pERK activation

By Targets:	PERK (5) Akt (1) Apoptosis (5) Autophagy (2) DGK (2) ERK (1) Eukaryotic Initiation Factor (eIF) (1) GnRH Receptor (1) Histamine Receptor (1) Isotope-Labeled Compounds (1) MEK (1) mGluR (1) Microtubule/Tubulin (1) PKC (1) Raf (1)
By Research Areas:	Cancer (13) Endocrinology (1) Metabolic Disease (2) Neurological Disease (4)

Targets Recommended: PERK FAP LAG-3

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-119240

CCT020312

15+ Cited Publications

PERK Autophagy Neurological Disease Cancer

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.

CCT020312 15+ Cited Publications	PERK Autophagy	Neurological Disease Cancer
CCT020312 is a selective *EIF2AK3/PERK* activator. CCT020312 elicits EIF2A phosphorylation in cells.

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-107415

PLX7922

Raf Cancer

PLX7922, a RAF inhibitor, can bind with BRAF ^V600E. PLX7922 inhibits pERK in BRAF ^V600E cell lines, and activates pERK in mutant NRAS cell lines .

PLX7922	Raf	Cancer
PLX7922, a RAF inhibitor, can bind with BRAF ^V600E. PLX7922 inhibits pERK in BRAF ^V600E cell lines, and activates pERK in mutant NRAS cell lines .

HY-137207

MK-28 3 Publications Verification	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-137813S

PERK-IN-4-d3	Isotope-Labeled Compounds PERK	Neurological Disease Metabolic Disease Cancer
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 IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].

HY-153343

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-153343A

(S)-BAY 2965501	DGK ERK	Cancer
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). 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-101991

ML291	PERK Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the *PERK/eIF2a/CHOP* (apoptotic) arm of the UPR and reduce leukemic cell burden .

HY-105173

Teverelix EP 24332	GnRH Receptor Histamine Receptor	Endocrinology Cancer
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer .

HY-10254

Mirdametinib Maximum Cited Publications 82 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-147513

AKT-IN-12	Akt Apoptosis	Cancer
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC₅₀ value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .

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-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-149918

Antiproliferative agent-23	Microtubule/Tubulin Apoptosis	Cancer
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .

Cat. No.	Product Name

HY-L054

Endoplasmic Reticulum Stress Compound Library	219 compounds
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer. MCE Endoplasmic Reticulum Stress Compound Library contains 219 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.

Endoplasmic Reticulum Stress Compound Library

219 compounds

Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.

MCE Endoplasmic Reticulum Stress Compound Library contains 219 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.

Cat. No.	Product Name	Target	Research Area

HY-105173

Teverelix EP 24332	GnRH Receptor Histamine Receptor	Endocrinology Cancer
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer .

Cat. No.	Product Name	Chemical Structure

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 IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].

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Isotope-Labeled Compounds

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