectively inhibits the phosphorylation of ERK1/2 at Thr202/Tyr204 in A375 melanoma cells, with an IC50 of 2 nM. This compound is primarily utilized in cancer research to investigate therapeutic strategies that disrupt the MEK/ERK signaling axis. -
p38 MAPK Inhibitor
Chicanine is a lignan derived from Schisandra chinensis that functions as a selective inhibitor of p38 MAPK. It effectively inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2, and IκB-α, demonstrating significant anti-inflammatory activity. This compound is valuable for research applications centered around inflammation, signaling pathways, and the modulation of MAPK-related processes. -
ERK Inhibitor
ZINC12409120 is a highly selective ERK inhibitor that targets the mitogen-activated protein kinase pathway. It disrupts the interaction between FGF23 and α-Klotho, leading to inhibition of ERK activity with an IC50 of 5.0 μM. This compound is valuable for research applications focused on cellular signaling pathways and their implications in various disease models. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 9 is a covalent inhibitor targeting ERK1/2, exhibiting sub-micromolar activity in cellular assays with a GI50 of 0.47 μM in A375 cells. This compound effectively downregulates phospho-ERK1/2 levels, thereby impacting downstream signaling pathways. Additionally, ERK1/2 Inhibitor 9 is functionalized with trans-cyclo-octene (TCO) and Tz-Thalidomide, enabling the formation of ERK-CLIPTAC for targeted degradation of ERK1/2. This makes it a valuable tool for research into cancer signaling mechanisms and targeted protein degradation strategies. -
ERK/JNK Inhibitor
Ambuic acid is a potent inhibitor targeting the ERK/JNK pathway, demonstrating notable anti-inflammatory effects. It displays significant antimicrobial activity against Staphylococcus aureus, with an IC50 value of 43.9 μM for the ATCC 6538 strain. Additionally, Ambuic acid inhibits the biosynthesis of cyclic peptide quorum sensing molecules in gram-positive bacteria, making it a valuable compound for research in antimicrobial and anti-inflammatory applications. -
ERK2 Inhibitor
ERK2-IN-4 is a selective inhibitor of the ERK2 pathway, demonstrating a Ki of 0.006 μM. This compound effectively disrupts ERK signaling, making it a valuable tool in cancer research. Its specificity and potency allow for detailed studies of ERK2's role in tumorigenesis and related signaling pathways. -
ERK5 Inhibitor
ERK5-IN-5 is an inhibitor of the ERK5 kinase, showcasing significant anti-cancer properties. This compound demonstrates notable anti-proliferative effects, with an IC50 value of 6.23 µg/mL against A549 lung cancer cells. ERK5-IN-5 is suitable for research applications focused on cancer biology and signaling pathways involving ERK5 modulation. -
HPK1 Inhibitor
HPK1-IN-61 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), exhibiting a Ki value of 0.4 nM. Additionally, it demonstrates strong inhibitory activity against Abl with an IC50 of less than 0.51 nM, and LCK with an IC50 of 24 nM. This compound is valuable for research applications focused on immune signaling and kinase regulation. -
BCR-ABL/SRC/p38 Inhibitor
CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications. -
Raf Inhibitor
ML786 is a potent Raf inhibitor with oral bioavailability, demonstrating IC50 values of 2.1 nM for V600EΔB-Raf, 4.2 nM for wild-type B-Raf, and 2.5 nM for C-Raf. Additionally, ML786 exhibits inhibitory effects on Abl-1, DDR2, EPHA2, KDR, and RET, with IC50 values under 0.5 nM, 7.0 nM, 11 nM, 6.2 nM, and 0.8 nM, respectively. This compound is suitable for research applications focused on cancer biology, helping to advance understanding of therapeutic targets within malignancies. -
HPK1 Inhibitor
HPK1-IN-2 dihydrochloride is a potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), exhibiting an IC50 of less than 0.05 μM. This compound also demonstrates inhibitory effects on Lck kinase with an IC50 range between 0.05 μM and 0.5 μM, as well as on Flt3, with an IC50 of less than 0.05 μM. Its biological activity and targeted inhibition make HPK1-IN-2 dihydrochloride a valuable tool for research focused on antitumor mechanisms and kinase pathway analyses. -
PDGFRβ/B-Raf Inhibitor
KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies. -
MEK Inhibitor
L-783277 is a potent MEK inhibitor with an IC50 of 4 nM, demonstrating significant inhibition against various kinases, including VEGFR2/3, FLT1/3/4, KDR, and PDGFRα. Although it exhibits low selectivity within its kinase targets, L-783277 effectively reduces cell viability and proliferation in H295R cells, with IC50 values of 22 μM and 21 μM, respectively. This compound is applicable in cancer research, particularly in the study of adrenocortical carcinoma. -
ERK/Insulin Receptor Inhibitor
ERK Inhibitor II (Negative Control) is a selective inhibitor of extracellular signal-regulated kinase (ERK) primarily affecting the insulin receptor pathway. This compound serves as a tool for investigating the role of ERK in various biological processes, particularly in the research of diabetes and insulin signaling mechanisms. Its application extends to studying the modulation of ERK activity and understanding associated cellular responses. -
MEK1/2 Inhibitor
SMK-17 is a selective, non-ATP-competitive inhibitor of MEK1 and MEK2, exhibiting IC50 values of 62 nM and 56 nM, respectively. By binding to the allosteric pocket of MEK1/2, SMK-17 effectively modulates the MAPK signaling pathway. This compound demonstrates significant biological activity by inducing apoptosis in tumor cell lines with β-catenin mutations, making it a valuable tool for cancer research and therapeutic investigations targeting these mutations. -
B-Raf Inhibitor
INU-152 is a potent and selective inhibitor of B-Raf, a key kinase in the MAPK signaling pathway. This compound effectively reduces tumor cell proliferation, enhances autophagy, and induces apoptosis through the inhibition of B-Raf activity. INU-152 demonstrates significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3), making it a valuable tool for cancer research applications. -
JNK Inhibitor
Cyy-272 is a potent orally active inhibitor of c-Jun N-terminal kinase (JNK), exhibiting IC50 values of 1.25 μM for JNK1, 1.07 μM for JNK2, and 1.24 μM for JNK3. This compound demonstrates significant anti-inflammatory properties by inhibiting JNK phosphorylation, effectively mitigating acute lung injury induced by lipopolysaccharide. Additionally, Cyy-272 reduces inflammation in cardiomyocytes and cardiac tissues affected by high lipid concentrations, contributing to decreased cardiac hypertrophy, fibrosis, and apoptosis. It is valuable for research into the mechanisms of obese cardiomyopathy and related cardiovascular disorders. -
TAK1 Inhibitor
Triptriolide is a TAK1 inhibitor that plays a pivotal role in regulating apoptosis in mouse podocytes. It enhances cell survival and protects podocyte function by modulating the Bcl-2 family proteins and inhibiting Caspase-3 activity. Additionally, Triptriolide activates the TAK1-NF-κB signaling pathway, leading to the upregulation of podocin. This reagent is relevant for studies focusing on kidney health and podocyte resilience under stress conditions. -
ERK1/2 Inhibitor
Methyl helicterate is a triterpenoid compound that functions as an inhibitor of the ERK1/2 signaling pathway. It demonstrates significant biological activity by inhibiting hepatic stellate cell activation and promoting apoptosis in these cells. This manipulation of the ERK1/2 pathway positions methyl helicterate as a valuable reagent for research focused on liver fibrosis and related conditions. -
p38/CK1 Inhibitor
Casein kinase 1δ-IN-29 is a potent inhibitor of p38α and casein kinase 1, demonstrating IC50 values of 0.041 µM for p38α, 0.005 µM for CK1δ, and 0.447 µM for CK1ε. This compound effectively interrupts the cell cycle at the subG1 phase and induces apoptosis in AC1-M88 cells. It serves as a valuable tool in research applications focused on cell cycle regulation and apoptosis pathways. -
B-Raf Inhibitor
B-Raf IN 9 is a potent B-Raf inhibitor with an IC50 of 24.79 nM, targeting the B-Raf signaling pathway. This compound induces apoptosis and causes cell cycle arrest at the G2/M phase. B-Raf IN 9 demonstrates significant antitumor activity against the human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM, making it a valuable tool for cancer research and therapeutic investigations. -
ERK1/2 Inhibitor
ERK1/2 inhibitor 13 is a potent dual inhibitor of ERK1 and ERK2, exhibiting IC50 values of 91.71 nM and 97.87 nM, respectively. This compound demonstrates significant activity in inhibiting the proliferation of tumor cell lines, including MCF-7, 4T1, MDA-MB-468, and HCC1970, with IC50 values ranging from 0.67 to 2.76 μM. Additionally, ERK1/2 inhibitor 13 effectually inhibits cancer cell migration and induces apoptosis and autophagy in MCF-7 cells, while also displaying antitumor and anti-metastatic properties in a 4T1 xenograft mouse model, making it a valuable reagent for cancer research applications. -
ERK1/2 Inhibitor
SF-3-030 is a selective, non-ATP competitive inhibitor of ERK1/2, targeting the MAPK signaling pathway. It has demonstrated the ability to induce apoptosis specifically in melanoma cells with mutated BRAF and activated ERK1/2 signaling. Additionally, SF-3-030 has shown potential in alleviating several characteristics of asthma in murine models, making it valuable for research focused on both melanoma and asthma pathophysiology. -
JNK2/3 Inhibitor
YL5084 is a covalent inhibitor targeting JNK2 and JNK3, demonstrating selectivity for these isoforms with IC50 values of 70 nM and 84 nM, respectively, while showing significantly reduced activity against JNK1 at 2173 nM. This compound exhibits JNK2-independent antiproliferative effects and effectively induces apoptosis without reliance on JNK2 pathways. YL5084 serves as a valuable tool for research into cellular signaling and cancer biology, particularly in studies focusing on the role of JNK isoforms in tumor growth and survival. -
TOPK Inhibitor
SKLB-C05 is a highly selective, orally active inhibitor of the T-Lymphokine-Activated Killer Cell-originated Protein Kinase (TOPK), exhibiting an IC50 of 0.5 nM. This compound has demonstrated the ability to induce apoptosis, downregulate c-Myc, and activate p53 while disrupting FAK/Src-mediated migratory signaling. Additionally, SKLB-C05 interferes with cell mitosis and displays significant anticancer activity specifically against TOPK-positive colorectal cancer, making it a valuable tool for cancer research. -
JNK3 Inhibitor
JNK3 inhibitor-5 is a selective inhibitor targeting JNK3, exhibiting a potent IC50 of 0.379 nM. This compound demonstrates significant neuroprotective activity by safeguarding neuronal cells from amyloid beta-induced apoptosis. Additionally, JNK3 inhibitor-5 is characterized by high cell permeability and is predicted to effectively cross the blood-brain barrier, making it a valuable tool for studying neurological disorders and related therapeutic applications. -
EGFR/BRAFV600E Inhibitor
EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
TNIK/MAP4K4 Inhibitor
Rentosertib is an orally active inhibitor of TNIK and MAP4K4, exhibiting IC50 values of 12-120 nM for both targets. This compound plays a crucial role in the modulation of signaling pathways involved in cell proliferation and survival. Relying on its potent inhibition, rentosertib is utilized in research applications exploring cancer biology and potential therapeutic interventions for related disorders. -
HPK1 Inhibitor
GNE-6893 is a selective inhibitor of HPK1, demonstrating a Ki of less than 0.02 nM. This compound enhances T cell receptor signaling and promotes IL-2 production in stimulated primary human T cells, making it valuable for the investigation of T cell activation mechanisms. GNE-6893 is particularly relevant for research applications focused on chronic refractory cancers. -
HPK1 Inhibitor
AZ3246 is a selective inhibitor of HPK1, exhibiting an IC50 of less than 3 nM. This compound promotes IL-2 secretion in T cells, with an EC50 of 90 nM, highlighting its immunomodulatory properties. AZ3246 serves as a valuable tool for research in cancer biology, particularly in the study of breast cancer therapeutics. -
HPK1 Inhibitor
HPK1-IN-68 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), with an IC50 value of 2.8 nM. This compound effectively blocks HPK1 signaling pathways, inhibits the phosphorylation of SLP76, and stimulates the production of the IL-2 cytokine. Additionally, HPK1-IN-68 counteracts the immunosuppressive effects of prostaglandin E2 (PGE2) and promotes the infiltration of CD3+/CD8+ T cells into tumor microenvironments, demonstrating T cell-dependent antitumor activity in a mouse colon cancer model. It is particularly relevant for research into colon cancer therapeutics. -
Pan-RAF Inhibitor
SJ-C1044 is a pan-RAF inhibitor that demonstrates both immunomodulatory and anti-tumor properties. This compound effectively targets wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values of 331, 257, and 187 nM, respectively, leading to inhibition of Kras activation and MEK-ERK phosphorylation, which reduces tumor cell proliferation. Additionally, SJ-C1044 exhibits inhibitory effects on VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM, respectively, contributing to the improvement of the tumor immune microenvironment via the inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is suitable for research applications in colorectal cancer studies. -
BRAF/VEGFR2 Inhibitor
Takeda-6D is a potent and orally active inhibitor targeting BRAF and VEGFR2, displaying IC50 values of 7.0 nM and 2.2 nM, respectively. This compound effectively suppresses angiogenesis by inhibiting the VEGFR2 signaling pathway in 293/KDR and VEGF-stimulated HUVEC cells. Additionally, Takeda-6D demonstrates significant inhibition of ERK1/2 phosphorylation, indicating its potential for antitumor activity in various cancer research applications. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
p38 MAPK Inhibitor
JNJ-49095397 is a selective inhibitor of p38 MAPK, targeting both the α and γ isoforms. This compound also exhibits inhibition of the SRC kinase family, particularly haematopoietic kinase (HCK). JNJ-49095397 demonstrates significant anti-inflammatory activities and is utilized in research focused on chronic obstructive pulmonary disease (COPD) and asthma. -
p38MAPK Inhibitor
SB 220025 is a selective inhibitor of p38 MAPK, operating through an ATP-competitive mechanism with an IC50 of 60 nM. This compound is effective in reducing the expression of the IL-8 gene in response to globular adiponectin, thereby decreasing inflammatory cytokine production and inhibiting angiogenesis. Additionally, SB 220025 demonstrates efficacy in preventing arthritis progression within chronic inflammatory disease models, making it a valuable tool for research on inflammation and related pathologies. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
P38-α/Syk Inhibitor
TOP1362 is a potent inhibitor targeting P38-α and Syk kinases, with Kd values of 26 nM and 18 nM, respectively. The compound demonstrates an IC50 of 14 nM in Src kinase activity assays, showcasing its efficacy in inhibiting P38-α, Src, and Syk. TOP1362 is applicable in research focused on dry eye syndrome and related pathways. -
RET/BRAF/S6K/Src Inhibitor
AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models. -
p38MAPK Inhibitor
SB 220025 (tri(hydrochloride)) is a reversible, orally active, ATP-competitive inhibitor of human p38 MAPK, with an IC50 of 60 nM. This compound also exhibits inhibition of p56Lck and PKC with IC50 values of 3.5 μM and 2.89 μM, respectively. SB 220025 trihydrochloride effectively reduces IL-8 gene expression in response to globular adiponectin and diminishes inflammatory cytokine production, making it a valuable tool for studying inflammation and angiogenesis. Additionally, it has shown efficacy in preventing the progression of arthritis in chronic inflammatory disease models. -
JNK/c-Met Inhibitor
JNK-IN-16 is a potent inhibitor of both JNK and c-Met, exhibiting IC50 values of 72 nM and 120 nM, respectively. This compound demonstrates significant anti-cancer activity, making it valuable for research in cancer biology and therapeutic development. Its dual inhibition profile allows for exploration in signaling pathways associated with tumor progression and metastasis. -
BTK/MNK Dual Inhibitor
QL-X-138 is a selective dual inhibitor of Bruton's tyrosine kinase (BTK) and MAPK-interacting kinase (MNK), demonstrating potent covalent binding to BTK and non-covalent binding to MNK. It exhibits IC50 values of 9.4 nM for BTK, and 107.4 nM and 26 nM for MNK1 and MNK2, respectively. Additionally, QL-X-138 displays antiviral activity against dengue virus serotype 2, with an IC50 of 3.5 μM. This compound is valuable for research involving B-cell malignancies and related therapeutic investigations. -
MAPKAPK2 Inhibitor
MK2-IN-1 is a selective inhibitor of MAPKAPK2 (MK2), exhibiting an IC50 of 0.11 µM. This compound significantly interferes with the phosphorylation of serine residues in Tfcp2l1, with an EC50 of 0.35 µM for phosphorylated HSP27. MK2-IN-1 serves as a valuable tool for studying the role of MK2 in cellular signaling pathways and its implications in various biological processes. -
TAK1/MAP4K2 Inhibitor
NG25 trihydrochloride is a potent dual inhibitor of TAK1 and MAP4K2, exhibiting IC50 values of 149 nM and 21.7 nM, respectively. This compound enhances the sensitivity of breast cancer cells to Doxorubicin, promoting apoptotic processes. NG25 trihydrochloride serves as a valuable tool for investigating therapeutic strategies in various cancer research applications. -
MAP4K4 Inhibitor
MAP4K4-IN-7 is a selective inhibitor of MAP4K4 that demonstrates moderate inhibitory activity against TNIK, MAP4K4, and MINK1, with pIC50 values of 6.8, 6.8, and 6.7, respectively. This compound can be utilized in research focused on cancer and neurological disorders, including conditions such as schizophrenia. Its ability to modulate MAP4K4 activity makes it a valuable tool for exploring therapeutic strategies in related pathologies. -
HPK1 Inhibitor
ZYF0033 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), achieving an IC50 of less than 10 nM by inhibiting the phosphorylation of MBP protein. This compound enhances anti-cancer immune responses, leading to a reduction in serine 376 phosphorylation of SLP76. In preclinical studies with the 4T-1 syngeneic mouse model, ZYF0033 demonstrated significant tumor growth inhibition and increased intratumoral infiltration of dendritic cells, natural killer cells, and CD107a+CD8+ T cells, while decreasing infiltration of various PD-1+ and TIM-3+ CD8+ T cell subsets. -
HPK1 Inhibitor
HPK1-IN-3 is a potent and selective ATP-competitive inhibitor of hematopoietic progenitor kinase 1 (HPK1; MAP4K1), exhibiting an IC50 of 0.25 nM. The compound demonstrates significant IL-2 potency, with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs). This makes HPK1-IN-3 a valuable tool for investigating the role of HPK1 in immune modulation and cellular signaling pathways. Its targeted inhibition offers potential applications in the study of hematopoietic cell functions and autoimmune disorders. -
HPK1 Inhibitor
DS21150768 is a selective inhibitor of HPK1, a key regulator of T-cell activation. This compound enhances T-cell function and may exhibit potential anticancer effects by modulating immune responses. DS21150768 is suitable for research applications focused on cancer immunotherapy and T-cell biology.
