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Catalog No.	Product Name	Information	Product Use Citations
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
S0726^New	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.
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.
S0911	Hypaphorine	Hypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways.
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.
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.	Sci Immunol, 2022, 7(68):eabi6763 Sci Adv, 2022, 8(4):eabi7711 Nat Commun, 2022, 13(1):1009
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.	J Immunother Cancer, 2022, 10(1)e003766 Front Oncol, 2022, 12:802482 Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
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.
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.	Cell Stem Cell, 2021, 28(2):257-272.e11 Front Cell Dev Biol, 2021, 9:742049 Cancers (Basel), 2021, 13(6)1205
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.
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 K_ATP current, influx of Ca²⁺ to the intracellular.
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.
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 Pharmacol, 2021, 12:656697
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
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
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.
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.
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
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.
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.
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.
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.	Cancer Res, 2022, canres.1397.2021 Theranostics, 2022, 12(3):1097-1116 J Exp Clin Cancer Res, 2022, 41(1):43
S7334	ERK5-IN-1	ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.	J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096 J Exp Clin Cancer Res, 2020, 12;39(1):50 Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9
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.	Sci Rep, 2022, 12(1):7 Dev Comp Immunol, 2022, 131:104377 Biochim Biophys Acta Mol Cell Res, 2021, 1869(1):119144
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.	Sci Rep, 2022, 12(1):7 Nature, 2021, 595(7869):730-734 Cell Rep, 2021, 37(1):109782
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.	Int J Biol Sci, 2022, 18(5):2047-2059 Cell Biosci, 2022, 12(1):25 Leukemia, 2021, 10.1038/s41375-021-01287-1
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.	Sci Rep, 2022, 12(1):7 ACS Omega, 2022, 7(4):3293-3311 Cell Stem Cell, 2021, 28(2):257-272.e11
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.	Cancer Res, 2022, canres.1397.2021 Cell Rep, 2022, 38(4):110306 PLoS Pathog, 2022, 18(1):e1010253
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
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
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.	Cancer Cell, 2022, S1535-6108(21)00662-0 JCI Insight, 2022, 7(3)e142843 J Mol Med (Berl), 2022, 10.1007/s00109-022-02179-2
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 Front Oncol, 2021, 11:698888
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).	Viruses, 2022, 14(4)805 J Cell Biochem, 2020, 121(1):723-734 Pathol Int, 2020, 70(7):403-412
S8708	AZD0364 (ATG-017)	AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.	Cell Stem Cell, 2021, 28(2):257-272.e11 Antioxidants (Basel), 2020, 9(7)E633 Antioxidants (Basel), 2020, 9(7):633
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
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.
S8896	BAY-885	BAY-885 is a highly potent and selective ERK5 inhibitor.
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.
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.
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
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.
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
S9698	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.
A5018	ERK2 Rabbit Recombinant mAb	ERK2 Rabbit Recombinant mAb detects endogenous levels of total ERK2.
A5036	Phospho-Erk1(T202/Y204)+Erk2 (T185/Y187) Rabbit Recombinant mAb	Phospho-Erk1(T202/Y204)+Erk2 (T185/Y187) Rabbit Recombinant mAb detects endogenous levels of phospho-Erk1(T202/Y204)+Erk2 (T185/Y187).	Biomed Res Int, 2020, 2020:6507510
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
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 Immunopharmacol, 2022, 103:108489 Eur J Neurosci, 2022, 10.1111/ejn.15596 Adv Sci (Weinh), 2021, e2103360
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.	Cell Commun Signal, 2021, 19(1):115
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.
E0102^New	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.
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.
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
S0726^New	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.
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.
S0911	Hypaphorine	Hypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways.
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.
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.	Sci Immunol, 2022, 7(68):eabi6763 Sci Adv, 2022, 8(4):eabi7711 Nat Commun, 2022, 13(1):1009
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.	J Immunother Cancer, 2022, 10(1)e003766 Front Oncol, 2022, 12:802482 Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
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.
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.	Cell Stem Cell, 2021, 28(2):257-272.e11 Front Cell Dev Biol, 2021, 9:742049 Cancers (Basel), 2021, 13(6)1205
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.
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 K_ATP current, influx of Ca²⁺ to the intracellular.
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.
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 Pharmacol, 2021, 12:656697
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
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
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.
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.
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
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.
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.
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.
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.	Cancer Res, 2022, canres.1397.2021 Theranostics, 2022, 12(3):1097-1116 J Exp Clin Cancer Res, 2022, 41(1):43
S7334	ERK5-IN-1	ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.	J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096 J Exp Clin Cancer Res, 2020, 12;39(1):50 Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9
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.	Sci Rep, 2022, 12(1):7 Dev Comp Immunol, 2022, 131:104377 Biochim Biophys Acta Mol Cell Res, 2021, 1869(1):119144
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.	Sci Rep, 2022, 12(1):7 Nature, 2021, 595(7869):730-734 Cell Rep, 2021, 37(1):109782
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.	Int J Biol Sci, 2022, 18(5):2047-2059 Cell Biosci, 2022, 12(1):25 Leukemia, 2021, 10.1038/s41375-021-01287-1
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.	Sci Rep, 2022, 12(1):7 ACS Omega, 2022, 7(4):3293-3311 Cell Stem Cell, 2021, 28(2):257-272.e11
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.	Cancer Res, 2022, canres.1397.2021 Cell Rep, 2022, 38(4):110306 PLoS Pathog, 2022, 18(1):e1010253
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
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
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.	Cancer Cell, 2022, S1535-6108(21)00662-0 JCI Insight, 2022, 7(3)e142843 J Mol Med (Berl), 2022, 10.1007/s00109-022-02179-2
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 Front Oncol, 2021, 11:698888
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).	Viruses, 2022, 14(4)805 J Cell Biochem, 2020, 121(1):723-734 Pathol Int, 2020, 70(7):403-412
S8708	AZD0364 (ATG-017)	AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.	Cell Stem Cell, 2021, 28(2):257-272.e11 Antioxidants (Basel), 2020, 9(7)E633 Antioxidants (Basel), 2020, 9(7):633
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
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.
S8896	BAY-885	BAY-885 is a highly potent and selective ERK5 inhibitor.
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.
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.
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
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.
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
S9698	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.
A5018	ERK2 Rabbit Recombinant mAb	ERK2 Rabbit Recombinant mAb detects endogenous levels of total ERK2.
A5036	Phospho-Erk1(T202/Y204)+Erk2 (T185/Y187) Rabbit Recombinant mAb	Phospho-Erk1(T202/Y204)+Erk2 (T185/Y187) Rabbit Recombinant mAb detects endogenous levels of phospho-Erk1(T202/Y204)+Erk2 (T185/Y187).	Biomed Res Int, 2020, 2020:6507510
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
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 Immunopharmacol, 2022, 103:108489 Eur J Neurosci, 2022, 10.1111/ejn.15596 Adv Sci (Weinh), 2021, e2103360
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.	Cell Commun Signal, 2021, 19(1):115
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.
E0102^New	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.
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.
S0726^New	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.
E0102^New	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.