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Results for "

ERK1/2 phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Akt (4) Apoptosis (11) Arrestin (1) Autophagy (2) Bacterial (1) Bcr-Abl (1) Bombesin Receptor (1) Bradykinin Receptor (1) c-Kit (1) c-Met/HGFR (4) CDK (1) COX (1) EGFR (3) Endogenous Metabolite (1) ERK (15) Formyl Peptide Receptor (FPR) (1) GPR55 (4) Histone Methyltransferase (1) IKK (1) Integrin (2) Itk (1) JNK (2) Keap1-Nrf2 (1) MEK (4) Melanocortin Receptor (3) mGluR (1) MMP (2) NF-κB (1) p38 MAPK (5) PDGFR (2) PERK (1) Phospholipase (1) PKC (1) PPAR (2) PROTACs (1) Protease Activated Receptor (PAR) (1) Raf (1) Reactive Oxygen Species (1) SHP2 (1) Src (2) Syk (2) Toll-like Receptor (TLR) (1) VEGFR (1)
By Research Areas:	Cancer (31) Cardiovascular Disease (4) Endocrinology (1) Infection (1) Inflammation/Immunology (12) Metabolic Disease (6) Neurological Disease (4)

By Targets:

Adrenergic Receptor (1)

Akt (4)

Apoptosis (11)

Arrestin (1)

Autophagy (2)

Bacterial (1)

Bcr-Abl (1)

Bombesin Receptor (1)

Bradykinin Receptor (1)

c-Kit (1)

c-Met/HGFR (4)

CDK (1)

COX (1)

EGFR (3)

Endogenous Metabolite (1)

ERK (15)

Formyl Peptide Receptor (FPR) (1)

GPR55 (4)

Histone Methyltransferase (1)

IKK (1)

Integrin (2)

Itk (1)

JNK (2)

Keap1-Nrf2 (1)

MEK (4)

Melanocortin Receptor (3)

mGluR (1)

MMP (2)

NF-κB (1)

p38 MAPK (5)

PDGFR (2)

PERK (1)

Phospholipase (1)

PKC (1)

PPAR (2)

PROTACs (1)

Protease Activated Receptor (PAR) (1)

Raf (1)

Reactive Oxygen Species (1)

SHP2 (1)

Src (2)

Syk (2)

Toll-like Receptor (TLR) (1)

VEGFR (1)

By Research Areas:

Cancer (31)

Cardiovascular Disease (4)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (12)

Metabolic Disease (6)

Neurological Disease (4)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Targets Recommended: Oxidative Phosphorylation DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122246

ML192	GPR55 PKC ERK Arrestin	Metabolic Disease
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, *ERK1/2* phosphorylation and PKCβII translocation .

HY-124740

ML00253764	Melanocortin Receptor	Cancer
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .

HY-50706

Selumetinib Maximum Cited Publications 57 Publications Verification AZD6244; ARRY-142886	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-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-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-P3751

[Tyr8] Bradykinin	Bradykinin Receptor ERK	Cardiovascular Disease Endocrinology
[Tyr8] Bradykinin is a B₂ kinin receptor agonist. [Tyr8] Bradykinin also stimulates **ERK1/2 phosphorylation**. [Tyr8] Bradykinin can be used as an internal standard .

HY-50706A

Selumetinib sulfate Maximum Cited Publications 57 Publications Verification 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-100403

Ro 67-7476 5+ Cited Publications	mGluR	Cancer
Ro 67-7476 is a potent positive allosteric modulator of mGluR₁ and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC₅₀ of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC₅₀=163.3 nM) .

HY-N2858

Alpinumisoflavone acetate	Apoptosis	Cancer
Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .

HY-153445

MEK-IN-6	ERK MEK	Cancer
MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits *ERK1/2* (Thr202/Tyr204) phosphorylation in A375 cells (IC₅₀: 2 nM). MEK-IN-6 can be used for research of cancer .

HY-147301

Resomelagon AP1189	Melanocortin Receptor	Metabolic Disease Inflammation/Immunology
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC₁ and MC₃. Resomelagon induces ERK1/2 phosphorylation and Ca ²⁺ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research .

HY-147301A

Resomelagon acetate AP1189 acetate	Melanocortin Receptor	Metabolic Disease Inflammation/Immunology
Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC₁ and MC₃. Resomelagon acetate induces ERK1/2 phosphorylation and Ca ²⁺ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research .

HY-155533

YF704	SHP2	Cancer
YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC₅₀=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates *Erk1/2* and Akt phosphorylation levels in cancer cells .

HY-107640

WAY-170523	MMP	Cancer
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC₅₀ of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .

HY-13241

Ralimetinib dimesylate 10+ Cited Publications LY2228820 dimesylate	p38 MAPK Autophagy Apoptosis	Inflammation/Immunology Cancer
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

HY-N1987

Cucurbitacin IIb
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .

HY-146672

ITK inhibitor 6	Itk	Cancer
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC₅₀s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .

HY-150700

RLX-33	ERK	Metabolic Disease
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC₅₀ values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .

HY-13241A

Ralimetinib LY2228820	p38 MAPK Autophagy	Inflammation/Immunology Cancer
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .

HY-126477

NNK	Endogenous Metabolite	Cancer
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser ⁷⁰ and c-Myc at Thr ⁵⁸ and Ser ⁶² through activation of both *ERK1/2* and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .

HY-13905

Flumatinib mesylate HHGV678 mesylate	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀ values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .

HY-16697

CID 16020046 1 Publications Verification	GPR55	Cancer
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC₅₀ of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca ²⁺ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .

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-N10047

7,8-Didehydrocimigenol	NF-κB PPAR	Cardiovascular Disease
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-154985

DSO-5a	PPAR Bombesin Receptor ERK	Metabolic Disease
DSO-5a is a potent, selective, orally active BB₃ agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB₃ and activates *ERK1/2* phosphorylation. DSO-5a can be used in diabetes-related research .

HY-155417

GPR34 receptor antagonist 3	Others	Neurological Disease
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC₅₀ is 0.680 μM. GPR34 receptor antagonist 3 inhibited *ERK1/2* phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .

HY-76474

BAY 61-3606	Syk Apoptosis	Inflammation/Immunology Cancer
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i of 7.5 nM and an IC₅₀ of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .

HY-14985

BAY 61-3606 dihydrochloride 5 Publications Verification	Syk Apoptosis	Inflammation/Immunology Cancer
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i of 7.5 nM an IC₅₀ of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .

HY-N0774

Isofraxidin 1 Publications Verification	COX MMP Toll-like Receptor (TLR)	Inflammation/Immunology
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-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-111083

ML191 CID23612552	GPR55	Others
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC₅₀=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC₅₀=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .

HY-108554

Q94 hydrochloride	Protease Activated Receptor (PAR)	Others
Q94 hydrochloride, a selective PAR₁ antagonist (IC₅₀=916 nM), can selectively block PAR₁/Gαq interaction and signalling. Q94 hydrochloride blocks PAR₁-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced *ERK1/2* and MLC phosphorylation .

HY-153606

SOS1 agonist-1	Others	Cancer
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role ^{[1] ^.}

HY-151379

EM127	Histone Methyltransferase	Cancer
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (K_D=13 μM) and site-specificity. EM127 effectively inhibits *ERK1/2* phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .

HY-N2484

Methylnissolin Astrapterocarpan	PDGFR ERK	Cardiovascular Disease
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-N11439

Albanol B	CDK Akt ERK Apoptosis Bacterial	Infection Neurological Disease Cancer
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-153864

PROTAC MEK1 Degrader-1	PROTACs MEK ERK	Cancer
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC₅₀ value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit *ERK1/2* phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .

HY-116461

ML-184 CID2440433	GPR55	Neurological Disease
ML-184 (CID2440433) is a selective GPR55 agonist with an EC₅₀ of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55 . ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro .

HY-18318

Takeda-6D	Raf VEGFR PERK	Cancer
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC₅₀ values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of *ERK1/2* phosphorylation. Takeda-6D shows antitumor activity .

HY-145384

ROC-0929	Phospholipase	Inflammation/Immunology
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A₂ (sPLA₂s) with an IC₅₀ of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of *ERK1/2* and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca ²⁺-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .

HY-12927

SX-517
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca ²⁺ flux (IC₅₀=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC₅₀=60 nM) and *ERK1/2* phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .

HY-13404

Capmatinib 5+ Cited Publications INC280; INCB28060	c-Met/HGFR Apoptosis	Cancer
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .

HY-13404B

Capmatinib hydrochloride INC280 hydrochloride; INCB-28060 hydrochloride	c-Met/HGFR Apoptosis	Cancer
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .

HY-13404C

Capmatinib dihydrochloride hydrate 5+ Cited Publications INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate	c-Met/HGFR Apoptosis	Cancer
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .

HY-13404A

Capmatinib dihydrochloride INC280 dihydrochloride; INCB28060 dihydrochloride	c-Met/HGFR Apoptosis	Cancer
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .

HY-151431

Nrf2/HO-1 activator 2	Keap1-Nrf2 Reactive Oxygen Species ERK Akt JNK	Neurological Disease
Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD) .

HY-W744699

Larixol (+)-Larixol	Src ERK Akt	Inflammation/Immunology
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-W745090

Isomaltulose monohydrate	Formyl Peptide Receptor (FPR) Src ERK Akt p38 MAPK	Others
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate 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. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .

HY-103211

L748337	Adrenergic Receptor	Cardiovascular Disease Metabolic Disease Cancer
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The K_i values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to G_i to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC₅₀ value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .

HY-147183

JBJ-09-063	EGFR	Cancer
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .

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