ERK

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ERKシグナル伝達経路

ERK製品

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S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
S7101 SCH772984 SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
Nat Commun, 2024, 15(1):383
Cell Rep Med, 2024, 5(2):101420
Theranostics, 2024, 14(4):1561-1582
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
S1531 BIX 02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Exp Mol Med, 2023, 55(6):1247-1257
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S7554 Ravoxertinib (GDC-0994) Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
EMBO J, 2023, e114153.
Pharmacol Res, 2023, 197:106955
Mol Cancer Ther, 2023, 22(2):227-239
S7854 Ulixertinib (BVD-523) Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Mol Cancer, 2023, 10.1186/s12943-023-01868-x
ACS Cent Sci, 2023, 9(4):719-732
Cancer Res, 2023, 83(2):316-331
S8534 Temuterkib (LY3214996) Temuterkib (LY3214996) is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
Nat Commun, 2024, 15(1):1300
Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
Wiley Online Library, 2024, 10.1002/pgr2.15
S7524 FR 180204 FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.
Int J Mol Sci, 2023, 24(7)6228
Biochem J, 2023, 480(9):587-605
bioRxiv, 2023, 2023.01.19.524758
S7525 XMD8-92 XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Cell Death Dis, 2023, 14(1):32
Cell Death Dis, 2023, 14(1):32
S7709 VX-11e VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK inhibitor with IC50 of 17 nM (ERK1) and 15 nM (ERK2), over 200-fold selective over other kinases tested.
Int J Biol Sci, 2024, 20(2):569-584
PLoS One, 2024, 19(1):e0295629
ACS Cent Sci, 2023, 9(4):719-732
S7963 TIC10 (ONC201) TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
Elife, 2023, 12e85898
J Biol Chem, 2023, S0021-9258(23)02442-0
Neoplasia, 2023, 39:100894
S8708 AZD0364 (ATG-017) AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
Cells, 2023, 12(12)1624
Commun Biol, 2023, 6(1):872
Commun Biol, 2023, 6(1):872
S7334 ERK5-IN-1 ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.
Nat Commun, 2023, 14(1):3364
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
J Exp Clin Cancer Res, 2020, 12;39(1):50
S8701 MK-8353 (SCH900353) MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).
J Exp Clin Cancer Res, 2023, 42(1):75
Life Sci Alliance, 2023, 6(8)e202201685
Viruses, 2022, 14(4)805
S7921 DEL-22379 DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
Cells, 2022, 11(3)425
Cells, 2022, 11(3)425
Front Mol Biosci, 2022, 9:1030725
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
S8569 KO-947 KO-947 is a potent and selective inhibitor of ERK1/2 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations.
Phytomedicine, 2022, 98:153963
CNS Neurosci Ther, 2022, 10.1111/cns.13945
Front Endocrinol (Lausanne), 2022, 13:896753
S9102 Magnolin Magnolin is a natural compound abundantly found in Magnolia flos targeting ERK1 (IC50=87 nM) and ERK2 (IC50=16.5 nM) and inhibits cell transformation induced by tumor promoters such as epidermal growth factor (EGF).
Cell Rep, 2023, 42(4):112294
Cell Adhesion & Migration, 2023, 17(1)
Connect Tissue Res, 2020, 1-10
S0881 Mitochonic acid 5 (MA-5) Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Animals (Basel), 2024, 14(3):368.
J Ovarian Res, 2022, 15(1):103
Neural Regen Res, 2021, 16(9):1813-1820
S3275 Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
SSRN , 2024, 10.2139/ssrn.4696834
Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
Cell Commun Signal, 2021, 19(1):115
S3292 Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S7752 Pluripotin (SC1) Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Pluripotin also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively.
Antiviral Res, 2018, 157:57-67
Reprod Domest Anim, 2018, 53(5):1052-1059
E2203 DMU-212 DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.
Blood Sci, 2023, 5(3):160-169
S3785 Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S8801 CC-90003 CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.
Cell Death Discov, 2021, 7(1):375
S8896 BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor.
Bioengineered, 2022, 13(5):12888-12898
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
Pathol Oncol Res, 2019, 25(1):301-309
S0454 Adjudin Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation.
Brain Res Bull, 2022, 182:80-89
S6596 AG-126 AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.
J Immunol, 2019, 203(12):3225-3236
S3940 3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S0911 Hypaphorine Hypaphorine, an indole alkaloid isolated from Pisolithus tinctorius, exhibits neurological and glucose-lowering effects in rodents.
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S0726 XMD8-85 (ERK5-IN-1) XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S9975 ASN007 ASN007(ERAS 007, ERK-IN-3) is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with 2 nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S4884 Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S4953 Usnic acid Usnic acid (Usniacin) is a furandione found uniquely in lichen that is used widely in cosmetics, deodorants, toothpaste and medicinal creams as well as some herbal products. It exhibits antiviral, antiprotozoal, antiproliferative, anti-inflammatory and analgesic activity. Usnic acid inhibits breast tumor angiogenesis and growth by suppressing VEGFR2-mediated AKT and ERK1/2 signaling pathways.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
S0872 ASTX-029 ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S6760 LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
Theranostics, 2024, 14(4):1561-1582
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E0102 I-191 I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
S0844 NDMC101 NDMC101 inhibits osteoclastogenesis which also ameliorates paw swelling and inflammatory bone destruction, associating with the inhibition of such transcription factors as NF-κB and NFATc1 as well as multiple protein kinases, including p38, ERK, and JNK.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. 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.
S9665 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S6177 CP 43 Cp 43 (Compound 43, TAO Kinase inhibitor 1, TAOK inhibitor 43) is a ATP-competitive and selective TAO Kinase inhibitor with IC50s of 11 nM and 15 nM for TAOK1 and TAOK2, respectively.
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378,MTU) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
S8831 MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.
S9306 Corynoxeine Corynoxeine, which could be isolated from Uncaria rhynchophylla, is a useful and prospective compound in the prevention and treatment for vascular diseases. It is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation.
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S6786 ERK5-IN-2 ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 of 0.82 μM and 3 μM for ERK5 and ERK5 MEF2D, respectively.
S3284 Tracheloside Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. Tracheloside significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation.
E2203 DMU-212 DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.
Blood Sci, 2023, 5(3):160-169
S7101 SCH772984 SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
Nat Commun, 2024, 15(1):383
Cell Rep Med, 2024, 5(2):101420
Theranostics, 2024, 14(4):1561-1582
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
S1531 BIX 02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Exp Mol Med, 2023, 55(6):1247-1257
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S7554 Ravoxertinib (GDC-0994) Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
EMBO J, 2023, e114153.
Pharmacol Res, 2023, 197:106955
Mol Cancer Ther, 2023, 22(2):227-239
S7854 Ulixertinib (BVD-523) Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Mol Cancer, 2023, 10.1186/s12943-023-01868-x
ACS Cent Sci, 2023, 9(4):719-732
Cancer Res, 2023, 83(2):316-331
S8534 Temuterkib (LY3214996) Temuterkib (LY3214996) is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
Nat Commun, 2024, 15(1):1300
Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
Wiley Online Library, 2024, 10.1002/pgr2.15
S7524 FR 180204 FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.
Int J Mol Sci, 2023, 24(7)6228
Biochem J, 2023, 480(9):587-605
bioRxiv, 2023, 2023.01.19.524758
S7525 XMD8-92 XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Cell Death Dis, 2023, 14(1):32
Cell Death Dis, 2023, 14(1):32
S7709 VX-11e VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK inhibitor with IC50 of 17 nM (ERK1) and 15 nM (ERK2), over 200-fold selective over other kinases tested.
Int J Biol Sci, 2024, 20(2):569-584
PLoS One, 2024, 19(1):e0295629
ACS Cent Sci, 2023, 9(4):719-732
S7963 TIC10 (ONC201) TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
Elife, 2023, 12e85898
J Biol Chem, 2023, S0021-9258(23)02442-0
Neoplasia, 2023, 39:100894
S8708 AZD0364 (ATG-017) AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
Cells, 2023, 12(12)1624
Commun Biol, 2023, 6(1):872
Commun Biol, 2023, 6(1):872
S7334 ERK5-IN-1 ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.
Nat Commun, 2023, 14(1):3364
J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096
J Exp Clin Cancer Res, 2020, 12;39(1):50
S8701 MK-8353 (SCH900353) MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).
J Exp Clin Cancer Res, 2023, 42(1):75
Life Sci Alliance, 2023, 6(8)e202201685
Viruses, 2022, 14(4)805
S7921 DEL-22379 DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
Cells, 2022, 11(3)425
Cells, 2022, 11(3)425
Front Mol Biosci, 2022, 9:1030725
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
S8569 KO-947 KO-947 is a potent and selective inhibitor of ERK1/2 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations.
Phytomedicine, 2022, 98:153963
CNS Neurosci Ther, 2022, 10.1111/cns.13945
Front Endocrinol (Lausanne), 2022, 13:896753
S9102 Magnolin Magnolin is a natural compound abundantly found in Magnolia flos targeting ERK1 (IC50=87 nM) and ERK2 (IC50=16.5 nM) and inhibits cell transformation induced by tumor promoters such as epidermal growth factor (EGF).
Cell Rep, 2023, 42(4):112294
Cell Adhesion & Migration, 2023, 17(1)
Connect Tissue Res, 2020, 1-10
S3292 Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Pharmacol, 2021, 12:656697
S7752 Pluripotin (SC1) Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Pluripotin also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively.
Antiviral Res, 2018, 157:57-67
Reprod Domest Anim, 2018, 53(5):1052-1059
S3785 Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S8801 CC-90003 CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.
Cell Death Discov, 2021, 7(1):375
S8896 BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor.
Bioengineered, 2022, 13(5):12888-12898
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
Pathol Oncol Res, 2019, 25(1):301-309
S0454 Adjudin Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation.
Brain Res Bull, 2022, 182:80-89
S6596 AG-126 AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.
J Immunol, 2019, 203(12):3225-3236
S0911 Hypaphorine Hypaphorine, an indole alkaloid isolated from Pisolithus tinctorius, exhibits neurological and glucose-lowering effects in rodents.
S0726 XMD8-85 (ERK5-IN-1) XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.
S3242 Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.
S9975 ASN007 ASN007(ERAS 007, ERK-IN-3) is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with 2 nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S4884 Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S4953 Usnic acid Usnic acid (Usniacin) is a furandione found uniquely in lichen that is used widely in cosmetics, deodorants, toothpaste and medicinal creams as well as some herbal products. It exhibits antiviral, antiprotozoal, antiproliferative, anti-inflammatory and analgesic activity. Usnic acid inhibits breast tumor angiogenesis and growth by suppressing VEGFR2-mediated AKT and ERK1/2 signaling pathways.
S0872 ASTX-029 ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
E0102 I-191 I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
S9075 Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. 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.
S9665 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S6177 CP 43 Cp 43 (Compound 43, TAO Kinase inhibitor 1, TAOK inhibitor 43) is a ATP-competitive and selective TAO Kinase inhibitor with IC50s of 11 nM and 15 nM for TAOK1 and TAOK2, respectively.
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378,MTU) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
S8831 MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
S9306 Corynoxeine Corynoxeine, which could be isolated from Uncaria rhynchophylla, is a useful and prospective compound in the prevention and treatment for vascular diseases. It is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation.
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S6786 ERK5-IN-2 ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 of 0.82 μM and 3 μM for ERK5 and ERK5 MEF2D, respectively.
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
S3275 Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
SSRN , 2024, 10.2139/ssrn.4696834
Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
Cell Commun Signal, 2021, 19(1):115
S3940 3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
S6760 LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
Theranostics, 2024, 14(4):1561-1582
E2660 Pamoic acid disodium Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.
E2203 DMU-212 DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.
Blood Sci, 2023, 5(3):160-169
S0881 Mitochonic acid 5 (MA-5) Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Animals (Basel), 2024, 14(3):368.
J Ovarian Res, 2022, 15(1):103
Neural Regen Res, 2021, 16(9):1813-1820
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S3284 Tracheloside Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. Tracheloside significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation.

ERK阻害剤の選択性比較

Tags: ERK inhibitor|ERK agonist|ERK activator|ERK inducer|ERK antagonist|ERK signaling pathway|ERK assay kit