ERK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

ERK Products

Catalog No.	Information	Product Use Citations	Product Validations
S1014	Bosutinib (SKI-606) Bosutinib (SKI-606) 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.	Br J Anaesth, 2021, S0007-0912(21)00090-8 EBioMedicine, 2021, 69:103457 Cell Chem Biol, 2021, S2451-9456(21)00303-2	A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .
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.	Cancers (Basel), 2021, 13(6)1205 Nat Commun, 2020, 11(1):1383 J Biol Chem, 2020, 295(3):673-689	Expression of iNOS, Fra-1, Fra-2, JunB, JunD, and FosB in PMN. (A) PMN were treated with or without SB203580 (40 μM), BIX02189 (30 μM), or SP600125 (40 μM) for 1 h before addition of NDMA (0.74 μg/μl). The cytoplasmic and nuclear fractions obtained from the cells were used to detect iNOS, Fra-1, Fra-2, JunB, JunD, and FosB protein levels by Western blot. The results shown are representative of five independent experiments.
S1396	Resveratrol (SRT501) Resveratrol (SRT501, trans-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.	Int J Mol Sci, 2021, 22(5)2354 Phytomedicine, 2021, 89:153601 Acta Biochim Biophys Sin (Shanghai), 2021, gmab042	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
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.	J Extracell Vesicles, 2021, 10(8):e12091 Proc Natl Acad Sci U S A, 2021, 118(24)e2025030118 Leukemia, 2021, 10.1038/s41375-021-01287-1	K562 cells were exposed to ERK inhibitor SCH772984 (1 uM, 2 uM, 5 uM) for 48 h. Apoptosis was analyzed by Annexin V-APC labeling.
S0911^New	Hypaphorine Hypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways.
S8569^New	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.	Front Oncol, 2021, 11:698888
S1321^New	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.
S6920^New	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.
S3242^New	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 K_ATP current, influx of Ca²⁺ to the intracellular.
S9698^New	Ezatiostat Ezatiostat (TER199, TLK199, Telintra), 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.
S3284^New	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.
S8831^New	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.
S3292^New	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. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.	Front Pharmacol, 2021, 12:656697
S6882^New	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.
S7921	DEL-22379 DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.	Cell Mol Bioeng, 2018, 11(6):451-469
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.	Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
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.
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.	Mol Cell, 2020, 80(6):1104-1122.e9 ACS Chem Biol, 2019, 14(5):1020-1029 Eur J Pharmacol, 2019, 857:172423	Established HCC cell lines, HepG2 (A-C) and Huh-7 (D), primary human HCC cells (D, "Pri_1/Pri _2"), as well as HL-7702 human hepatocytes (D) and primary human adult hepatocytes ("Hepatocytes", D), were either left untreated ("C", same for all figures), or treated with applied concentration of TIC10 (0.1-30 μM), cells were then cultured in conditional medium for applied time; Cell proliferation was tested by MTT assay (A and D), clonogenicity assay (B) and [H3] Thymidine incorporation assay (C). Experiments in this figure were repeated for five times, with similar results obtained. n = 5 for each repeat. Bars stand for mean ± SD. *p < 0.05 vs. group "C".
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 Cell Biochem, 2020, 121(1):723-734 Pathol Int, 2020, 70(7):403-412
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.
S8708	AZD0364 (ATG-017) AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.	Antioxidants (Basel), 2020, 9(7)E633 Antioxidants (Basel), 2020, 9(7):633
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.
S7709	VX-11e VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK2 inhibitor with K_i of <2 nM, over 200-fold selective over other kinases tested.	Cancers (Basel), 2020, 27;12(5)pii: E1087 Cancer Genomics Proteomics, 2020, 17(5):517-527 Nat Genet, 2019, 51(2):207-216
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.
S8896	BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor.
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
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.
S7334	ERK5-IN-1 ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.	J Exp Clin Cancer Res, 2020, 12;39(1):50 Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9 Biomed Res, 2020, 41(3):119-129	The effect of ERK5-IN-1 on botrocetin/VWF-induced human platelet two-wave aggregation.
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).	Connect Tissue Res, 2020, 1-10 Chem Pharm Bull (Tokyo), 2020, 68(5):421-427
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 K_d of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.	Onco Targets Ther, 2020, 13:9689-9700 Med Sci Monit, 2020, 26:e918370 Life Sci, 2020, 241:117150	The mRNA level of DCLK1 after MET or ERK5 inhibition in mesothelioma cells. The mRNA level of DCLK1 in (A) H290 and (B) H513 cells treated with MET inhibitor XL184 or ERK5 inhibitor XMD8-92 measured using quantitative real-time PCR (*P<0.0001, one-way ANOVA and Scheffe multiple comparisons).
S8534	LY3214996 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.	Cell Rep, 2021, 35(11):109235 Cancer Lett, 2021, 510:37-47 Cancers (Basel), 2021, 13(2)E199
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
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.	Sci Rep, 2021, 11(1):11234 EMBO Rep, 2020, e48686 Mol Cancer, 2020, 19(1):139	Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (ulixerinib, GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.
S3138	Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
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.
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.	Front Pharmacol, 2021, 12:625289 Oncol Rep, 2021, 46(1)120 Theranostics, 2020, 16;10(14):6448-6466	ERK1/2 inhibition reverse EMT in H1299- EML4-ALK cells. H1299-EML4-ALK cells were treated with FR180204 (10 μM), crizotinib (10 nM) and S3I-201(20 μM) for 24 h, cell extracts were analyzed by immunoblotting.
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
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.
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.
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.	Leukemia, 2021, 10.1038/s41375-021-01287-1 Cell Rep, 2021, 35(11):109233 Cell Death Dis, 2021, 12(1):85	Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.
S1013	Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with K_i of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.	Nature, 2021, 10.1038/s41586-020-03118-2 Sci Adv, 2021, 7(23)eabg2697 Sci Adv, 2021, 7(3)eabc6364	Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
S3275^New	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.
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. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
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.
S9665^New	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.
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.
S0881	Mitochonic acid 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.	Neural Regen Res, 2021, 16(9):1813-1820 Neural Regen Res, 2021, 16(9):1813-1820 Cell Mol Biol Lett, 2018, 23:14

Catalog No.	Information	Product Use Citations	Product Validations
S1014	Bosutinib (SKI-606) Bosutinib (SKI-606) 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.	Br J Anaesth, 2021, S0007-0912(21)00090-8 EBioMedicine, 2021, 69:103457 Cell Chem Biol, 2021, S2451-9456(21)00303-2	A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .
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.	Cancers (Basel), 2021, 13(6)1205 Nat Commun, 2020, 11(1):1383 J Biol Chem, 2020, 295(3):673-689	Expression of iNOS, Fra-1, Fra-2, JunB, JunD, and FosB in PMN. (A) PMN were treated with or without SB203580 (40 μM), BIX02189 (30 μM), or SP600125 (40 μM) for 1 h before addition of NDMA (0.74 μg/μl). The cytoplasmic and nuclear fractions obtained from the cells were used to detect iNOS, Fra-1, Fra-2, JunB, JunD, and FosB protein levels by Western blot. The results shown are representative of five independent experiments.
S1396	Resveratrol (SRT501) Resveratrol (SRT501, trans-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.	Int J Mol Sci, 2021, 22(5)2354 Phytomedicine, 2021, 89:153601 Acta Biochim Biophys Sin (Shanghai), 2021, gmab042	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
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.	J Extracell Vesicles, 2021, 10(8):e12091 Proc Natl Acad Sci U S A, 2021, 118(24)e2025030118 Leukemia, 2021, 10.1038/s41375-021-01287-1	K562 cells were exposed to ERK inhibitor SCH772984 (1 uM, 2 uM, 5 uM) for 48 h. Apoptosis was analyzed by Annexin V-APC labeling.
S0911^New	Hypaphorine Hypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways.
S8569^New	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.	Front Oncol, 2021, 11:698888
S1321^New	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.
S6920^New	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.
S3242^New	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 K_ATP current, influx of Ca²⁺ to the intracellular.
S9698^New	Ezatiostat Ezatiostat (TER199, TLK199, Telintra), 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.
S3284^New	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.
S8831^New	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.
S3292^New	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. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.	Front Pharmacol, 2021, 12:656697
S6882^New	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.
S7921	DEL-22379 DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.	Cell Mol Bioeng, 2018, 11(6):451-469
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.	Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
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.
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.	Mol Cell, 2020, 80(6):1104-1122.e9 ACS Chem Biol, 2019, 14(5):1020-1029 Eur J Pharmacol, 2019, 857:172423	Established HCC cell lines, HepG2 (A-C) and Huh-7 (D), primary human HCC cells (D, "Pri_1/Pri _2"), as well as HL-7702 human hepatocytes (D) and primary human adult hepatocytes ("Hepatocytes", D), were either left untreated ("C", same for all figures), or treated with applied concentration of TIC10 (0.1-30 μM), cells were then cultured in conditional medium for applied time; Cell proliferation was tested by MTT assay (A and D), clonogenicity assay (B) and [H3] Thymidine incorporation assay (C). Experiments in this figure were repeated for five times, with similar results obtained. n = 5 for each repeat. Bars stand for mean ± SD. *p < 0.05 vs. group "C".
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 Cell Biochem, 2020, 121(1):723-734 Pathol Int, 2020, 70(7):403-412
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.
S8708	AZD0364 (ATG-017) AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.	Antioxidants (Basel), 2020, 9(7)E633 Antioxidants (Basel), 2020, 9(7):633
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.
S7709	VX-11e VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK2 inhibitor with K_i of <2 nM, over 200-fold selective over other kinases tested.	Cancers (Basel), 2020, 27;12(5)pii: E1087 Cancer Genomics Proteomics, 2020, 17(5):517-527 Nat Genet, 2019, 51(2):207-216
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.
S8896	BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor.
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
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.
S7334	ERK5-IN-1 ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.	J Exp Clin Cancer Res, 2020, 12;39(1):50 Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9 Biomed Res, 2020, 41(3):119-129	The effect of ERK5-IN-1 on botrocetin/VWF-induced human platelet two-wave aggregation.
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).	Connect Tissue Res, 2020, 1-10 Chem Pharm Bull (Tokyo), 2020, 68(5):421-427
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 K_d of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.	Onco Targets Ther, 2020, 13:9689-9700 Med Sci Monit, 2020, 26:e918370 Life Sci, 2020, 241:117150	The mRNA level of DCLK1 after MET or ERK5 inhibition in mesothelioma cells. The mRNA level of DCLK1 in (A) H290 and (B) H513 cells treated with MET inhibitor XL184 or ERK5 inhibitor XMD8-92 measured using quantitative real-time PCR (*P<0.0001, one-way ANOVA and Scheffe multiple comparisons).
S8534	LY3214996 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.	Cell Rep, 2021, 35(11):109235 Cancer Lett, 2021, 510:37-47 Cancers (Basel), 2021, 13(2)E199
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
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.	Sci Rep, 2021, 11(1):11234 EMBO Rep, 2020, e48686 Mol Cancer, 2020, 19(1):139	Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (ulixerinib, GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.
S3138	Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378) is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
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.
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.	Front Pharmacol, 2021, 12:625289 Oncol Rep, 2021, 46(1)120 Theranostics, 2020, 16;10(14):6448-6466	ERK1/2 inhibition reverse EMT in H1299- EML4-ALK cells. H1299-EML4-ALK cells were treated with FR180204 (10 μM), crizotinib (10 nM) and S3I-201(20 μM) for 24 h, cell extracts were analyzed by immunoblotting.
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
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.
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.
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.	Leukemia, 2021, 10.1038/s41375-021-01287-1 Cell Rep, 2021, 35(11):109233 Cell Death Dis, 2021, 12(1):85	Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.

Catalog No.	Information	Product Use Citations	Product Validations
S1013	Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with K_i of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.	Nature, 2021, 10.1038/s41586-020-03118-2 Sci Adv, 2021, 7(23)eabg2697 Sci Adv, 2021, 7(3)eabc6364	Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
S3275^New	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.
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. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
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.

Catalog No.	Information	Product Use Citations	Product Validations
S9665^New	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.

Catalog No.

Information

Product Use Citations

Product Validations

S9665^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
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.
S0881	Mitochonic acid 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.	Neural Regen Res, 2021, 16(9):1813-1820 Neural Regen Res, 2021, 16(9):1813-1820 Cell Mol Biol Lett, 2018, 23:14

Catalog No.

Information

Product Use Citations

Product Validations

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.

S0881

Mitochonic acid 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.

Neural Regen Res, 2021, 16(9):1813-1820

Cell Mol Biol Lett, 2018, 23:14

Choose Your Country or Region

By Signaling Pathways

By product type

ERK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

ERK Products