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Results for "

p-ERK

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PERK (64) Acyltransferase (2) Akt (18) Aminotransferases (Transaminases) (1) Anaplastic lymphoma kinase (ALK) (1) Angiotensin Receptor (2) AP-1 (2) Apoptosis (59) Aryl Hydrocarbon Receptor (1) ATF6 (2) Atg8/LC3 (6) Autophagy (16) Bcl-2 Family (9) Bcr-Abl (1) c-Fms (1) c-Met/HGFR (2) Cannabinoid Receptor (3) Carnitine Palmitoyltransferase (CPT) (2) Caspase (12) CDK (6) COX (1) CXCR (1) Cyclophilin (1) DAPK (1) DGK (2) DNA/RNA Synthesis (2) Dopamine Receptor (1) Drug Derivative (1) EGFR (12) Endogenous Metabolite (2) Epigenetic Reader Domain (1) ERK (41) Eukaryotic Initiation Factor (eIF) (11) Ferroptosis (3) FGFR (4) FLT3 (5) Fungal (4) HDAC (1) Heme Oxygenase (HO) (3) HIF/HIF Prolyl-Hydroxylase (1) HSP (4) iGluR (1) Interleukin Related (2) IRE1 (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (4) JAK (3) JNK (8) Keap1-Nrf2 (2) Lipase (1) LPL Receptor (1) MDM-2/p53 (3) MEK (10) mGluR (3) Microtubule/Tubulin (6) Mitochondrial Metabolism (1) MMP (2) Molecular Glues (3) mTOR (3) MyD88 (1) NADPH Oxidase (1) NF-κB (10) NO Synthase (1) Nuclear Hormone Receptor 4A/NR4A (3) P-glycoprotein (1) p38 MAPK (16) p62 (5) PARP (1) PD-1/PD-L1 (3) Phosphatase (2) Phosphodiesterase (PDE) (1) Phospholipase (1) PI3K (7) PKC (2) Potassium Channel (3) PROTACs (11) Protein Arginine Deiminase (1) Pyroptosis (2) Raf (4) RAR/RXR (1) Ras (38) Reactive Oxygen Species (ROS) (18) Reference Standards (15) ROCK (1) ROS Kinase (1) Serotonin Transporter (5) SHP2 (9) Sigma Receptor (1) Small Interfering RNA (siRNA) (3) SOD (1) SOS1 (8) SphK (1) Src (1) STAT (4) STING (1) Syk (2) TAM Receptor (1) TNF Receptor (2) Toll-like Receptor (TLR) (1) Trk Receptor (1) VDAC (1) VEGFR (3) Xanthine Oxidase (3)
By Research Areas:	Cancer (163) Cardiovascular Disease (16) Endocrinology (5) Infection (5) Inflammation/Immunology (17) Metabolic Disease (16) Neurological Disease (21)
Click Chemistry:	Alkynes (4)
Oligonucleotides:	Mouse Pre-designed siRNA Sets (2) Human Pre-designed siRNA Sets (1) siRNAs (3)

191

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Oligonucleotides

GMP Molecules

Targets Recommended: PERK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10254

Mirdametinib Maximum Cited Publications 154 Publications Verification PD0325901; PD325901	MEK Autophagy Apoptosis	Cancer
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC₅₀ of 0.33 nM. Mirdametinib exhibits a K_i ^app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .

HY-18072

GSK2606414 120+ Cited Publications	PERK Autophagy Apoptosis	Cancer
GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC₅₀ of 0.4 nM.

HY-12495

ISRIB (trans-isomer) 45+ Cited Publications	PERK Autophagy Apoptosis	Neurological Disease
ISRIB (trans-isomer) is a potent inhibitor of *PERK* with an IC₅₀ of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC₅₀=5 nM).

HY-14268

Febuxostat 10+ Cited Publications TEI 6720; TMX 67	Xanthine Oxidase	Cardiovascular Disease Metabolic Disease Cancer
Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a K_i value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .

HY-13820

GSK2656157 60+ Cited Publications	PERK Autophagy Apoptosis	Cancer
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC₅₀ of 0.9 nM.

HY-12661A

*AMG PERK* 44** 5+ Cited Publications	PERK Autophagy	Cancer
AMG PERK 44 is an orally active and highly selective *PERK* inhibitor with an IC₅₀ of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC₅₀=7300 nM) and B-Raf (IC₅₀ >1000 nM), respectively. AMG PERK 44 induces autophagy .

HY-119240

CCT020312 35+ Cited Publications	PERK Autophagy	Neurological Disease Cancer
CCT020312 is a selective *EIF2AK3/PERK* activator. CCT020312 elicits EIF2A phosphorylation in cells.

HY-148273

Setidegrasib ASP-3082; KRAS G12D inhibitor 17	PROTACs Ras ERK Akt	Cancer
Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC₅₀: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses *p-ERK, p-AKT, p-S6* levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .

HY-14463

Onalespib 10+ Cited Publications AT13387	HSP	Cancer
Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) .

HY-100403

Ro 67-7476 20+ 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-N0777

Isorhamnetin-3-O-glucoside 3 Publications Verification	Others PERK ERK Akt PI3K Lipase	Metabolic Disease
Isorhamnetin-3-O-glucoside is an orally active natural compound. Isorhamnetin 3-O-glucoside increases *P-ERK, ERK, P-Akt (Ser473), P-PI3K, and PDX-1. Isorhamnetin 3-O-glucoside downregulates C/EBPα* and inhibits lipase. Isorhamnetin 3-O-glucoside reduces lipids and inhibits obesity .

HY-145015

Tuspetinib HM43239	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .

HY-B0168A

Milnacipran hydrochloride 2 Publications Verification	Serotonin Transporter PERK	Neurological Disease
Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (K_i values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits *pERK1/2* activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .

HY-N0745

Senkyunolide I	Caspase ERK Keap1-Nrf2 Heme Oxygenase (HO) Apoptosis	Neurological Disease Inflammation/Immunology
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates *p-Erk1/2* and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .

HY-153343

Veludacigib 3 Publications Verification BAY 2965501	DGK	Cancer
BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer .

HY-N2450

Sulforaphene 1 Publications Verification	Apoptosis EGFR ERK NF-κB Microtubule/Tubulin	Cancer
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-176786

MCB-36	PROTACs Ras Apoptosis PERK p38 MAPK Caspase TNF Receptor	Cancer
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities K_d ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .

HY-137207

MK-28 5+ Cited Publications	PERK	Neurological Disease
MK-28 is a potent and selective *PERK* activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .

HY-N0687

Vindoline 1 Publications Verification	Microtubule/Tubulin Apoptosis NF-κB PERK	Metabolic Disease Inflammation/Immunology Endocrinology
Vindoline is an orally active vinca alkaloid. Vindoline can be extracted from the leaves of Catharanthus roseus. Vindoline has a weak inhibitory effect on the self-assembly of tubulin. Vindoline alleviates Apoptosis, inhibits p-p65 and *p-ERK*. Vindoline improves diabetes, bone loss, osteoarthritis, and kidney damage .

HY-N6857

Armepavine	AP-1 NF-κB p38 MAPK ERK JNK	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia .

HY-114189

GW284543 1 Publications Verification UNC10225170	MEK	Cancer
GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein .

HY-153740

PF-07284892 ARRY-558	SHP2	Cancer
PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC₅₀ value of 21 nM. PF-07284892 decreases the expression of pERK .

HY-156625

Nedometinib 1 Publications Verification NFX-179	MEK PERK p38 MAPK	Cancer
Nedometinib (NFX-179) is a specific MEK1 inhibitor with an IC₅₀ of 135 nM. Nedometinib inhibits *p-ERK, MAPK*. Nedometinib exerts anticancer activity against squamous cell carcinoma. Nedometinib can be used for research in dermatosis, neurofibromatosis .

HY-13984

NT-1 1 Publications Verification EGFR mutant-IN-3	EGFR ERK Apoptosis Drug Derivative	Cancer
NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR ^WT with an IC₅₀ of 0.4 nM. NT-1 also inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M. NT-1 exerts deeper inhibition on p-EGFR and *p-ERK, and induces tumor cell apoptosis*. NT-1 can be used in colorectal cancer research .

HY-157231A

HC-5404-Fu	PERK	Cancer
HC-5404-Fu is an orally active *PERK* inhibitor with an IC₅₀ of 0.001 μM against human PERK. HC-5404-Fu blocks *PERK* activation induced by VEGFR-TKI and disrupts the adaptive stress response triggered by VEGFR-TKI. HC-5404-Fu enhances anti-angiogenic effects by inhibiting newly formed and mature tumor blood vessels in renal cell carcinoma models. HC-5404-Fu can be used in research related to renal cell carcinoma .

HY-163985

PROTAC FGFR2 degrader 1	PROTACs FGFR Apoptosis	Cancer
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC₅₀ of 6.46 nM, the FGFR2 IC₅₀ is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .

HY-14268R

Febuxostat (Standard) TEI 6720 (Standard); TMX 67 (Standard)	Reference Standards Xanthine Oxidase	Cardiovascular Disease Metabolic Disease
Febuxostat (Standard) is the analytical standard of Febuxostat. This product is intended for research and analytical applications. Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a K_i value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .

HY-135220

PERK-IN-2 1 Publications Verification	PERK	Cancer
PERK-IN-2 is a potent *PERK* inhibitor with an IC₅₀ of 0.2 nM .

HY-137813

PERK-IN-4	PERK	Neurological Disease Metabolic Disease Cancer
PERK-IN-4 is a potent and selective *PERK* (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. *PERK* is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .

HY-153832

MSU-42011	RAR/RXR NO Synthase	Cancer
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of *p-ERK* protein. MSU-42011 has immunomodulatory and antitumor activity .

HY-P3136

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and *p-ERK1/2*. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-158196

PERK/eIF2α activator 1	PERK Apoptosis	Cancer
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC₅₀ value of 23 μM .

HY-117720

OSU-2S	PKC Apoptosis	Cancer
OSU-2S is a potent PKCδ activator. OSU-2S inhibits cell proliferation and migration. OSU-2S decreases the expression of p-ERK1/2, increases the expression of PKCδ (38 kDa) when combined with Sorafenib (HY-10201). OSU-2S induces Apoptosis. OSU-2S slao is a non-immunosuppressive analogue of FTY720. OSU-2S shows anticancer activity .

HY-P3136A

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and *p-ERK1/2*. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-B0168

Milnacipran 2 Publications Verification	Serotonin Transporter PERK	Neurological Disease
Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (K_i values of 31 and 8.5 nM, respectively). Milnacipran inhibits *pERK1/2* activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .

HY-145835

PERK-IN-5	PERK	Cancer
PERK-IN-5 is a highly potent, selectively and orally bioavailable *PERK* inhibitor (IC₅₀s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .

HY-142283AS

Dosimertinib-d5 mesylate AZD-9291-d5 mesylate; Mereletinib-d5 mesylate	EGFR	Cancer
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) .

HY-162445

KRASG12D-IN-3	Ras PERK	Cancer
KRASG12D-IN-3 is an orally active KRAS ^G12D inhibitor. KRASG12D-IN-3 inhibits the growth of gastric cancer and pancreatic cancer cells. KRASG12D-IN-3 inhibits the activity of *p-ERK* in gastric cancer cells. KRASG12D-IN-3 can be used for the research of gastric cancer and pancreatic cancer .

HY-P991664

AG01	Src Akt ERK TAM Receptor c-Met/HGFR MMP HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and *p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF*. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers .

HY-113916

Onalespib lactate AT13387 lactate	HSP	Cancer
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an K_d value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .

HY-115527

SHP244	SHP2	Cancer
SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC₅₀ value for SHP2 ^WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers .

HY-142283

Dosimertinib	Isotope-Labeled Compounds EGFR	Cancer
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) .

HY-146544

KRAS inhibitor-14	Ras	Cancer
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC₅₀s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .

HY-168482

NF-κB/MAPK-IN-2	NF-κB p38 MAPK	Cancer
NF-κB/MAPK-IN-2 (compound 14) is a potent NF-κB and MAPK Inhibitor. NF-κB/MAPK-IN-2 decreases the protein expression of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. NF-κB/MAPK-IN-2 reduces the LPS-induced release of TNF-α and IL-6. NF-κB/MAPK-IN-2 inhibits nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 has the potential for the research of sepsis .

HY-178176

PROTAC CB1R Degrader-1	PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis	Cancer
PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC₅₀ of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, *p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis*. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .

HY-173119

SKLB-D18	ERK Autophagy Apoptosis p62 mTOR Reactive Oxygen Species (ROS) Ferroptosis	Cancer
SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC₅₀ of 38.69 nM and a K_d of 126.9 nM against human ERK1, an IC₅₀ of 40.12 nM and a K_d of 209.8 nM against ERK2, and an IC₅₀ of 59.72 nM and a K_d of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of *p-ERK5, p-RSKp90, p-c-Myc* and c-Myc, and upregulates the level of *p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II* accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer .

HY-N3480

Isogosferol (+)-Isogospherol; Isogospherol	Others	Inflammation/Immunology
Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2 .

HY-153160

PERK-IN-6	PERK	Cancer
PERK-IN-6 (Compound 5) is a *PERK* inhibitor with an IC₅₀ of 2.5 nM .

HY-146543

KRAS inhibitor-13	Ras	Cancer
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC₅₀s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .

HY-146533

KRAS inhibitor-12	Ras	Cancer
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC₅₀s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W050044

L-Azetidine-2-carboxylic acid 1 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite PERK Atg8/LC3 Autophagy Bcl-2 Family Apoptosis Eukaryotic Initiation Factor (eIF) ATF6
L-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the *PERK* pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects .

HY-N0777

Isorhamnetin-3-O-glucoside 3 Publications Verification	Flavonols Cruciferous vegetables Flavonoids Classification of Application Fields Phenols Polyphenols Metabolic Disease Plants Brassicaceae Disease Research Fields Source Classification	Others PERK ERK Akt PI3K Lipase
Isorhamnetin-3-O-glucoside is an orally active natural compound. Isorhamnetin 3-O-glucoside increases *P-ERK, ERK, P-Akt (Ser473), P-PI3K, and PDX-1. Isorhamnetin 3-O-glucoside downregulates C/EBPα* and inhibits lipase. Isorhamnetin 3-O-glucoside reduces lipids and inhibits obesity .

HY-N0745

Senkyunolide I	Structural Classification Natural Products Classification of Application Fields Dicerothamnus rhinocerotis Umbelliferae Plants Inflammation/Immunology Disease Research Fields Source Classification	Caspase ERK Keap1-Nrf2 Heme Oxygenase (HO) Apoptosis
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates *p-Erk1/2* and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .

HY-N2450

Sulforaphene 1 Publications Verification	Natural Products Classification of Application Fields Plants Brassicaceae Disease Research Fields Cancer Source Classification 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-N0687

Vindoline 1 Publications Verification	Apocynaceae Alkaloids Structural Classification Classification of Application Fields Plants Disease Research Fields Indole Alkaloids Catharanthus roseus (L.) G. Don Source Classification Cancer	Microtubule/Tubulin Apoptosis NF-κB PERK
Vindoline is an orally active vinca alkaloid. Vindoline can be extracted from the leaves of Catharanthus roseus. Vindoline has a weak inhibitory effect on the self-assembly of tubulin. Vindoline alleviates Apoptosis, inhibits p-p65 and *p-ERK*. Vindoline improves diabetes, bone loss, osteoarthritis, and kidney damage .

HY-N6857

Armepavine	Structural Classification Classification of Application Fields Plants Nymphaeaceae Alkaloids Monophenols other families Phenols Nelumbo nucifera Gaertn. Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields Source Classification	AP-1 NF-κB p38 MAPK ERK JNK
Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia .

HY-W010451

1,2,4-Trihydroxybenzene Hydroxyhydroquinone	Cardiovascular Disease Microorganisms Classification of Application Fields Phenols Polyphenols Disease Research Fields Source Classification	PERK Eukaryotic Initiation Factor (eIF) Potassium Channel Apoptosis
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the *PERK-eIF2α* signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .

HY-N3480

Isogosferol (+)-Isogospherol; Isogospherol	Coumarins Ageratina altissima (L.) R.M.King & H.Rob. Phenylpropanoids Umbelliferae Plants Source Classification	Others
Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2 .

HY-N2450R

Sulforaphene (Standard)	Structural Classification Natural Products Plants Brassicaceae Source Classification Raphanus sativus Linn.	Reference Standards 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-N0687R

Vindoline (Standard)	Apocynaceae Alkaloids Structural Classification Plants Indole Alkaloids Catharanthus roseus (L.) G. Don Source Classification	Reference Standards Microtubule/Tubulin Apoptosis NF-κB PERK
Vindoline (Standard) is an analytical standard of Vindoline (HY-N0687). This product is intended for research and analytical applications. Vindoline is an orally active vinca alkaloid. Vindoline can be extracted from the leaves of Catharanthus roseus. Vindoline has a weak inhibitory effect on the self-assembly of tubulin. Vindoline alleviates Apoptosis, inhibits p-p65 and *p-ERK*. Vindoline improves diabetes, bone loss, osteoarthritis, and kidney damage .

HY-N7830

7α,15-Dihydroxydehydroabietic acid	Nanhaia speciosa (Champ. ex Benth.) J. Compton & Schrire Terpenoids Labiatae Diterpenoids Plants Source Classification	ERK
7α,15-Dihydroxydehydroabietic acid is a natural abietane-type diterpenoid with antiangiogenic effects .

HY-W050044R

L-Azetidine-2-carboxylic acid (Standard)	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite PERK Atg8/LC3 Autophagy Bcl-2 Family Apoptosis Eukaryotic Initiation Factor (eIF) ATF6
L-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the PERK pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects .

HY-W010451R

1,2,4-Trihydroxybenzene (Standard) Hydroxyhydroquinone (Standard)	Structural Classification Microorganisms Phenols Polyphenols Source Classification	Reference Standards PERK Potassium Channel Apoptosis Eukaryotic Initiation Factor (eIF)
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the *PERK-eIF2α* signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .

HY-N12561

Pestanoid A	Microorganisms Terpenoids Diterpenoids Source Classification	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-N13201

12-Deoxyphorbol 13-palmitate	Structural Classification Natural Products Euphorbia fischeriana Steud. Euphorbiaceae Plants Source Classification	Apoptosis CDK
12-Deoxyphorbol 13-palmitate is a traditional Chinese medicine monomer with antitumor activity that can be isolated from the root of Euphorbia fischeriana. 12-Deoxyphorbol 13-palmitate induces gastric cancer cell cycle arrest and apoptosis by regulating key cell cycle regulators such as cyclin B、cyclin A and CDC2. In addition, 12-Deoxyphorbol 13-palmitate can significantly weaken *APOL2–SERCA2–PERK–HES1* signaling and slow liver fibrosis by targeting APOL2 .

HY-W097625R

6-Methoxyflavone (Standard)	Structural Classification Flavonoids Flavones Thymelaeaceae Plants Pimelea simplex F.Muell. Source Classification	Toll-like Receptor (TLR) MyD88 p38 MAPK NF-κB Heme Oxygenase (HO) Reference Standards PERK
6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .

Cat. No.	Product Name	Chemical Structure

HY-142283AS

Dosimertinib-d5 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) .

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) .

HY-B0168S

Milnacipran-d10 hydrochloride

Milnacipran-d₁₀ (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (K_i values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .

HY-137813S

PERK-IN-4-d3
PERK-IN-4-d₃ is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .

HY-B0168AS

Milnacipran-d5 hydrochloride

Milnacipran-d₅ hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (K_i values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .

HY-180885S

KRAS G12D-IN-35
KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses *p-ERK* in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .

Targets Recommended: PERK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15001G

Stemregenin 1 SR1	Aryl Hydrocarbon Receptor	Cancer
Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC₅₀ of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the study of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases .

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