Search Result

Pathways Recommended:	MAPK/ERK Pathway

Results for "

ERK Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ERK (143) 5-HT Receptor (1) Acyltransferase (2) Akt (12) AMPK (1) AP-1 (1) Apoptosis (69) Arginase (1) Arrestin (1) Aryl Hydrocarbon Receptor (2) Autophagy (14) Bacterial (2) Bcr-Abl (1) Beta-secretase (2) Bombesin Receptor (1) c-Kit (3) c-Met/HGFR (5) Calcium Channel (1) Cannabinoid Receptor (1) Casein Kinase (2) Caspase (10) CCR (1) CDK (5) Chloride Channel (1) Cholinesterase (ChE) (2) COX (6) CXCR (1) Cyclic GMP-AMP Synthase (1) Cytochrome P450 (1) Dengue virus (1) Dipeptidyl Peptidase (1) Drug Metabolite (1) DYRK (1) E1/E2/E3 Enzyme (1) EBV (1) EGFR (12) Endogenous Metabolite (14) Epigenetic Reader Domain (2) FAK (2) Farnesyl Transferase (1) FGFR (2) Flavivirus (1) FLT3 (6) Formyl Peptide Receptor (FPR) (1) Fungal (1) GnRH Receptor (1) GPR55 (3) GSK-3 (5) HDAC (2) HIF/HIF Prolyl-Hydroxylase (1) Histone Methyltransferase (1) HSP (2) HSV (1) ICMT (1) IKK (1) Insulin Receptor (2) Integrin (2) Interleukin Related (6) Isotope-Labeled Compounds (6) Itk (1) JAK (2) JNK (9) Macrophage migration inhibitory factor (MIF) (1) MAPKAPK2 (MK2) (2) MEK (27) Melanocortin Receptor (1) MicroRNA (1) Microtubule/Tubulin (3) MMP (4) MNK (1) Neuropeptide Y Receptor (1) NF-κB (22) NO Synthase (1) Organoid (3) p38 MAPK (14) PAI-1 (1) PAK (1) Parasite (1) PARP (1) PDGFR (5) PERK (6) PGE synthase (1) Phosphatase (8) Phosphodiesterase (PDE) (2) Phospholipase (2) PI3K (5) Pim (1) PKA (1) PKC (2) Potassium Channel (4) PPAR (2) Prostaglandin Receptor (1) PROTACs (2) Raf (3) RANKL/RANK (1) RAR/RXR (1) Ras (21) Reactive Oxygen Species (4) RET (1) Ribosomal S6 Kinase (RSK) (1) ROCK (1) SHP2 (7) Sirtuin (1) Sodium Channel (9) SphK (2) Src (4) STAT (4) Survivin (1) Syk (4) TAM Receptor (1) TGF-beta/Smad (1) Tie (1) TNF Receptor (4) Toll-like Receptor (TLR) (1) Topoisomerase (1) Trk Receptor (1) TrxR (1) Tyrosinase (2) VEGFR (6) Wnt (3) β-catenin (3)
By Research Areas:	Cancer (211) Cardiovascular Disease (25) Endocrinology (1) Infection (6) Inflammation/Immunology (57) Metabolic Disease (18) Neurological Disease (14)
Click Chemistry:	Alkynes (1)

287

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

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Inhibitory Antibodies

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Click Chemistry

Targets Recommended: ERK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153738

ERK1/2 inhibitor 9	ERK	Cancer
ERK1/2 inhibitor 9 (Probe 1) is a covalent *ERK1/2* inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .

HY-112287

ERK1/2 inhibitor 1 4 Publications Verification	ERK	Cancer
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 .

HY-142433

ERK1/2 inhibitor 7

ERK Cancer

ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC₅₀ of 0.94 nM for ERK2 (WO2021110168A1, WX006) .

ERK1/2 inhibitor 7	ERK	Cancer
ERK1/2 inhibitor 7 is a potent *ERK* inhibitor with an IC₅₀ of 0.94 nM for ERK2 (WO2021110168A1, WX006) .

HY-112469

ERK Inhibitor II (Negative control)	ERK Insulin Receptor	Metabolic Disease
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes .

HY-162460

ERK1/2 inhibitor 10	ERK	Cancer
ERK1/2 inhibitor 10 (Compound 36c) is a potent *ERK1/2* inhibitor (IC₅₀: 0.11/0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .

HY-142437

ERK1/2 inhibitor 8

ERK Cancer

ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC₅₀ of 0.48 nM for ERK2 (WO2021110168A1, WX007) .

ERK1/2 inhibitor 8	ERK	Cancer
ERK1/2 inhibitor 8 is a potent *ERK* inhibitor with an IC₅₀ of 0.48 nM for ERK2 (WO2021110168A1, WX007) .

HY-145026

ERK1/2 inhibitor 4	ERK	Inflammation/Immunology Cancer
ERK1/2 inhibitor 5 is a potent inhibitor of *ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor* 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .

HY-145027

ERK1/2 inhibitor 5	ERK	Cancer
ERK1/2 inhibitor 5 is a potent inhibitor of *ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor* 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .

HY-145025

ERK1/2 inhibitor 3	ERK	Inflammation/Immunology Cancer
ERK1/2 inhibitor 3 is a potent inhibitor of *ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor* 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .

HY-145028

ERK1/2 inhibitor 6	ERK	Inflammation/Immunology Cancer
ERK1/2 inhibitor 6 is a potent inhibitor of *ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor* 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1) .

HY-156393

Laxiflorin B

ERK Cancer

Laxiflorin B, a herbal compound, is a novel selective ERK1/2 inhibitor that has antitumor activity .

Laxiflorin B	ERK	Cancer
Laxiflorin B, a herbal compound, is a novel selective *ERK*1/2 inhibitor that has antitumor activity .

HY-P5977

STE-MEK1(13) Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide	ERK	Cancer
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH?) is a cell permeable *ERK1/2* inhibitor (IC₅₀: 13-30?μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .

HY-P10074

TAT-MEK1	ERK	Inflammation/Immunology
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC₅₀ in vitro for ERK2 is 29 μM .

HY-149414

MY-673	Microtubule/Tubulin Apoptosis ERK TGF-beta/Smad	Cancer
MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro .

HY-148510

HKB99	Phosphatase	Cancer
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 inhibits the formation of invasive pseudopodia and increases the level of PAI-2 in vitro. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC) .

HY-121280

ERK2-IN-4	ERK	Cancer
ERK2-IN-4 (Compound 6o) is an effective and selective *ERK2* inhibitor with a K_i of 0.006 μM. ERK2-IN-4 inhibits the ERK signaling pathway and can be used in cancer research .

HY-18849

ERK2-IN-3

ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 ^WT and Erk2 ^DS1 activation loop phosphorylation, with IC₅₀ of 5 μM and 42 nM, respectively .

ERK2-IN-3
ERK2-IN-3 (compound 2) is a inhibitor of *ERK2, and inhibits* Erk2 ^WT and Erk2 ^DS1 activation loop phosphorylation, with IC₅₀ of 5 μM and 42 nM, respectively .

HY-150606

ERK5-IN-4	ERK	Cancer
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits *ERK5* (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC₅₀ of 77 nM and 300 nM, respectively .

HY-113592

ERK-IN-4	ERK	Cancer
ERK-IN-4 is an *ERK* inhibitor binds preferentially to ERK2 with a K_d of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .

HY-14403

ERK5-IN-1

ERK Cancer

ERK5-IN-1 is a potent ERK5 inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.
HY-156394

Laxiflorin B-4

ERK Cancer

Laxiflorin B-4 is modificative compound of Laxiflorin B (HY-156393), exhibited higher affinity for ERK1/2 and stronger tumor suppression .
HY-153350

ERK-IN-7

ERK Cancer

ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent ERK inhibitor with IC₅₀ of 5 nM and 7 nM against ERK1 and ERK2, respectively .

ERK5-IN-1	ERK	Cancer
ERK5-IN-1 is a potent *ERK5* inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.

Laxiflorin B-4	ERK	Cancer
Laxiflorin B-4 is modificative compound of Laxiflorin B (HY-156393), exhibited higher affinity for ERK1/2 and stronger tumor suppression .

ERK-IN-7	ERK	Cancer
ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent *ERK* inhibitor with IC₅₀ of 5 nM and 7 nM against ERK1 and ERK2, respectively .

HY-128341

ERK5-IN-2	ERK	Cardiovascular Disease Cancer
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. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .

HY-N0590

Corynoxeine 4 Publications Verification	ERK	Cardiovascular Disease
Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent *ERK1/ERK2* inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.

HY-156450

ERK5-IN-5	ERK	Cancer
ERK5-IN-5 (compound 4a) is an *ERK5* kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC₅₀ value of 6.23 µg/mL for A549 cells .

HY-136579

ASN007 ERK-IN-3	ERK	Cancer
ASN007 (ERK-IN-3) is a potent and orally active inhibitor of *ERK. ASN007 inhibits* *ERK1/2* with low single-digit nM IC₅₀ values. ASN007 can be used for the research of cancers driven by RAS mutations .

HY-136579A

ASN007 benzenesulfonate ERK-IN-3 benzenesulfonate	ERK	Cancer
ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of *ERK. ASN007 benzenesulfonate inhibits* *ERK1/2* with low single-digit nM IC₅₀ values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations .

HY-156451

ERK5-IN-6	ERK	Cancer
ERK5-IN-6 (compound 5J) is an *ERK5* kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC₅₀ value of 4.56 µg/mL for A549 cells .

HY-150605

ERK5-IN-3	ERK	Cancer
ERK5-IN-3 (compound 33j) is a potent and selective *ERK5* (extracellular signal-related kinase 5) inhibitor, with an IC₅₀ of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC₅₀ of 31 nM .

HY-15947

Ravoxertinib 40+ Cited Publications GDC-0994	ERK	Cancer
Ravoxertinib (GDC-0994) is an orally active *ERK* kinase inhibitor with an IC₅₀ of 6.1 nM and 3.1 nM for *ERK1* and *ERK2*, respectively.

HY-15947A

Ravoxertinib hydrochloride 40+ Cited Publications GDC-0994 hydrochloride	ERK	Cancer
Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for *ERK* kinase activity with IC₅₀ of 6.1 nM and 3.1 nM for *ERK1* and *ERK2*, respectively.

HY-15665

XMD17-109

5 Publications Verification

ERK Cancer

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC₅₀ of 162 nM.
HY-112300

ERK2 IN-1

ERK Cancer

ERK2 IN-1 is a selective ERK2 inhibitor with an IC₅₀ of 7 nM .

XMD17-109 5 Publications Verification	ERK	Cancer
XMD17-109 is a novel, specific *ERK-5* inhibitor, with an IC₅₀ of 162 nM.

ERK2 IN-1	ERK	Cancer
ERK2 IN-1 is a selective *ERK2* inhibitor with an IC₅₀ of 7 nM .

HY-161462

ERK2/p38α MAPK-IN-1	ERK p38 MAPK	Cancer
ERK2/p38α MAPK-IN-1 (Compound 1, In silico Hit-2) is a potent and selective *ERK2* and p38α MAPK inhibitor, with an IC₅₀ of 82 μM for ERK2. ERK2/p38α MAPK-IN-1 binds to the allosteric site of ERK2 and p38α MAPK in distinct manners. ERK2/p38α MAPK-IN-1 can be used for the research of type 2 diabetes .

HY-15816A

Ulixertinib hydrochloride 20+ Cited Publications BVD-523 hydrochloride; VRT752271 hydrochloride	ERK	Cancer
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of *ERK1/2* kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-50846

SCH772984 115+ Cited Publications	ERK	Cancer
SCH772984 is a highly selective and ATP-competitive *ERK* inhibitor, with IC₅₀s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations .

HY-133084

ERK-IN-2

ERK Cancer

ERK-IN-2 is a ERK2 inhibitor with an IC₅₀ value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM .
HY-161363

ERK2 allosteric-IN-1

ERK Metabolic Disease Cancer

ERK2 allosteric-IN-1 (compound 1) is a selective and allosteric ERK2 inhibitor with the IC₅₀ of 11 μM .

ERK-IN-2	ERK	Cancer
ERK-IN-2 is a *ERK2* inhibitor with an IC₅₀ value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM .

ERK2 allosteric-IN-1	ERK	Metabolic Disease Cancer
ERK2 allosteric-IN-1 (compound 1) is a selective and allosteric *ERK2* inhibitor with the IC₅₀ of 11 μM .

HY-N1374

Magnolin 1 Publications Verification	ERK	Inflammation/Immunology
Magnolin, a major component of Magnolia liliiflora, inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of *ERK1* and *ERK2* with IC₅₀s of 87 nM and 16.5 nM, respectively.

HY-107622

(E/Z)-BIX02188	Others	Metabolic Disease
(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .

HY-135906

CK2/ERK8-IN-1	Casein Kinase ERK Pim DYRK Apoptosis	Cancer
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (K_i of 0.25 µM) and *ERK8* (MAPK15, ERK7) inhibitor with IC₅₀s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with K_is of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .

HY-112181

KO-947

3 Publications Verification

ERK Cancer

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.

KO-947 3 Publications Verification	ERK	Cancer
KO-947 is a potent and selective inhibitor of *ERK1/2* kinases with potential utility in MAPK pathway dysregulated tumors.

HY-12275

FR 180204 15+ Cited Publications	Flavivirus Dengue virus ERK Apoptosis	Cancer
FR 180204 is an ATP-competitive and selective *ERK* inhibitor. FR 180204 inhibits *ERK1* and *ERK2* with IC₅₀s of 0.51 μM (K_i=0.31 μM) and 0.33 μM (K_i=0.14 μM), respectively .

HY-15816

Ulixertinib 20+ Cited Publications BVD-523; VRT752271	ERK	Cancer
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of *ERK1/2* kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-N2283

Deltonin 1 Publications Verification	ERK Akt Endogenous Metabolite	Cancer
Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits *ERK1/2* and AKT activation.

HY-133084A

ERK-IN-2 free base	ERK	Cancer
ERK-IN-2 free base is a *ERK2* inhibitor with an IC₅₀ value of 1.8 nM. ERK-IN-2 free base might lead to off-target toxicity and/or off-target activity at dose >10 μM .

HY-50706A

Selumetinib sulfate 55+ Cited Publications AZD6244 sulfate; ARRY-142886 sulfate	MEK Apoptosis	Cancer
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2* inhibitor,* with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

HY-18932

DEL-22379 1 Publications Verification	ERK Apoptosis	Cancer
DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a K_d estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC₅₀ of ~0.5 μM.

HY-150687

ZINC12409120	ERK	Metabolic Disease
ZINC12409120 is a high selective *ERK* inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC₅₀ of 5.0 μM .

HY-151367

SHR2415	ERK	Cancer
SHR2415 is a highly potent, selective and orally active *ERK1/2* inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC₅₀ values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC₅₀ value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer .

Cat. No.	Product Name

HY-L010

MAPK Compound Library

519 compounds

MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.

MCE designs a unique collection of 519 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

HY-L164

Serine/Threonine Kinase Inhibitor Library

1286 compounds

Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.

MCE designs a unique collection of 1286 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

Cat. No.	Product Name	Target	Research Area

HY-P0178A

LXW7 TFA	Integrin	Inflammation/Immunology
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .

HY-P5977

STE-MEK1(13) Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide	ERK	Cancer
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH?) is a cell permeable *ERK1/2* inhibitor (IC₅₀: 13-30?μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .

HY-P10074

TAT-MEK1	ERK	Inflammation/Immunology
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC₅₀ in vitro for ERK2 is 29 μM .

HY-P0178

LXW7	Integrin	Inflammation/Immunology
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .

HY-P4136

*Myristoyl-MEK1 Derived Peptide Inhibitor* 1**	ERK	Cancer
Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits *ERK* activation with an IC₅₀ of 10 μM .

HY-P4497

Prolylserine	ERK	Cancer
Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of *ERK, but not cAMP response element binding protein (CREB)* .

HY-P4133

*MEK1 Derived Peptide Inhibitor* 1**	ERK MEK	Cancer
MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of *ERK2* by MEK1 with an IC₅₀ value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable .

HY-149205

CXJ-2	PI3K ERK	Inflammation/Immunology
CXJ-2 is a cyclic peptide, and exhibits moderate affinity toward elastin derived peptides (EDPs). CXJ-2 exhibits potent activities to inhibit the *PI3K/ERK* pathway and decrease hepatic stellate cell proliferation and migration. CXJ-2 possesses potent antifibrotic efficacy .

HY-P3206

Serum thymic factor Thymulin; Thymic factor	Peptides	Inflammation/Immunology
Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide. Serum thymic factor induces hyperalgesia. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor has anti-diabetic, analgesic and anti-inflammatory effects .

HY-P2262

TAT-DEF-Elk-1 1 Publications Verification TDE	Peptides	Neurological Disease
TAT-DEF-Elk-1 (TDE) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity .

HY-P2262A

TAT-DEF-Elk-1 TFA TDE TFA	Peptides	Neurological Disease
TAT-DEF-Elk-1 TFA (TDE TFA) is a cell-penetrating peptide inhibitor of Elk-1, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 TFA blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 TFA is a useful tool to analyze the role of Elk-1 in this process during the development of neuronal plasticity .

HY-P2265

SAH-SOS1A	Ras	Cancer
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-103544

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P	JNK Interleukin Related Bombesin Receptor	Inflammation/Immunology Cancer
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca ²⁺ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer

HY-P2265A

SAH-SOS1A TFA	Ras	Cancer
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0590

Corynoxeine 4 Publications Verification	Cardiovascular Disease Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Classification of Application Fields Source classification Rubiaceae Plants Disease Research Fields Indole Alkaloids	ERK
Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent *ERK1/ERK2* inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.

HY-N1374

Magnolin 1 Publications Verification	Structural Classification Classification of Application Fields Source classification Magnoliaceae Lignans Magnolia Liliflora Desr. Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	ERK
Magnolin, a major component of Magnolia liliiflora, inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of *ERK1* and *ERK2* with IC₅₀s of 87 nM and 16.5 nM, respectively.

HY-N2283

Deltonin 1 Publications Verification	Structural Classification Classification of Application Fields Source classification Dioscorea Zingiberensis C.H.Wright Plants Endogenous metabolite Disease Research Fields Steroids Cancer Dioscoreaceae	ERK Akt Endogenous Metabolite
Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits *ERK1/2* and AKT activation.

HY-W001174

2,5-Dihydroxyacetophenone	Structural Classification Classification of Application Fields Source classification Phenols Polyphenols Scrophulariaceae Plants Rehmannia glutinosa (Gaert.) Libosch. ex Fisch. et Mey Inflammation/Immunology Disease Research Fields	ERK NF-κB
2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the *ERK1/2* and NF-κB signaling pathways .

HY-156393

Laxiflorin B	Structural Classification Isodon eriocalyx var. laxiflora C. Y. Wu et H. W. Li Terpenoids Labiatae Source classification Diterpenoids Plants	ERK
Laxiflorin B, a herbal compound, is a novel selective *ERK*1/2 inhibitor that has antitumor activity .

HY-107417

Hypothemycin	Structural Classification Monophenols Microorganisms Antifungal Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Phenols Disease Research Disease Research Fields Cancer	VEGFR MEK FLT3 PDGFR ERK
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and *ERK1/ERK2*, respectively .

HY-N10175

Berkeleyacetal C	Other Terpenoids Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Terpenoids Source classification Endogenous metabolite Disease Research Fields Inflammation/Immunology	Fungal Endogenous Metabolite
Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways .

HY-N3828

epi-Eriocalyxin A	Other Terpenoids Structural Classification Isodon eriocalyx var. laxiflora C. Y. Wu et H. W. Li Classification of Application Fields Terpenoids Labiatae Source classification Plants Disease Research Fields Cancer	Apoptosis ERK JNK
epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits *ERK1/2* and JNK activation, which suppresses Bcl-2 expression .

HY-N0371

Pachymic acid 3 Publications Verification 3-O-Acetyltumulosic acid	Triterpenes Classification of Application Fields Terpenoids Source classification Polyporaceae Poria cocos Plants Disease Research Fields Cancer	Akt ERK
Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and *ERK* signaling pathways.

HY-142026

Vitisin A (+)-Vitisin A	Structural Classification Microorganisms Source classification Vitis vinifera cv. Zalema Phenols Polyphenols Plants Vitaceae	NF-κB ERK
Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots .

HY-N0774

Isofraxidin 1 Publications Verification	Structural Classification Monophenols Classification of Application Fields Source classification Coumarins Phenols Phenylpropanoids Acanthopanax senticosus (Rupr. et Maxim.) Harms Plants Inflammation/Immunology Disease Research Fields Araliaceae	COX MMP Toll-like Receptor (TLR)
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of *ERK1/2* in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .

HY-N10047

7,8-Didehydrocimigenol	Triterpenes Structural Classification Terpenoids Source classification Ranunculaceae Plants Cimicifuga foetida Linn.	NF-κB PPAR
7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .

HY-N2484

Methylnissolin Astrapterocarpan	Cardiovascular Disease Monophenols Flavonoids Classification of Application Fields Leguminosae Source classification Phenols Astragalus membranaceus var. mongholicus (Bunge)P.K.Hsiao Plants Other Flavonoids Disease Research Fields	PDGFR ERK
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC₅₀ of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the *ERK1/2* MAP kinase cascade .

HY-19696

Tauroursodeoxycholate Maximum Cited Publications 57 Publications Verification Tauroursodeoxycholic acid; TUDCA; UR 906	Structural Classification Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids Cancer	ERK Caspase Endogenous Metabolite Apoptosis
Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits *ERK*.

HY-19696A

Tauroursodeoxycholate sodium Maximum Cited Publications 57 Publications Verification Tauroursodeoxycholic acid sodium; TUDCA sodium; UR 906 sodium	Structural Classification Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids Cancer	ERK Caspase Apoptosis Endogenous Metabolite
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits *ERK*.

HY-19700

trans-Zeatin 1 Publications Verification	Structural Classification Natural Products Zea mays L. Classification of Application Fields Source classification Plants Endogenous metabolite Cytokinin Agricultural Research Gramineae Other Diseases Phytohormone Disease Research Fields	MEK ERK Endogenous Metabolite
trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced *MEK/ERK* activation.

HY-113509

Lipoxin A4 1 Publications Verification LXA4	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Inflammation/Immunology	Interleukin Related Endogenous Metabolite
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC₅₀ value of 25.74 nM .

HY-N0265

Asperosaponin VI 1 Publications Verification	Cardiovascular Disease Triterpenes Classification of Application Fields Terpenoids Dipsacaceae Source classification Plants Dipsacus asper Disease Research Fields	Caspase Apoptosis
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .

HY-N1818

Deoxysappanone B 3-Deoxysappanone B	Structural Classification Leguminosae Caesalpinia sappan L. Source classification Phenols Polyphenols Plants	p38 MAPK
Deoxysappanone B (3-Deoxysappanone B) is a homoisoflavone compound isolated from Caesalpinia sappan L (Lignum Sappan). Deoxysappanone B has anti-neuroinflammatory and neuroprotective effects and inhibits the production of neuroinflammatory mediators by blocking the IκB kinase (IKK)-NF-κB and p38/ERK MAPK pathways. Deoxysappanone B can be used in disease studies of neuritis and inflammation-related neurological damage .

HY-19696B

Tauroursodeoxycholate dihydrate Maximum Cited Publications 57 Publications Verification Tauroursodeoxycholic acid dihydrate; TUDCA dihydrate; UR 906 dihydrate	Structural Classification Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids Cancer	ERK Caspase Apoptosis Endogenous Metabolite
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits *ERK* .

HY-N2270

Chicanine	Structural Classification Monophenols Classification of Application Fields Source classification Lignans Phenols Phenylpropanoids Plants Schisandraceae Schisandra chinensis (Turcz.) Baill. Inflammation/Immunology Disease Research Fields	p38 MAPK ERK IKK
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .

HY-N12561

Pestanoid A	Structural Classification Microorganisms Terpenoids Source classification Diterpenoids	ERK p38 MAPK JNK
Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC₅₀ of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .

HY-N1504

Loureirin B	Dracaena cochinchinensis (Lour.) S. C. Chen Structural Classification Monophenols Flavonoids Classification of Application Fields Source classification Phenols Metabolic Disease Agavaceae Plants Dihydrochalcones Disease Research Fields	PAI-1 Potassium Channel ERK JNK
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC₅₀ of 26.10 μM; Loureirin B also inhibits K_ATP, the phosphorylation of *ERK* and JNK, and has anti-diabetic activity.

HY-N6264

26-Deoxyactein	Triterpenes Classification of Application Fields Terpenoids Source classification Ranunculaceae Metabolic Disease Plants Cimicifuga foetida Linn. Cimicifuga racemosa (L.) Nutt. Disease Research Fields	Aryl Hydrocarbon Receptor ERK
26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels .

HY-N12740

Napyradiomycin B4	Structural Classification Natural Products Microorganisms Source classification	MEK ERK
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced *MEK-ERK* signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis .

HY-N11439

Albanol B	Structural Classification Natural Products Source classification Phenols Polyphenols Morus alba L. Plants Moraceae	CDK Akt ERK Apoptosis Bacterial
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and *ERK1/2* .

HY-N2051

Zeylenone	Natural Products Classification of Application Fields Uvaria grandiflora Roxb. Source classification Plants Annonaceae Disease Research Fields Cancer	Apoptosis
Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways .

HY-N10079

Suchilactone Jatrophan	Structural Classification Polygala chinensis Linnaeus Source classification Polygalaceae Lignans Phenylpropanoids Plants	SHP2
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .

HY-W744699

Larixol (+)-Larixol	Larix decidua Miller Structural Classification Natural Products Pinaceae Source classification Plants	Src ERK Akt
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM), cathepsin G release (IC₅₀: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .

HY-N0226

Epiberberine	Alkaloids Source classification Ranunculaceae Coptis chinensis Franch. Plants Isoquinoline Alkaloids	Cholinesterase (ChE) Beta-secretase
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .

HY-N0809

Sesamolin 2 Publications Verification	Sesamum indicum Linn. Source classification Other Phenylpropanoids Phenylpropanoids Pedaliaceae Plants	p38 MAPK JNK Caspase
Sesaminol, isolated from Sesamum indicum, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression .

HY-N3711

Dehydrocrenatine	Simaroubaceae Source classification Plants Indole Alkaloids Picrasma chinensis P. Y. Chen	JNK ERK Apoptosis
Dehydrocrenatidine, a β-carboline alkaloid that can be isolated from Picrasma quassioides. Dehydrocrenatidine induces cell apoptosis by activates *ERK* and JNK. Dehydrocrenatidine inhibits invasion and migration of cancer cells, it also suppresses neuronal excitability to exert analgesic effects .

HY-N3261

Methyllinderone	Structural Classification Flavonoids Source classification Lindera erythrocarpa Makino Plants Lauraceae Other Flavonoids	AP-1 ERK STAT
Methyllinderone is an inhibitor of *AP-1/STAT/ERK*. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis .

HY-N0226A

Epiberberine chloride 3 Publications Verification	Alkaloids Structural Classification Neurological Disease Classification of Application Fields Coptis chinensis Franch. Ranunculaceae Source classification Metabolic Disease Plants Isoquinoline Alkaloids Disease Research Fields	Cholinesterase (ChE) Beta-secretase Reactive Oxygen Species
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .

HY-N2450

Sulforaphene	Structural Classification Natural Products Classification of Application Fields Source classification Plants Brassicaceae Disease Research Fields Cancer Raphanus sativus Linn.	Apoptosis EGFR ERK NF-κB Microtubule/Tubulin
Sulforaphene, isolated from radish seeds, exhibits an ED₅₀ against velvetleaf seedlings approximately 2 x 10 ^-4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, *p-ERK1/2, NF‐κB* and other signals .

HY-N3806

Enniatin B	Infection Cardiovascular Disease Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields	Acyltransferase ERK
Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 113 μM in an enzyme assay using rat liver microsomes . Enniatins B decreases the activation of *ERK* (p44/p42) .

HY-134000

Emodic acid NSC624610	Quinones Structural Classification Human Gut Microbiota Metabolites Microorganisms Leguminosae Cercis chinensis Bunge Anthraquinones Source classification Plants Endogenous metabolite	p38 MAPK NF-κB ERK JNK VEGFR MMP
Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, *ERK* and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells .

HY-N0745

Senkyunolide I	Natural Products Classification of Application Fields Source classification Dicerothamnus rhinocerotis Plants Umbelliferae Disease Research Fields Inflammation/Immunology	Caspase
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3 .

HY-N6959

Osmundacetone	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Labiatae Source classification Phenols Polyphenols Metabolic Disease Helianthella quinquenervis (Hook.) A.Gray Plants Disease Research Fields	Reactive Oxygen Species Apoptosis
Osmundacetone is a natural product isolated from Osmundae Rhizoma, with neuroprotective and anti-apoptotic effects. Osmundacetone also has DPPH scavenging activity and anti-oxidative stress activity. Osmundacetone inhibits MAPK phosphorylation, including JNK, ERK, and p38 kinase. Osmundacetone can be a potential agent for the research of neurodegenerative diseases .

HY-N6704

Enniatin A1	Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Anticancer Disease Research Fields Cancer	ERK Apoptosis
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. 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 microsomes .

HY-N2963

Broussonin E	Structural Classification Thymelaeaceae Source classification Daphne giraldii Nitsche Phenols Polyphenols Plants	ERK p38 MAPK JAK STAT TNF Receptor Interleukin Related COX Arginase
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the *ERK* and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis .

HY-N3071

Picrasidine I	Simaroubaceae Source classification Plants Quassia amaraL. Indole Alkaloids	Apoptosis Reactive Oxygen Species
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell apoptosis by downregulats *ERK* and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1 .

HY-N6796

Manumycin A	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Disease Research Fields Other Antibiotics	Farnesyl Transferase Ras Apoptosis Phospholipase
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (K_i=1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling . Manumycin A is a nSMase inhibitor (EC₅₀=0.25 μM) .

HY-N7110

6-Hydroxyflavone	Structural Classification Monophenols Flavonoids Scutellaria baicalensis Georgi Classification of Application Fields Flavones Labiatae Source classification Phenols Plants Inflammation/Immunology Disease Research Fields	Akt ERK JNK
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .

HY-16558

Butein 3 Publications Verification 2’,3,4,4’-tetrahydroxy Chalcone	Structural Classification Chalcones Flavonoids other families Classification of Application Fields Anti-aging Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)
Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60 ^c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).

HY-N2510

Myristicin Myristicine	Structural Classification Simple Phenylpropanols Source classification Myristicaceae Phenylpropanoids Plants Myristica fragrans Houtt.	5-HT Receptor EGFR ERK Apoptosis Bacterial
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the *EGFR/ERK* signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .

HY-N3807

Enniatin B1 1 Publications Verification	Cardiovascular Disease Infection Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields	Acyltransferase ERK NF-κB
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 73 μM in an enzyme assay using rat liver microsomes . 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 .

HY-N0498

Nitidine chloride 2 Publications Verification	Alkaloids Classification of Application Fields Source classification Rutaceae Zanthoxylum nitidum (Roxb.) DC. Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields	Parasite Apoptosis STAT Topoisomerase ERK FAK p38 MAPK NF-κB
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, *ERK* and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway .

HY-N10802

6-O-Isobutyrylbritannilactone	Structural Classification Terpenoids Helianthus tuberosus L. Orchidaceae Source classification Plants Compositae	ERK Akt PI3K Epigenetic Reader Domain
6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. 6-O-Isobutyrylbritannilactone, a sesquiterpene, can be isolated from the flowers of Inula britannica. 6-O-Isobutyrylbritannilactone inhibits IBMX (HY-12318)-induced melanin production in B16F10 cells. 6-O-Isobutyrylbritannilactone also regulates *ERK, PI3K/AKT, and CREB*, shows antimelanogenic activity in zebrafish embryos models .

HY-N0678

Icaritin 1 Publications Verification Anhydroicaritin	Flavonols Structural Classification Classification of Application Fields Source classification Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Phenols Polyphenols Epimedium brevicornu Maxim. Berberidaceae Disease Research Fields Cancer	Autophagy Apoptosis
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC₅₀ of 8 µM) and primary CML cells (IC₅₀ of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate *MAPK/ERK/JNK* and JAK2/STAT3 /AKT signalings, also enhances osteogenesis ^[3.

Cat. No.	Product Name	Chemical Structure

HY-14188S

Amiodarone-d4 hydrochloride

Amiodarone-d₄ (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].

HY-19696AS

Tauroursodeoxycholate-d4 sodium
Tauroursodeoxycholate-d₄ (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-19696S

Tauroursodeoxycholate-d5
Tauroursodeoxycholate-d₅ is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-19696S1

Tauroursodeoxycholate-d4
Tauroursodeoxycholate-d₄ is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-19696S2

Tauroursodeoxycholate-d4-1
Tauroursodeoxycholate-d₄-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-113509S

Lipoxin A4-d5

Lipoxin A4-d₅ is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].

HY-19700S

trans-Zeatin-d5
trans-Zeatin-d₅ is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.

HY-114436S

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-142283AS

Dosimertinib mesylate
Dosimertinib-d₅ (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d₅ (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d₅ (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d₅ (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

HY-B0185AS1

Lidocaine-d6 hydrochloride

Lidocaine-d₆ (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].

HY-B0185AS

Lidocaine-d10 hydrochloride

Lidocaine-d₁₀ (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].

HY-B0185S1

Lidocaine-d10

Lidocaine-d₁₀ is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].

HY-B0185S

Lidocaine-d10 N-Oxide

N-Oxide Lidocaine-d₁₀ is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].

HY-142283

Dosimertinib
Dosimertinib-d₃-d₃ is a potent and orally active EGFR inhibitor. Dosimertinib-d₃-d₃ decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d₃-d₃ shows antiproliferative and anti-tumor activity. Dosimertinib-d₃-d₃ has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

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