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. |
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 . |
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| S1531 |
BIX 02189BIX02189 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. |
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. |
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| 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. |
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. |
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| S7101 |
SCH772984SCH772984 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. |
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.
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| S0911New |
HypaphorineHypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways. |
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| S8569New |
KO-947KO-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. |
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| S1321New |
Urolithin BUrolithin 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. |
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| S0726 |
XMD8-85 (ERK5-IN-1)XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively. |
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| S7921 |
DEL-22379DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM. |
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| S3242 |
Loureirin BLoureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular. |
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| S3901 |
Astragaloside IVAstragaloside 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. |
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| S0949 |
Cucurbitacin IIbCucurbitacin 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. |
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| 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. |
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".
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| 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). |
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| S4884 |
Trans-ZeatinTrans-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. |
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| S8708 |
AZD0364 (ATG-017)AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2. |
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| S4953 |
Usnic acidUsnic 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. |
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| S0872 |
ASTX-029ASTX-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. |
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| S7709 |
VX-11eVX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested. |
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| S3785 |
Notoginsenoside R1Notoginsenoside 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. |
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| S8801 |
CC-90003CC-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. |
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| S6920 |
SEA0400SEA0400 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. |
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| S6882 |
HI-TOPK-032HI-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. |
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| S3292 |
FalcarindiolFalcarindiol (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. |
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| S8896 |
BAY-885BAY-885 is a highly potent and selective ERK5 inhibitor. |
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| S9374 |
2',5'-Dihydroxyacetophenone2',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. |
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| S9075 |
Mulberroside AMulberroside 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. |
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| 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. |
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| S7334 |
ERK5-IN-1ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM. |
The effect of ERK5-IN-1 on botrocetin/VWF-induced human platelet two-wave aggregation.
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| S9102 |
MagnolinMagnolin 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). |
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| S7525 |
XMD8-92XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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). |
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| 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. |
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| 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. |
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| 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. |
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.
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| S3138 |
MethylthiouracilMethylthiouracil (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. |
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| S8831 |
MRTX-1257MRTX-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. |
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| S0454 |
AdjudinAdjudin (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. |
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| S7524 |
FR 180204FR 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. |
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.
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| S6596 |
AG-126AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. |
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| S9306 |
CorynoxeineCorynoxeine, 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. |
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| S6786 |
ERK5-IN-2ERK5-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. |
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| 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. |
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.
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| S1013 |
Bortezomib (PS-341)Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki 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. |
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.
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| S3940 |
3'-Hydroxypterostilbene3'-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. |
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| S3275 |
Senkyunolide ISenkyunolide 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. |
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| S9698 |
EzatiostatEzatiostat (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. |
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| S6760 |
LM22B-10LM22B-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. |
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| E0102New |
I-191I-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. |
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| 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. |
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| S0881 |
Mitochonic acid 5Mitochonic 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. |
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| S3284 |
TrachelosideTracheloside 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. |
| 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. |
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 . |
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| S1531 |
BIX 02189BIX02189 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. |
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. |
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| 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. |
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. |
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| S7101 |
SCH772984SCH772984 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. |
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.
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| S0911New |
HypaphorineHypaphorine which is abundantly found in vaccaria semen, counteracts inflammation via inhibition of ERK or/and NFκB signaling pathways. |
||
| S8569New |
KO-947KO-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. |
||
| S1321New |
Urolithin BUrolithin 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. |
||
| S0726 |
XMD8-85 (ERK5-IN-1)XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively. |
||
| S7921 |
DEL-22379DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM. |
||
| S3242 |
Loureirin BLoureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular. |
||
| S3901 |
Astragaloside IVAstragaloside 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. |
||
| S0949 |
Cucurbitacin IIbCucurbitacin 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. |
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| 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. |
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".
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| 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). |
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| S4884 |
Trans-ZeatinTrans-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. |
||
| S4953 |
Usnic acidUsnic 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-029ASTX-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-11eVX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested. |
||
| S3785 |
Notoginsenoside R1Notoginsenoside 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. |
||
| S8801 |
CC-90003CC-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. |
||
| S6920 |
SEA0400SEA0400 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. |
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| S6882 |
HI-TOPK-032HI-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. |
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| S3292 |
FalcarindiolFalcarindiol (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. |
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| S8896 |
BAY-885BAY-885 is a highly potent and selective ERK5 inhibitor. |
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| S9374 |
2',5'-Dihydroxyacetophenone2',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. |
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| S9075 |
Mulberroside AMulberroside 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. |
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| 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. |
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| S7334 |
ERK5-IN-1ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM. |
The effect of ERK5-IN-1 on botrocetin/VWF-induced human platelet two-wave aggregation.
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| S9102 |
MagnolinMagnolin 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). |
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| S7525 |
XMD8-92XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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). |
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| 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. |
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| 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. |
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| 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. |
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.
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| S3138 |
MethylthiouracilMethylthiouracil (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. |
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| S8831 |
MRTX-1257MRTX-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. |
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| S0454 |
AdjudinAdjudin (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. |
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| S7524 |
FR 180204FR 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. |
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.
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| S6596 |
AG-126AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. |
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| S9306 |
CorynoxeineCorynoxeine, 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. |
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| S6786 |
ERK5-IN-2ERK5-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. |
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| 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. |
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.
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| 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 Ki 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. |
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.
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| S3940 |
3'-Hydroxypterostilbene3'-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. |
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| S3275 |
Senkyunolide ISenkyunolide 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. |
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| S9698 |
EzatiostatEzatiostat (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. |
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| S6760 |
LM22B-10LM22B-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 |
|---|---|---|---|
| E0102New |
I-191I-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. |
| 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. |
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| S0881 |
Mitochonic acid 5Mitochonic 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. |
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| S3284 |
TrachelosideTracheloside 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. |
