Search Result
Results for "
ERK1/2 phosphorylation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-122246
-
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GPR55
PKC
ERK
Arrestin
|
Metabolic Disease
|
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
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-
-
- HY-124740
-
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Melanocortin Receptor
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Cancer
|
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .
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-
-
- HY-50706
-
Selumetinib
Maximum Cited Publications
61 Publications Verification
AZD6244; ARRY-142886
|
MEK
Apoptosis
|
Cancer
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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
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-
-
- HY-P3751
-
-
-
- HY-50706A
-
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
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-
-
- HY-100403
-
|
mGluR
|
Cancer
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist?and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
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-
-
- HY-153445
-
|
ERK
MEK
|
Cancer
|
MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
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-
-
- HY-162460
-
|
ERK
|
Cancer
|
ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
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-
-
- HY-P5977
-
Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide
|
ERK
|
Cancer
|
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
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-
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- HY-N2858
-
|
Apoptosis
|
Cancer
|
Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .
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-
-
- HY-147301
-
AP1189
|
Melanocortin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research .
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-
-
- HY-147301A
-
AP1189 acetate
|
Melanocortin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon acetate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research .
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-
-
- HY-155533
-
|
SHP2
|
Cancer
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YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
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-
-
- HY-107640
-
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MMP
|
Cancer
|
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .
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-
-
- HY-13241
-
LY2228820 dimesylate
|
p38 MAPK
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
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-
-
- HY-N1987
-
|
Apoptosis
|
Inflammation/Immunology
|
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
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-
-
- HY-146672
-
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Itk
|
Cancer
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
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-
-
- HY-150700
-
|
ERK
|
Metabolic Disease
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
|
-
-
- HY-13241A
-
LY2228820
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Cancer
|
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
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-
-
- HY-126477
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NNK
1 Publications Verification
|
Endogenous Metabolite
|
Cancer
|
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
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-
-
- HY-13905
-
HHGV678 mesylate
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
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-
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- HY-16697
-
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GPR55
|
Cancer
|
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
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-
-
- HY-P0178
-
|
Integrin
|
Inflammation/Immunology
|
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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-
-
- HY-N10047
-
|
NF-κB
PPAR
|
Cardiovascular Disease
|
7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .
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-
-
- HY-154985
-
|
PPAR
Bombesin Receptor
ERK
|
Metabolic Disease
|
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
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-
-
- HY-155417
-
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Others
|
Neurological Disease
|
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
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-
-
- HY-76474A
-
|
Apoptosis
Syk
|
Inflammation/Immunology
Cancer
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BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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-
-
- HY-76474
-
|
Syk
Apoptosis
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Inflammation/Immunology
Cancer
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
-
- HY-14985
-
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
-
- HY-N0774
-
|
ERK
COX
MMP
Toll-like Receptor (TLR)
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Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
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-
-
- HY-P0178A
-
|
Integrin
|
Inflammation/Immunology
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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-
-
- HY-111083
-
CID23612552
|
GPR55
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Others
|
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .
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-
-
- HY-147301B
-
AP1189 methanesulfonate
|
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
Resomelagon methanesulfonate (AP1189 methanesulfonate) is the methanesulfonate salt form of Resomelagon (HY-147301). Resomelagon methanesulfonate is an orally active melanocortin receptor (MR) agonist. Resomelagon methanesulfonate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon methanesulfonate exhibits anti-inflammatory activity in mouse peritonitis and peritonitis model. Resomelagon methanesulfonate can be used for obesity and chronic inflammation research .
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-
-
- HY-162616
-
|
HDAC
Apoptosis
|
Cancer
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
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-
-
- HY-108554
-
|
Protease Activated Receptor (PAR)
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Others
|
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
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-
-
- HY-153606
-
|
Others
|
Cancer
|
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role [1] .
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-
-
- HY-130176
-
|
Opioid Receptor
ERK
Adenylate Cyclase
|
Neurological Disease
|
UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
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-
-
- HY-151379
-
|
Histone Methyltransferase
|
Cancer
|
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
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-
-
- HY-117982
-
|
GnRH Receptor
ERK
|
Endocrinology
|
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
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-
-
- HY-N2484
-
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .
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-
-
- HY-N11439
-
|
CDK
Akt
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Cancer
|
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2 .
|
-
-
- HY-153864
-
|
PROTACs
MEK
ERK
|
Cancer
|
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
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-
-
- HY-126477R
-
|
Endogenous Metabolite
|
Cancer
|
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
|
-
-
- HY-18318
-
|
Raf
VEGFR
PERK
|
Cancer
|
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity .
|
-
-
- HY-N7140
-
γ-Linolenic acid
|
Endogenous Metabolite
Apoptosis
NF-κB
ERK
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases .
|
-
-
- HY-129636A
-
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
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-
-
- HY-116461
-
CID2440433
|
GPR55
|
Neurological Disease
|
ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55 . ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro .
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-
-
- HY-N0774R
-
|
ERK
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
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-
-
- HY-164551
-
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
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-
-
- HY-145384
-
|
Phospholipase
|
Inflammation/Immunology
|
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .
|
-
- HY-12927
-
|
CXCR
|
Inflammation/Immunology
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
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-
- HY-13404
-
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404B
-
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404C
-
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404A
-
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-151431
-
|
Keap1-Nrf2
Reactive Oxygen Species
ERK
Akt
JNK
|
Neurological Disease
|
Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD) .
|
-
- HY-129636
-
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-13404R
-
|
c-Met/HGFR
Apoptosis
|
Cancer
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Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-W744699
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(+)-Larixol
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Src
ERK
Akt
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Inflammation/Immunology
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Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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- HY-W745090
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Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
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Others
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Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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- HY-116504
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Others
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Cancer
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WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
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- HY-162888
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PDGFR
ERK
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Cardiovascular Disease
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WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
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- HY-156041
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Lyso-PE (egg); LPE (egg); L-α-lysophosphatidylethanolamine
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Endogenous Metabolite
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Metabolic Disease
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Lysophosphatidylethanolamine (LPE) is a naturally-occurring lysophospholipid that can be generated via deacylation of phosphatidylethanolamine by phospholipase A2 (PLA2). It increases the phosphorylation of ERK1/2 in PC12 cells, an effect that can be blocked by the MEK inhibitors U-0126 (HY-12031A) and PD 98059 (HY-12028) and the EGFR inhibitor AG-1478 (HY-13524).1 LPE also increases neurite outgrowth and expression of neurofilament M in PC12 cells. LPE inhibits the activity of phospholipase D (PLD) partially purified from cabbage.3 This product contains lysophosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 position and a hydroxy group at the sn-2 position.
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- HY-103211
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Adrenergic Receptor
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Cardiovascular Disease
Metabolic Disease
Cancer
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L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
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- HY-147183
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EGFR
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Cancer
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JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
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- HY-147183A
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EGFR
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Cancer
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JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
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- HY-147183B
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EGFR
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Cancer
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JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
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- HY-N0092R
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Adenosine Receptor
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
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Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR . Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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- HY-N12561
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ERK
p38 MAPK
JNK
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Others
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Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
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- HY-N9541
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Others
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Inflammation/Immunology
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Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
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- HY-N2270
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p38 MAPK
ERK
IKK
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Inflammation/Immunology
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Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
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- HY-101798
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PI3K
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Cancer
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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 .
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- HY-113308
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Others
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Others
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Taurolithocholic acid is a bile acid that has the activity of increasing cell viability, inducing the S phase of the cell cycle, and promoting DNA synthesis in a concentration-dependent manner in the intrahepatic cholangiocarcinoma cell line RMCCA-1. It can also increase the phosphorylation of EGFR and ERK 1/2 and the expression of cyclin D1 in RMCCA-1 cells, and its induced RMCCA-1 cell growth can be inhibited by specific antagonists and inhibitors.
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Cat. No. |
Product Name |
Type |
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- HY-W745090
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Biochemical Assay Reagents
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Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3751
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- HY-P0178A
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Integrin
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Inflammation/Immunology
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LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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- HY-P5977
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Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide
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ERK
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Cancer
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STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
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- HY-P5986
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Peptides
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Others
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mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .
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- HY-P0178
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Integrin
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Inflammation/Immunology
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LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N1987
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-
-
- HY-126477
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-
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- HY-N0774
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-
-
- HY-N2484
-
-
-
- HY-N11439
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-
-
- HY-N7140
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-
-
- HY-N2858
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-
-
- HY-N10047
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-
-
- HY-126477R
-
-
-
- HY-N0774R
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-
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- HY-W744699
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(+)-Larixol
|
Larix decidua Miller
Structural Classification
Natural Products
Pinaceae
Source classification
Plants
|
Src
ERK
Akt
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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-
-
- HY-N0092R
-
|
Structural Classification
Natural Products
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
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Adenosine Receptor
Endogenous Metabolite
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Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR . Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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-
-
- HY-N12561
-
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Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
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ERK
p38 MAPK
JNK
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Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
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-
-
- HY-N9541
-
|
Structural Classification
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source classification
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Others
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
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-
-
- HY-N2270
-
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