Search Result

Results for "

pERK

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PERK (63) Acyltransferase (2) Akt (15) AMPK (1) Anaplastic lymphoma kinase (ALK) (1) Angiotensin Receptor (2) AP-1 (1) Apoptosis (60) ATF6 (2) Atg8/LC3 (6) Autophagy (17) Bcl-2 Family (9) Bcr-Abl (1) Btk (1) c-Met/HGFR (1) Cannabinoid Receptor (3) Carnitine Palmitoyltransferase (CPT) (2) Caspase (13) CDK (3) COX (1) CXCR (1) Cyclophilin (1) DAPK (1) DGK (2) DNA/RNA Synthesis (2) Dopamine Receptor (1) Drug Derivative (1) EGFR (11) Endogenous Metabolite (3) Epigenetic Reader Domain (2) ERK (37) Eukaryotic Initiation Factor (eIF) (12) Ferroptosis (3) FGFR (4) FLT3 (5) Fungal (1) GnRH Receptor (1) HDAC (1) Heme Oxygenase (HO) (2) HIF/HIF Prolyl-Hydroxylase (1) Histamine Receptor (1) HSP (4) iGluR (1) Interleukin Related (1) IRE1 (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (4) JAK (3) JNK (8) Keap1-Nrf2 (1) Lipase (1) LPL Receptor (1) MDM-2/p53 (3) MEK (10) mGluR (3) Microtubule/Tubulin (6) Mitochondrial Metabolism (1) Mitogen- and Stress-Activated Protein Kinase (MSK) (1) MMP (2) Molecular Glues (3) mTOR (3) MyD88 (1) NF-κB (9) NO Synthase (1) Nuclear Hormone Receptor 4A/NR4A (3) P-glycoprotein (1) p38 MAPK (15) p62 (5) PARP (2) PD-1/PD-L1 (3) Phosphatase (3) Phosphodiesterase (PDE) (1) PI3K (6) PKC (2) Potassium Channel (3) Prostaglandin Receptor (1) PROTACs (13) Protease Activated Receptor (PAR) (1) Protein Arginine Deiminase (1) Pyroptosis (2) Raf (7) RAR/RXR (1) Ras (39) Reactive Oxygen Species (ROS) (19) Reference Standards (13) ROS Kinase (1) Serotonin Transporter (5) SHP2 (10) 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) Thrombin (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) Trk Receptor (1) VDAC (1) VEGFR (5)
By Research Areas:	Cancer (161) Cardiovascular Disease (12) Endocrinology (6) Infection (3) Inflammation/Immunology (16) Metabolic Disease (14) Neurological Disease (22)
Click Chemistry:	Alkynes (4)
Oligonucleotides:	Mouse Pre-designed siRNA Sets (2) Human Pre-designed siRNA Sets (1) siRNAs (3)

188

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Oligonucleotides

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-148439

Daraxonrasib 5+ Cited Publications RMC-6236; RAS-IN-2	Ras PERK	Cancer
Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC₅₀ values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits *pERK*. Daraxonrasib has anti-tumor activity against KRAS mutant tumors .

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-15816

Ulixertinib 45+ 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-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-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-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-119240

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

HY-N0878

Bufotalin 4 Publications Verification	Apoptosis Reactive Oxygen Species (ROS)	Cancer
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .

HY-15816A

Ulixertinib hydrochloride 45+ 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-100548

GSK621 5+ Cited Publications	AMPK Autophagy Apoptosis	Cancer
GSK621 is a specific AMPK activator, with IC₅₀ values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation .

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-153181

Trametiglue 1 Publications Verification	MEK	Cancer
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions .

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-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-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-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-137092

IACS-13909 3 Publications Verification	SHP2 Phosphatase	Cancer
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC₅₀ of 15.7 nM and a K_d of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .

HY-W010451

1,2,4-Trihydroxybenzene Hydroxyhydroquinone	PERK Eukaryotic Initiation Factor (eIF) Potassium Channel Apoptosis	Cardiovascular Disease Cancer
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-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-136390

ML417 1 Publications Verification	Dopamine Receptor	Neurological Disease
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC₅₀ of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons .

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-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-168669

PROTAC K-Ras Degrader-5	PROTACs Ras Caspase ERK	Cancer
PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC₅₀ of <100 nM for KRAS ^G12D. PROTAC K-Ras Degrader-5 recruits KRAS ^G12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses *pERK* levels downstream of KRAS ^G12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer .

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-153663

TH-Z827	Ras	Cancer
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC₅₀ of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC₅₀ value of 42 μM .

HY-159795

Claturafenib PF-07799933; ARRY-440	Raf PERK	Cancer
Claturafenib ( PF-07799933) is an orally active inhibitor of pan-mutant BRAF. Claturafenib inhibits *pERK* in cells (IC₅₀ value of 1.6 nM in HT29 cells). Claturafenib has anticancer activity against BRAF ^G469A mutant NSCLC and BRAF ^K601E mutant melanoma .

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-145702

MAP855	MEK ERK	Cancer
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC₅₀=3 nM, pERK EC₅₀=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .

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-138294

RAS/RAS-RAF-IN-1 2 Publications Verification	Ras Raf	Cancer
RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a K_D of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity .

HY-153343A

(S)-Veludacigib (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-12736A

GSK143 dihydrochloride 1 Publications Verification	Syk ERK	Inflammation/Immunology Cancer
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1) . GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .

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-161235

BTX-7312	SOS1 Molecular Glues Ras	Cancer
BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers *pERK* and pS6 and shows antiproliferative activity in various KRAS-mutated cells .

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-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-P11162

FGF7p	FGFR Akt ERK mTOR Apoptosis	Inflammation/Immunology
FGF7p is a small molecule peptide and a potential bladder protector. FGF7p can activate downstream signaling pathways of FGFR2 in the urinary tract epithelium (pFRS2α, pAKT and pERK). FGF7p alleviates cyclophosphamide induced apoptosis and tissue damage in urinary tract epithelial cells by activating AKT and its downstream anti apoptotic targets (pBAD, pS6/mTORC1). FGF7p is commonly used in the study of inflammatory conditions .

HY-175880

AMG-34	Eukaryotic Initiation Factor (eIF)	Cancer
AMG-34 is a GCN2-targeting agent with IC₅₀ values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, *PERK, HRland PKR*, respectively .

HY-161233A

BTX-6654 formate	PROTACs SOS1 ERK	Cancer
BTX-6654 formate is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 formate reduces downstream signaling markers *pERK* and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .

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-179443

SOS1-IN-25	SOS1 Ras	Cancer
SOS1-IN-25 is an SOS1 inhibitor. SOS1-IN-25 exhibits inhibitory activity against KRAS ^G12C/SOS1 complex formation (IC₅₀ = 11.11 nM). SOS1-IN-25 leads to a dose-dependent decrease in pERK levels. SOS1-IN-25 can be used for the study of leukemia .

HY-144657A

(4S)-PROTAC SOS1 degrader-1 diTFA	PROTACs Ras	Cancer
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .

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-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-161233

BTX-6654	PROTACs SOS1 ERK	Cancer
BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers *pERK* and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .

HY-12736

GSK143	Syk ERK	Inflammation/Immunology Cancer
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC₅₀=7.1) . GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .

HY-153160

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

Cat. No.	Product Name

HY-L054

Endoplasmic Reticulum Stress Compound Library

356 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 356 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-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-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-P11162

FGF7p	FGFR Akt ERK mTOR Apoptosis	Inflammation/Immunology
FGF7p is a small molecule peptide and a potential bladder protector. FGF7p can activate downstream signaling pathways of FGFR2 in the urinary tract epithelium (pFRS2α, pAKT and pERK). FGF7p alleviates cyclophosphamide induced apoptosis and tissue damage in urinary tract epithelial cells by activating AKT and its downstream anti apoptotic targets (pBAD, pS6/mTORC1). FGF7p is commonly used in the study of inflammatory conditions .

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-P11011A

Peptide R54 acetate Pep R54 acetate; CXCR4 antagonist peptide 19 acetate	CXCR ERK Akt	Cancer
Peptide R54 acetate (Pep R54 acetate) is a CXCR4 antagonist. Peptide R54 acetate inhibits CXCL12-dependent activation of *pERK1/2* and pAKT. The combination of Peptide R54 acetate and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer .

Cat. No.	Product Name	Target	Research Area	Image

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 .

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-N0878

Bufotalin 4 Publications Verification	Animals Classification of Application Fields Disease Research Fields Steroids Source Classification Cancer	Apoptosis Reactive Oxygen Species (ROS)
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .

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-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-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-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-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-N0878R

Bufotalin (Standard)	Structural Classification Animals Steroids Source Classification	Reference Standards Apoptosis Reactive Oxygen Species (ROS)
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .

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-123647

Satratoxin H	Structural Classification Natural Products Microorganisms Source Classification	Endogenous Metabolite p38 MAPK JNK Caspase PARP ERK Apoptosis Reactive Oxygen Species (ROS)
Satratoxin H is a toxic metabolite of Stachybotrys atra. Satratoxin H induces caspase-3 and PARP cleavage via p38 MAPK and JNK pathways, stimulates JNK, ERK, and p38 MAPK phosphorylation, and activates JNK and p38 MAPK in a glutathione-sensitive manner. Satratoxin H induces DNA double-stranded breaks, apoptotic body formation, intracellular reactive oxygen species generation, and endoplasmic reticulum stress via ATF6, *PERK, and IRE1* pathways. Satratoxin H can be used for the research of central nervous system disorders and melanoma .

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 .

Host:	Mouse (1) Rabbit (5)
Reactivity:	Human (4) Rat (6) Mouse (6)
Application:	IHC-P (1) ICC/IF (3) IP (1) IHC-F (1) WB (6) FC (1) ELISA (3)
Isotype:	IgG, Kappa (1) IgG (4) IgG1 (1)
Conjugation:	Non-conjugated (6)
Clonality:	Polyclonal (1) Monoclonal (4) Recombinant (2)
Modification:	Phosphorylated (2) Unmodified (3)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P85324

	PERK Antibody (YA5016) EIF2AK3; PEK; pERK; Eukaryotic translation initiation factor 2-alpha kinase 3; PRKR-like endoplasmic reticulum kinase; Pancreatic eIF2-alpha kinase; HsPEK	WB, ELISA	Mouse, Rat
	PERK Antibody (YA5016) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to PERK.

HY-P86542

	PERK Antibody (YA6234) EIF2AK3; PEK; pERK; Eukaryotic translation initiation factor 2-alpha kinase 3; PRKR-like endoplasmic reticulum kinase; Pancreatic eIF2-alpha kinase; HsPEK	WB, ICC/IF, IP, ELISA	Human, Mouse, Rat
	PERK Antibody (YA6234) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PERK.

HY-P87807

	*Phospho-PERK* (Thr980) Antibody (YA7492)**	WB, ICC/IF, ELISA	Mouse, Rat
	Phospho-PERK (Thr980) Antibody (YA7492) is a Rabbit-derived and non-conjugated IgG, Kappa monoclonal antibody, targeting to Phospho-PERK (Thr980).

HY-P80781

	PERK Antibody (YA233) EIF2AK3; PEK; pERK; Eukaryotic translation initiation factor 2-alpha kinase 3; PRKR-like endoplasmic reticulum kinase; Pancreatic eIF2-alpha kinase; HsPEK	WB	Human, Mouse, Rat
	PERK Antibody (YA233) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PERK.

HY-P81190

	*Phospho-PERK* (Thr980) Antibody** 2 Publications Verification p-pERK(Thr980); pERK(Phospho Thr980); pERK(Phospho T980); mo(Thr980)/hu (Thr982)/rat (Thr974); HRI; HsPEK; Pancreatic eIF2-alpha kinase; PEK; PRKR like endoplasmic reticulum kinase; WRS; DKFZp781H1925; EC 2.7.11.1; EIF2AK3; Eukaryotic translation initiation factor 2 alpha kinase 3; Heme regulated EIF2 alpha kinase.	WB, IHC-P, IHC-F, ICC/IF, FC	Human, Mouse, Rat
	Phospho-PERK (Thr980) Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to Phospho-PERK (Thr980).

HY-P80781A

	PERK Antibody (YA233)(PBS only) EIF2AK3; PEK; pERK; Eukaryotic translation initiation factor 2-alpha kinase 3; PRKR-like endoplasmic reticulum kinase; Pancreatic eIF2-alpha kinase; HsPEK	WB	Human, Mouse, Rat
	PERK Antibody (YA233) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PERK.

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Cat. No.	Product Name		Classification

HY-176786

MCB-36		Alkynes
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-179300

KRAS-IN-48 free base		Alkynes
KRAS-IN-48 free base (Compound 1-01) is a mutant KRAS inhibitor, with K_d values of 2.58 nM and 5.49 μM for KRAS G12D and KRAS G12V, respectively. KRAS-IN-48 free base affects *pERK* expression in cells harboring KRAS G12D and KRAS G12V mutations, with IC₅₀ values of 1.1 μM and 1.51 μM, respectively. KRAS-IN-48 free base can be used in the research of cancer .

HY-180920

KRAS G12D-IN-36		Alkynes
KRAS G12D-IN-36 (Compound 53a) is a highly selective and orally active KRAS-G12D inhibitor with an IC₅₀ of 1.63 nM. KRAS G12D-IN-36 effectively inhibits p-ERK with an IC₅₀ of 8.4 nM. KRAS G12D-IN-36 shows potent anti-proliferative activity against AsPC-1 cells. KRAS G12D-IN-36 can be used for research on pancreatic cancer .

HY-180200

RNK08954		Alkynes
RNK08954 is an orally active KRAS^G12D inhibitor with a K_d of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRAS^G12D form, suppresses downstream KRAS-mediated signaling pathways *p-ERK1/2* experssion. RNK08954 inhibits KRAS^G12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .

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