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GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM .
Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis .
ASK1-IN-5 (S-99) is an inhibitor of apoptosissignal-regulated kinase 1 (ASK1) and is useful in the study of autoimmune and neurodegenerative diseases .
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes .
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation .
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
DL-threo-Dihydrosphingosine is a extracellular signal-regulated kinase(ERK)signalling cassette inhibitor and is effective against both growth factor- and G-protein-dependent activation of ERK. DL-threo-Dihydrosphingosine inhibits smooth muscle cell proliferation and can be used for study of asthma .
12-epi-LTB4 is an agonist for BLT1 and BLT2. 12-epi LTB4 exhibits a partial agonistic activity against mBLT1 and mBLT2, and induces phosphorylation of extracellular signal-regulated kinase in primary mouse keratinocytes .
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
Insulin Detemir is an artificial insulin, shows effect on controlling blood sugar levels. Insulin Detemir stimulates GLP-1 secretion as a consequence of enhanced Gcg expression by a mechanism involving activation of Akt- and/or extracellular signal-regulated kinase (ERK)-dependent-cat and CREB signaling pathways. Insulin Detemir can be used for type 2 diabetes research .
AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity .
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
Lyso-sulfatide (bovine) ammonium, a derivative of the glycosphingolipid sulfatide, acts as an extracellular signal regulating the migration of a neural precursor cell line (B35 neuroblastoma cells) by rapidly promoting process retraction and cell rounding .
RIPK2-IN-2 (example 25) is a RIP2 kinasePROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases .
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .
ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1) .
NSC 295642 is a phosphatase inhibitor. NSC 295642 can significantly increase phospho-Erk cytonuclear differences in intact cells. NSC 295642 can be used for the research of cancer .
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic agent candidate for cancer research .
Sphinganine 1-phosphate (D-erythro-Dihydrosphingosine 1-phosphate) is a polar sphingolipid metabolite that regulates cell migration, differentiation, survival and complex physiological processes .
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
Insulin Detemir is an artificial insulin, shows effect on controlling blood sugar levels. Insulin Detemir stimulates GLP-1 secretion as a consequence of enhanced Gcg expression by a mechanism involving activation of Akt- and/or extracellular signal-regulated kinase (ERK)-dependent-cat and CREB signaling pathways. Insulin Detemir can be used for type 2 diabetes research .
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
Sphinganine 1-phosphate (D-erythro-Dihydrosphingosine 1-phosphate) is a polar sphingolipid metabolite that regulates cell migration, differentiation, survival and complex physiological processes .
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
The p38 gamma/MAPK12 protein is an important serine/threonine kinase in the MAP kinase pathway and can respond to extracellular stimuli such as pro-inflammatory cytokines or stress. p38 MAPK activates transcription factors such as ELK1 and ATF2, each of which phosphorylates approximately 200 to 300 substrates. p38 gamma/MAPK12 Protein, Human (sf9) is the recombinant human-derived p38 gamma/MAPK12 protein, expressed by Sf9 insect cells , with tag free and with residual Gly-Pro in N-terminal (not related to functional changes).
ERK1 protein is an important serine/threonine kinase in the MAP kinase pathway and cooperates with MAPK1/ERK2 to activate the MAPK/ERK cascade. Stimulated by KIT and KITLG/SCF, this pathway plays a key role in cell growth, adhesion, survival, and differentiation. ERK1 Protein, Human (GST) is the recombinant human-derived ERK1 protein, expressed by E. coli , with N-GST labeled tag. The total length of ERK1 Protein, Human (GST) is 378 a.a., .
The p38 gamma/MAPK12 protein is an important serine/threonine kinase in the MAP kinase pathway and can respond to extracellular stimuli such as pro-inflammatory cytokines or stress. p38 MAPK activates transcription factors such as ELK1 and ATF2, each of which phosphorylates approximately 200 to 300 substrates. p38 gamma/MAPK12 Protein, Human (sf9, His-GST) is the recombinant human-derived p38 gamma/MAPK12 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
ERK3 Protein, an atypical MAPK, phosphorylates MAP2 and MAPKAPK5. Interacting with MAPKAPK5, ERK3/MAPK6 undergoes Ser-189 phosphorylation, facilitating MAPKAPK5 activation. Activated MAPKAPK5 reciprocally phosphorylates ERK3/MAPK6. The complex's precise functional implications, especially in cell cycle entry, remain elusive. ERK3 Protein, Human is the recombinant human-derived ERK3 protein, expressed by E. coli , with tag free. The total length of ERK3 Protein, Human is 319 a.a., .
ERK3 Protein, an atypical MAPK, phosphorylates MAP2 and MAPKAPK5. Interacting with MAPKAPK5, ERK3/MAPK6 undergoes Ser-189 phosphorylation, facilitating MAPKAPK5 activation. Activated MAPKAPK5 reciprocally phosphorylates ERK3/MAPK6. The complex's precise functional implications, especially in cell cycle entry, remain elusive. ERK3 Protein, Human (His) is the recombinant human-derived ERK3 protein, expressed by E. coli , with N-6*His labeled tag. The total length of ERK3 Protein, Human (His) is 319 a.a., .
MAPK4, an atypical MAPK protein, phosphorylates microtubule-associated protein 2 (MAP2) and MAPKAPK5, forming a complex with intricate phosphorylation events. Interaction with MAPKAPK5 leads to ERK3/MAPK6 phosphorylation at Ser-189, activating MAPKAPK5, which reciprocally phosphorylates ERK3/MAPK6. The specific cellular role of this interplay, while unclear, suggests ERK3's potential involvement in promoting entry into the cell cycle. MAPK4 Protein, Human (Sf9, His, GST) is the recombinant human-derived MAPK4 protein, expressed by Sf9 insect cells , with N-8*His, N-GST labeled tag. The total length of MAPK4 Protein, Human (Sf9, His, GST) is 586 a.a., .
phospho-ERK1 + 2 (Thr183/Tyr185) Antibody is an unconjugated, approximately 42/44 kDa, rabbit-derived, anti-phospho-ERK1 + 2 (Thr183/Tyr185) polyclonal antibody. phospho-ERK1 + 2 (Thr183/Tyr185) Antibody can be used for: WB, ELISA, IHC-P, IHC-F, ICC, IF expriments in human, mouse, and predicted: rat, chicken, dog, cow, horse, rabbit, guinea pig background without labeling.
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