||XMD17-109 is a new selective ERK-5 inhibitor (EC50: 4.2 uM, HEK293 cells).
||NVP-231 is a potent, specific and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits ceramide binding to CerK.
||FR180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.
||ISRIB is a potent and selective PERK inhibitor.
||Roscovitine is a potent inhibitor of Cdk2/cyclin E (IC50: 0.1 µM). It also inhibits Cdk7/cyclin H, Cdk5/p35, and Cdc2/cyclin B (IC50s: 0.49/0.16/0.65 µM).
||RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
||BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
||GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.
||Notoginsenoside R1 has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.
||VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
||Galangin is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
||SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and prevents glutamate-induced
||Magnolin reduces the renal oxidative stress, suppresses caspase-3 activity, and increases Bcl-2 expression in vivo and in vitro. Magnolin has anti-inflammatory and antioxidative ef
||Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.
||Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9
||LY-3214996 is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.
||The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. It blocks the production of TNF-α in vitro2 and in vivo, attenuating sign
||SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
||AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
||A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
||ISRIB (trans-isomer), the trans-isomer of ISRIB, is a effective and specific PERK inhibitor (IC50: 5 nM).
||BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.
||GDC-0994 is an effective and orally available ERK1/2 inhibitor (IC50: 1.1/0.3 nM).
||DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ～0.5 μM.
||Pluripotin (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
||Ulixertinib (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.
||1. Dimethylacrylshikonin is a promising agent for developing an improved strategy for radiotherapy against tumors. (a) Injection of Dimethylacrylshikonin combined with IR treatment
||1. Prunetin significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity/adipogenesis ef
||1. Tetrahydrocoptisine has effective effects in suppressing inflammation. 2. Tetrahydrocoptisine possesses a protective effect on LPS-induced ALI through inhibiting of NF-κB signa
||1. Cornuside has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3.
||1. Isofraxidin protects leukemia cells from radiation-induced apoptosis via ROS/mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS
||1. Atractylenolide II has antimelanoma effect by inhibiting STAT3 signalling. 2. Atractylenolide II has cytotoxic/apoptotic effects may via p38 activation , ERK and Akt inactivatio
||1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/A
||1. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. 2. Avicularin inhibits the accumula
||1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful i
||1. Corynoxeine is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation and may be useful in the prevention and treatment of vascular diseases and restenosis after an
||Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and in
||Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
||ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM). It also inhibits LRRK2[G2019S] (IC50: 26 nM).
||ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.
||CAFESTOL is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has stro
||KO-947 is a potent and specific inhibitor of ERK1/2 kinases.
||Mogrol is a biometabolite of mogrosides. Mogrol acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
||Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6/8.8 µM). It also can inhibit ERK2 (IC50: 52 µM).
||Hederacolchiside A1 shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and
||Chrysoeriol has antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities, it also shows selective bronchodilator effect.
||Lupalbigenin sensitizes detachment-induced cell death in human lung cancer cell through down-regulation of pro-survival proteins.
||Pulsatilla saponin D
||Pulsatilla saponin D exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic ag
||Rhamnocitrin can enhance the immune function, improve the formation of spleen cells of mice serum hemolysin of chicken red blood cell immune.
||Xanthyletin has anti-inflammatory, anti-tumor and anti-bacterial activities, it also inhibits symbiotic fungus cultivated by leaf-cutting ants.
||Peonidin chloride has antioxidant activity. Peonidin has show potent inhibitory and apoptotic effects on cancer cells in vitro, notably metastatic human breast cancer cells.
||2-Hydroxy-3-methylanthraquinone enhances apoptosis of U937 cells,in part,through activation of p-p38MAPK and downregulation of p-ERK1/2; triggers caspase-3 activation mediated apop
||Dietary beta-tocopherol and linoleic acid, serum insulin,and waist circumference predict circulating sex hormone-binding globulin in premenopausal women.
||Bufarenogin has inhibitory activity on human kidney Na(+)/K(+)-ATPase, it has cytotoxicity against HepG2 and MCF-7 human cancer cells.
||Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it ca
||(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive
||Isomeranzin has anti-inflammatory activity, it suppresses inflammation by inhibiting M1 macrophage polarization through the p65, NF-κB and ERK pathway.
||Meranzin hydrate exhibits antidepressive and prokinetic-like effects through the regulation of the common mediator, the alpha 2-adrenoceptor , and α±-amino-3-hydroxy-5-methyl-4-i
||Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 pathway. (20Z) -Pseudogi
||Decursinol angelate has anti-tumor, anti-inflammatory, anti-oxidant, and hepatoprotective activities, it inhibits VEGF-induced angiogenesis via suppression of the VEGFR-2-signaling
||Dehydroeffusol possesses anti-cancer, anxiolytic and sedative properties, it may antagonize the spasmogenic activity of various agents, and therefore, could be a promising agent in
||Dihydrorotenone is a potent mitochondrial inhibitor and probably induces Parkinsonian syndrome.
||Fustin shows protective effects on 6-hydroxydopamine-induced neuronal cell death.
||Isocryptotanshinone inhibits protein tyrosine phosphatase 1B (PTP1B) activity with 50% inhibitory concentration values of 56.1±6.3 μM, PTP1B acts as a negative regulator of insul
||Isorhamnetin 3-O-galactoside shows antioxidant, anti-inflammatory, neuroprotective,and barrier protective activities, it could be used as a candidate therapeutic for treatment of s
||Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration o
||Rubrofusarin-6-O-beta-D-gentiobioside can significantly decrease the expression of TGF-beta1 and fibronectin and NF-kappaB DNA binding activity, suggests that it has potential as a
||Rupestonic acid derivatives have an anti-influenza virus activity, they inhibit IAV by up-regulating HO-1-mediated IFN response.
||Saponarin shows in vitro and in vivo hepatoprotective and antioxidant activity against CCl4-induced liver damage.
||MK-2 Inhibitor III
||MK-2 Inhibitor III is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)
||MK-8353 is a potent, selective and orally available inhibitor of ERK1/2 (IC50s of 23.0 nM and 8.8 nM, respectively)
||PERK-IN-2 is a potent inhibitor of PERK(IC50 of 0.2 nM).
||PERK-IN-3 is a potent inhibitor of PERK(IC50 of 7.4 nM).
||AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).
||JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology. JWG-071 improv
||AMG PERK 44
||AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) and induces autophagy. It has 1000-fold and 160-fold selectivity over GCN2 (IC50: 7300 nM) and B-Raf (IC50
||AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1 (example 18; IC50: 0.6 nM).
||ASTX029 is a selective and orally bioavailable extracellular signal-regulated kinases 1 and 2 (ERK 1/2) inhibitor, with potential antineoplastic activity.
||CC-90003 is a selective inhibitor of ERK 1/2 with antitumor activity.
||Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).
||Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver
||Enniatins B decreases the activation of ERK (p44/p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50
||Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.Enniatin B1 is
||ERK-IN-1 is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly relate
||ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.ERK-IN-2 is a potent, highly seletive and orally active ERK2 inhibitor probe with an IC50 valu
||ERK1/2 inhibitor 1
||ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
||ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.
||BAY885 is a new ERK5 inhibitor.
||Pachymic acid is a natural product, and inhibits Akt and ERK signaling pathways.
||Omtriptolide, triptolide purified from the Chinese herb, is a water-soluble derivative prodrug.
||Tauroursodeoxycholate dihydrate is an endoplasmic reticulum stress inhibitor. Tauroursodeoxycholate also inhibits ERK. Tauroursodeoxycholate significantly decreases the expression
||Ilexgenin A is a novel pentacyclic triterpenoid, is a compound extracted from leaves of Ilex hainanensis Merr
||Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part, through downregulat
||Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infection. Ponicidin has an
||Bavachalcone is a major bioactive compounds isolated from Psoralea corylifolia L. it may be useful as a therapeutic drug for bone resorption-associated diseases.Bavachalcone can p
||Vincristine-induced nociceptive painful sensation, may be due to its potential of antioxidative, neuroprotective and calcium channel inhibitory action.Vincristine can treat MM, ERK
||Demethylwedelolactone is a natural product isolated from Eclipta alba, has trypsin inhibitory effect an IC50 of 3.0 μM. it exerts anti-invasive growth effect on breast cancer cel
||Cucurbitacin E is a natural product isolated from the climbing stem of Cucumic melo L. It significantly suppresses the activity of the cyclin B1/CDC2 complex.Cucurbitacin E has pre
||Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to
||Sulforaphene may be a potential anti- triple negative breast cancer natural compound and its /\''antiproliferation effects may be mediated by tumor suppressor Egr1; it has chemothe
||15-Methoxypinusolidic acid has anti-inflammatory effects, it inhibits LPS-induced iNOS expression and NO production, independent on MAPK and NF-kappaB. 15-Methoxypinusolidic acid s
||4,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the treatment of brain diseas
||(E)-4-(3,4-dimethoxyphenyl)but-3-en-1-ol may promote melanin synthesis via USF1 dependent fashion and could be used as a clinical therapeutic agent against hypopigmentation-associa
||4',6,7-Trimethoxyisoflavone promotes wound healing through NOX2 induction, which leads to collective migration and MMP activation.
||5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
||6,4'-Dihydroxy-7-methoxyflavanone has antioxidant, anti-inflammatory and neuroprotective effects. It shows inhibition of osteoclasts differentiation and function, it can be a poten
||6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values
||7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated E
||Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is endowed with estroge
||Bakkenolide IIIa has antioxidant, and neuroprotective effects, it protects against cerebral damage by inhibiting AKT and ERK1/2 activation and inactivated NF-ÎºB signaling.
||(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive mann
||Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin A shows estrogenic activity with ligand-binding activity of estrogen receptor, transcriptional activi
||Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway, and can be furth
||Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1), it selecti
||Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits canc
||Catalposide possesses antioxidant, anti-apoptotic, anti-microbial, anti-tumoral, and anti-inflammatory properties. Catalposide is a potent inducer of HO-1 and HO-1 induction is res
||Cearoin has anti-inflammatory, and antiallergic activities, it can markedly inhibit inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS
||Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC ar
||Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor receptor (EGFR): 1.1 and 4.
||Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neur
||Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tube formation, migrat
||Desoxo-narchinol A exhibits protective effects against LPS-induced endotoxin shock and inflammation through p38 deactivation, it shows inhibitory activity against LPS-induced NO pr
||Ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid has anti-cancer activity, it induces apoptosis of human malignant cancer cells, it also inhibits hepatocellular carcinoma in vitro
||Epieriocalyxin A can suppress Caco-2 colon cancer cell growth, it could be a potential drug for colon cancer therapy in the future.
||Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inh
||Ganoderic acid X
||Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.
||Gardenin A has antihyperlipidemic and hepatoprotective effects , it also promotes neuritogenesis through the activation of MAPK/ERK-, PKC-, and PKA-dependent, but not TrkA-dependen
||Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic
||Haginin A is an effective inhibitor of hyperpigmentation caused by UV irradiation or by pigmented skin disorders through downregulation via ERK and Akt/PKB activation, MITF, and al
||Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid peroxidation.Hirsutenon
||Isochamaejasmine has inhibition of NF-kappaB activation, which could reverse the anti-apoptotic effect; it induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 f
||Kaerophyllin has anti-fibrotic effects, it can protect the rat liver from TAA-caused injury and fibrogenesis by suppressing hepatic inflammation and inhibiting HSC activation, poss
||Lyoniresinol has antioxidant effect, it shows robust anti-melanogenic activity, decreases tyrosinase activity and melanin biosynthesis in B16F10 cells by activating ERK signaling,
||Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associa
||Manassantin B is a potent inhibitor of NF-ÎºB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-ÎºB. It also possesses anti-EBV lytic replicati
||Nyasol may have potential to be developed as medicines for the treatment of allergies by inhibiting the activation of mast cells. Nyasol shows anti-inflammatory properties by inhib
||Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth thro
||Quercetin 3,4'-dimethyl ether
||Quercetin 3,4'-dimethyl ether shows anti-lipid peroxidation activity (IC 50 values of 0.3 uM), it also shows anti-inflammatory activity. Quercetin 3,4'-dimethyl ether could be usef
||Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by
||Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-depe
||Tomatidine shows antibiotic, and anti-inflammatory activities, it significantly suppresses the activity of ACAT and leads to reduction of atherogenesis. Tomatidine inhibits the inv
||Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 +/- 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3
||BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
||Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphoryl
||Trans-Zeatina is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.
||1. Sauchinone is a useful adjunctive treatment for bacterial infection. 2. Sauchinone, an active lignan found in Saururus chinensis, to regulate the activation of HSCs, to prevent
||Sodium Tauroursodeoxycholate (TUDC)
||Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor, used for the treatment of gallstones and liver cirrhosis.
||A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
||Loureirin B can downregulate the expression of fibrosis-related molecules by regulating MMPs and TIMPs levels, inhibit scar fibroblast proliferation and suppress TGF-β1-induced fi