Search Result
Results for "
ERK phosphorylation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P3751
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-
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- HY-114436
-
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Ras
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Cancer
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MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-124097
-
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Insulin Receptor
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Metabolic Disease
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HNMPA-(AM)3 is a cell-permeable and selective insulin receptor tyrosine kinase inhibitor analog of HNMPA. HNMPA-(AM)3 greatly inhibits the ability of prothoracicotropic hormone (PTTH) to activate ERK phosphorylation and stimulate ecdysteroidogenesis. HNMPA-(AM)3 is also effective in inhibiting ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50 is 14.2 μM and 200 μM in mosquitoes and mammals, respectively) .
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- HY-157787
-
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LPL Receptor
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Neurological Disease
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Ginkgolic acid 2-phosphate is a potent sphingosine 1-phosphate agonist. Ginkgolic acid 2-phosphate induces ERK phosphorylation. Ginkgolic acid 2-phosphate interactes with S1P1 .
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- HY-146319
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-
-
- HY-114436S
-
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Isotope-Labeled Compounds
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Cancer
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-113592
-
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ERK
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Cancer
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ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
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- HY-123938
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CYH33
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PI3K
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Cancer
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Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors .
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- HY-123938A
-
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PI3K
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Cancer
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CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors .
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- HY-18849
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ERK
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Cancer
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ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
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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-122246
-
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GPR55
PKC
ERK
Arrestin
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Metabolic Disease
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ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
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-
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- HY-124740
-
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Melanocortin Receptor
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Cancer
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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-N9725
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16ξ-Hydroxycleroda-3,13-dien-15,16-olide
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Dipeptidyl Peptidase
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Metabolic Disease
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16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy .
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- HY-50706
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Selumetinib
Maximum Cited Publications
59 Publications Verification
AZD6244; ARRY-142886
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MEK
Apoptosis
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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-108330
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AG126
2 Publications Verification
Tyrphostin AG126
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ERK
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Inflammation/Immunology
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AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .
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- HY-50706A
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AZD6244 sulfate; ARRY-142886 sulfate
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MEK
Apoptosis
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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-162460
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ERK
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Cancer
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ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1/2 inhibitor (IC50: 0.11/0.08 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-N2858
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Apoptosis
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Cancer
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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-13241
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LY2228820 dimesylate
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p38 MAPK
Autophagy
Apoptosis
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Inflammation/Immunology
Cancer
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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
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Apoptosis
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Inflammation/Immunology
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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-150700
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ERK
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Metabolic Disease
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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 .
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- HY-13241A
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LY2228820
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p38 MAPK
Autophagy
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Inflammation/Immunology
Cancer
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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-12960
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FLT3-IN-1
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FLT3
c-Kit
Apoptosis
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Cancer
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SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
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- HY-153445
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ERK
MEK
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Cancer
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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-76474
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Syk
Apoptosis
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Inflammation/Immunology
Cancer
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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
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Syk
Apoptosis
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Inflammation/Immunology
Cancer
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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-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-N1966
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p38 MAPK
JNK
ERK
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Neurological Disease
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(E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress .
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- HY-147301
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AP1189
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Melanocortin Receptor
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Metabolic Disease
Inflammation/Immunology
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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
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AP1189 acetate
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Melanocortin Receptor
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Metabolic Disease
Inflammation/Immunology
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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
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SHP2
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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-100403
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mGluR
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Cancer
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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-110318
-
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CXCR
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Inflammation/Immunology
Cancer
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VUF11207 fumarate is a CXCR7 agonist that binds specifically to CXCR7. VUF11207 fumarate reduces CXCL12-mediated osteoclastogenesis and bone resorption by inhibiting ERK phosphorylation .
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- HY-107640
-
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MMP
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Cancer
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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-124404A
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ERK
DNA/RNA Synthesis
p38 MAPK
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Cancer
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12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells .
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- HY-113599
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EGFR
ERK
Akt
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Others
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Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .
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- HY-146672
-
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Itk
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Cancer
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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-126477
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NNK
1 Publications Verification
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Endogenous Metabolite
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Cancer
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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-15496
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ER-806201
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MEK
FLT3
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Cancer
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E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
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- HY-P3750
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-
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- HY-163283
-
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Amyloid-β
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Neurological Disease
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6’-Methyl paeonol is a paeonol derivative, which inihibits abnormal depolarizations and reduces the Amyloid β-induced ERK phosphorylation. 6’-Methyl paeonol exhibits alleviating activity against Alzheimer’s Disease .
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- HY-13905
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HHGV678 mesylate
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Bcr-Abl
c-Kit
PDGFR
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Cancer
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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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- HY-16697
-
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GPR55
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Cancer
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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
-
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Integrin
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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
-
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NF-κB
PPAR
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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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-
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- HY-154985
-
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PPAR
Bombesin Receptor
ERK
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Metabolic Disease
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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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-
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- HY-155417
-
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Others
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Neurological Disease
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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-P99183
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EMD 525797; DI17E6
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Integrin
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Cancer
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Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer .
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-
- HY-N0774
-
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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
-
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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-111083
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CID23612552
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GPR55
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Others
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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-147259
-
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c-Met/HGFR
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Cancer
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Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
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- HY-108554
-
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Protease Activated Receptor (PAR)
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Others
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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
-
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Others
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Cancer
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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-N1504
-
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PAI-1
Potassium Channel
ERK
JNK
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Metabolic Disease
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
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- HY-107426
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Muconomycin A
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Apoptosis
Reactive Oxygen Species
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Cancer
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
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- HY-151379
-
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Histone Methyltransferase
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Cancer
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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-149759
-
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SHP2
ERK
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Cancer
|
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM .
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- HY-N1960
-
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Apoptosis
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Inflammation/Immunology
|
Ophiopogonin A is a natural steroid that can be found in Ophiopogon japonicus. Ophiopogonin A dose-dependently inhibits hemorrhagic shock (HS)-induced tissue damage and apoptosis. ophiopogonin A dose-dependently promotes the phosphorylation of ERK in HS kidney tissues and hypoxia-treated HK-2 cells .
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- HY-161145
-
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EGFR
Apoptosis
Microtubule/Tubulin
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Cancer
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EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
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- HY-N2484
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Astrapterocarpan
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PDGFR
ERK
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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
-
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CDK
Akt
ERK
Apoptosis
Bacterial
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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 .
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- HY-153864
-
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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-108559
-
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Prostaglandin Receptor
|
Inflammation/Immunology
|
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
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-
- HY-N0809
-
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p38 MAPK
JNK
Caspase
|
Neurological Disease
Metabolic Disease
|
Sesaminol, isolated from Sesamum indicum, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression .
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- HY-101246
-
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RET
|
Cancer
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
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- HY-149710
-
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ICMT
ERK
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Cancer
|
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation .
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- HY-116461
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CID2440433
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GPR55
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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 .
|
-
- 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-N12561
-
|
ERK
p38 MAPK
JNK
|
Others
|
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 .
|
-
- HY-N2208
-
|
p38 MAPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities .
|
-
- 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 .
|
-
- HY-N6959
-
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
|
Osmundacetone is a natural product isolated from Osmundae Rhizoma, with neuroprotective and anti-apoptotic effects. Osmundacetone also has DPPH scavenging activity and anti-oxidative stress activity. Osmundacetone inhibits MAPK phosphorylation, including JNK, ERK, and p38 kinase. Osmundacetone can be a potential agent for the research of neurodegenerative diseases .
|
-
- HY-108626
-
NCGC84
|
Neuropeptide Y Receptor
|
Neurological Disease
|
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
|
-
- HY-100851A
-
|
5-HT Receptor
|
Cardiovascular Disease
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-110198
-
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
|
-
- HY-157888
-
|
SHP2
Phosphatase
|
Cancer
|
SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .
|
-
- HY-17600
-
ACP-196
|
Btk
|
Cancer
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17600S
-
ACP-196-d4
|
Btk
|
Cancer
|
Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P99768
-
TTAC-0001
|
VEGFR
|
Cancer
|
Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer .
|
-
- 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-156420
-
|
Others
|
Others
|
ATUX-1215 is an activator of protein phosphatase 2A (PP2A). ATUX-1215 reduced the phosphorylation of ERK, p38, JNK, and Akt and the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals. ATUX-1215 can slow the progression of lung fibrosis .
|
-
- 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-104066
-
Xiliertinib; HMPL-309
|
EGFR
|
Cancer
|
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-105226
-
PD134308
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .
|
-
- HY-104066A
-
Xiliertinib tartrate; HMPL-309 tartrate
|
EGFR
|
Cancer
|
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-105226B
-
PD134308 hemihydrate
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects .
|
-
- HY-P99275
-
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-134811
-
|
Ras
|
Cancer
|
KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-134000
-
NSC624610
|
p38 MAPK
NF-κB
ERK
JNK
VEGFR
MMP
|
Cancer
|
Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells .
|
-
- HY-112701
-
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
|
-
- HY-W010983
-
SC-236
1 Publications Verification
|
COX
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model .
|
-
- HY-W744699
-
(+)-Larixol
|
Src
ERK
Akt
|
Inflammation/Immunology
|
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 .
|
-
- HY-W745090
-
|
Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
|
Others
|
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 .
|
-
- HY-N0619
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-118140
-
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
|
-
- HY-103211
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
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 .
|
-
- HY-100035
-
|
ROCK
ERK
CDK
Apoptosis
|
Cancer
|
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
|
-
- HY-143293
-
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer .
|
-
- HY-N0619A
-
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-145491
-
|
ERK
NF-κB
|
Inflammation/Immunology
|
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
|
-
- HY-147183
-
|
EGFR
|
Cancer
|
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 .
|
-
- HY-147183A
-
|
EGFR
|
Cancer
|
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 .
|
-
- HY-147183B
-
|
EGFR
|
Cancer
|
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 .
|
-
- HY-P1844
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-120200
-
|
VEGFR
|
Cardiovascular Disease
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 .
|
-
- HY-150026
-
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-123468
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-128634
-
|
Apoptosis
PI3K
MEK
|
Cancer
|
CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
|
-
- HY-12624
-
ON123300
|
CDK
AMPK
PDGFR
|
Cancer
|
Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
|
-
- HY-P1844A
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-112348
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-134813
-
|
Ras
|
Cancer
|
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-P1845
-
|
ERK
EGFR
Reactive Oxygen Species
Calcium Channel
|
Neurological Disease
|
PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research .
|
-
- HY-109041
-
AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
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- HY-P1845A
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ERK
EGFR
Reactive Oxygen Species
Calcium Channel
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Neurological Disease
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PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research .
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- HY-148098
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Ras
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Cancer
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Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
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- HY-124858
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STAT
JAK
Apoptosis
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Cardiovascular Disease
Cancer
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SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .
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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-P1342
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Peptides
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Neurological Disease
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Prosaptide Tx14(A), a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) increases both ERK1 and ERK2 phosphorylation in Schwann cells .
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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-P1342A
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Peptides
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Neurological Disease
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Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells .
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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-P3750
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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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- 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-P2262
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TDE
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Peptides
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Neurological Disease
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TAT-DEF-Elk-1 (TDE) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity .
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- HY-P1844
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Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
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Inflammation/Immunology
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Chemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism .
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- HY-P1844A
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Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
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Inflammation/Immunology
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Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism .
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- HY-P2262A
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TDE TFA
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Peptides
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Neurological Disease
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TAT-DEF-Elk-1 TFA (TDE TFA) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 TFA blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 TFA is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity .
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- HY-P1845
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ERK
EGFR
Reactive Oxygen Species
Calcium Channel
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Neurological Disease
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PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research .
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- HY-P1845A
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ERK
EGFR
Reactive Oxygen Species
Calcium Channel
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Neurological Disease
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PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99183
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EMD 525797; DI17E6
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Integrin
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Cancer
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Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer .
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- HY-P99768
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TTAC-0001
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VEGFR
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Cancer
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Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer .
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- HY-P99275
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Human Anti-ERBB3 Recombinant Antibody
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EGFR
Akt
ERK
PARP
Survivin
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Cancer
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Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-17600S
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Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-114436S
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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Cat. No. |
Product Name |
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Classification |
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- HY-104066
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Xiliertinib; HMPL-309
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Alkynes
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Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-134811
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Alkynes
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KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-104066A
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Xiliertinib tartrate; HMPL-309 tartrate
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Alkynes
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Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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