Search Result

Pathways Recommended:	Neuronal Signaling JAK/STAT Signaling

Results for "

EGFR signaling

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (83) 5-HT Receptor (2) Akt (36) AMPK (3) Amylases (2) Anaplastic lymphoma kinase (ALK) (4) Apoptosis (57) Autophagy (10) Bacterial (3) Bcl-2 Family (5) BRK (1) c-Met/HGFR (2) Cadherin (1) Calcium Channel (1) CaMK (2) Cannabinoid Receptor (1) Caspase (12) CD276/B7-H3 (2) CDK (5) Complement System (2) COX (1) DNA/RNA Synthesis (2) Drug Metabolite (1) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) ERK (27) FABP (1) FAK (2) Ferroptosis (2) FGFR (2) Fungal (2) GLUT (1) Glycosidase (2) GSK-3 (1) HDAC (1) Hedgehog (1) Hippo (MST) (1) Histone Demethylase (1) HSP (5) IAP (1) IFNAR (2) IGF-1R (2) Interleukin Related (2) IRE1 (2) Isotope-Labeled Compounds (1) JAK (2) JNK (3) LYTACs (1) MDM-2/p53 (3) MEK (2) mGluR (1) Microtubule/Tubulin (3) Mitochondrial Metabolism (2) MMP (4) mTOR (9) MyD88 (1) Necroptosis (1) Neurotensin Receptor (1) NF-κB (6) NOD-like Receptor (NLR) (1) P-glycoprotein (3) p38 MAPK (10) PAK (1) PARP (4) PDGFR (3) PERK (4) PGE synthase (1) Phosphatase (3) PI3K (9) PROTACs (2) Pyroptosis (1) Raf (3) Ras (1) Reactive Oxygen Species (ROS) (6) Reference Standards (6) RET (1) RIG-I-like receptor (RLR) (1) SARS-CoV (1) SHP2 (1) SOD (2) Src (1) STAT (7) Survivin (2) TAM Receptor (1) TGF-β Receptor (2) TNF Receptor (4) Toll-like Receptor (TLR) (1) Topoisomerase (1) TRP Channel (3) Tyrosinase (2) VEGFR (6) Wnt (1) YAP (3)
By Research Areas:	Cancer (101) Cardiovascular Disease (4) Infection (11) Inflammation/Immunology (18) Metabolic Disease (9) Neurological Disease (12)
Click Chemistry:	Alkynes (2)

111

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: RGS Protein EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109061

Lazertinib 3 Publications Verification YH25448; GNS-1480	Apoptosis Akt TRP Channel EGFR ERK	Infection Neurological Disease Metabolic Disease Cancer
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation *EGFR* tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of *EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

HY-N2409

Delphinidin chloride 2 Publications Verification	Apoptosis EGFR JAK STAT	Cardiovascular Disease Cancer
Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC₅₀: 1.3 μM), shutting down downstream signaling cascades .

HY-P99406

Petosemtamab MCLA 158	EGFR	Cancer
Petosemtamab (MCLA 158) is an anti- EGFR (K_d: 0.22 nM) and anti-LGR5 (K_d: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .

HY-141523

Vociprotafib RMC-4630; SHP2-IN-7	SHP2 Phosphatase	Cancer
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .

HY-P9964

Necitumumab 11F8; IMC-11F8; LY3012211	EGFR	Cancer
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against *EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR* phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .

HY-148118A

Tri-GalNAc(OAc)3 TFA	LYTACs	Cancer
Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .

HY-P10408

Candidalysin	EGFR MMP Calcium Channel NOD-like Receptor (NLR) ERK p38 MAPK	Infection Inflammation/Immunology
Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the *EGFR-MAPK* signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity

HY-N1988

Cucurbitacin IIa 1 Publications Verification Hemslecin A	Survivin Apoptosis EGFR Caspase p38 MAPK Autophagy MEK Raf ERK STAT CaMK	Inflammation/Immunology Cancer
Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable *EGFR* inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the *EGFR-MAPK* signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer .

HY-10261B

(E/Z)-Afatinib (E/Z)-BIBW 2992	EGFR Apoptosis c-Met/HGFR Akt p38 MAPK Autophagy	Others Cancer
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .

HY-N1073

Wighteone 1 Publications Verification 6-Isopentenylgenistein; Erythrinin B	Apoptosis EGFR HSP ERK Akt	Infection Cancer
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR ^L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of *EGFR, and thereby inhibits the downstream ERK* and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR ^L858R/T790M mutation, and fungal infections .

HY-131686

Ganglioside GT1b (bovine) ammonium	Akt mTOR EGFR ERK	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Ganglioside GT1b (bovine) ammonium is a member of the ganglioside family. Ganglioside GT1b (bovine) ammonium acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b (bovine) ammonium induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b (bovine) ammonium enhances porcine oocyte maturation and induce activation of *EGFR* and ERK1/2 signaling. Ganglioside GT1b (bovine) ammonium is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b (bovine) ammonium can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease .

HY-13464

ALK-IN-1 Brigatinib analog	Anaplastic lymphoma kinase (ALK) EGFR	Cancer
ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and *EGFR* inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .

HY-P99866

Duligotuzumab MEHD-7945A; RG 7597	EGFR Akt p38 MAPK Apoptosis	Cancer
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting *EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT* and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .

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-109061B

Lazertinib mesylate 3 Publications Verification YH25448 mesylate; GNS-1480 mesylate	TRP Channel EGFR Akt ERK Apoptosis	Cancer
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation *EGFR* tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of *EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

HY-N2510

Myristicin Myristicine	5-HT Receptor EGFR ERK Apoptosis Bacterial	Infection Neurological Disease Inflammation/Immunology Cancer
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the *EGFR/ERK* signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .

HY-157581

MS39	EGFR PROTACs	Cancer
MS39 (compound 6) is a PROTAC targeting *EGFR. MS39 reduces the expression of EGFR* and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells .

HY-P9969

Matuzumab EMD 72000	EGFR	Cancer
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth. Deglycosylation and the possible elimination of ADCC activity can reduce the in vivo anti-tumor activity of Mattuzumab .

HY-137433

Befotertinib 2 Publications Verification D-0316	EGFR P-glycoprotein Apoptosis	Cancer
Befotertinib (D-0316) is an orally active *EGFR* inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR ^T790M, EGFR ^L858R and delE746-A750, forms covalent bonds with EGFR ^C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .

HY-135805

JBJ-04-125-02	EGFR	Cancer
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active *EGFR* inhibitor with an IC₅₀ of 0.26 nM for EGFR ^L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR ^{L858R/T790M/C797S} signaling. JBJ-04-125-02 has anti-tumor activities .

HY-100434

PD-161570	FGFR PDGFR EGFR Src TGF-β Receptor	Cardiovascular Disease Cancer
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, *EGFR* and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively . PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor .

HY-N0891

Tubeimoside II Tubeimoside-B	EGFR TGF-β Receptor RIG-I-like receptor (RLR) SARS-CoV	Infection Neurological Disease Cancer
Tubeimoside II is an orally active triterpenoid saponin and antiviral agent that binds to PACT/PRKRA with K_d values of 5.37 μM and 133.1 μM, respectively. Tubeimoside II inhibits oxidase-dependent *EGFR* activation and reduces TGF-β1-induced oxidative stress. Tubeimoside II activates the RIG-I signaling pathway and increases IFN-β secretion. Tubeimoside II suppresses TPA-induced ear edema, mouse sarcoma 180 growth, and TPA-induced skin tumor formation. Tubeimoside II exerts broad-spectrum antiviral activity against SARS-CoV-2, HCoV-OC43, and IAV-H1N1/FM1. Tubeimoside II can be used in research related to retinoblastoma, respiratory viral infections, skin tumors, and sarcoma 180 .

HY-P99406A

Petosemtamab (FUT8-KO)	EGFR	Cancer
Petosemtamab (FUT8-KO) is an anti-EGFR and anti-LGR5 monoclonal antibody expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucosyl loss enhances the ADCC effect of the antibody. Petosemtamab (FUT8-KO) leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab (FUT8-KO) can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC) .

HY-135699

TD52 2 Publications Verification	Apoptosis Phosphatase Akt	Cancer
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-21291

SU-4313	PDGFR EGFR IGF-1R	Cancer
SU-4313 is a potent protein tyrosine kinases (PTKs) modulator with IC₅₀s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation .

HY-113599

Isoprocurcumenol	EGFR ERK Akt	Others
Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate *EGFR* signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .

HY-N4309

Lotusine	Amylases Glycosidase	Neurological Disease Metabolic Disease Cancer
Lotusine is an orally active signaling pathway modulator and enzyme inhibitor, with an IC₅₀ of 30.60 μg/mL against α-amylase and an IC₅₀ of 36.15 μg/mL against α-glucosidase. Lotusine inhibits the EGFR-Akt-ERK signaling pathway by reducing the levels of phosphorylated EGFR, Akt and ERK. Lotusine induces apoptosis, triggers G₀/G₁ cell cycle arrest and inhibits cancer cell proliferation. Lotusine reduces lipid peroxidation and increases the activities of SOD, CAT and GPx. Lotusine is applicable to researches related to non-small cell lung cancer, type 2 diabetes and autism spectrum disorder .

HY-N6932

Voacamine	Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR	Metabolic Disease Cancer
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits *EGFR* to exert oncogenic activity against colorectal cancer .

HY-135699A

TD52 dihydrochloride 2 Publications Verification	Akt Phosphatase Apoptosis	Cancer
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-160187A

(Rac)-AAA	Cadherin MMP Akt FAK ERK NF-κB	Cancer
(Rac)-AAA is a regulator and inhibitor targeting GPR75. By blocking the 20-HETE-induced downregulation of GPR75 expression, (Rac)-AAA effectively inhibits the activation of key downstream signaling pathways including EGFR, AKT, NF-κB and FAK. (Rac)-AAA reverses 20-HETE-mediated epithelial-mesenchymal transition, which is specifically characterized by downregulating vimentin (vimentin), upregulating E-Cadherin, as well as reducing MMP-2 activity and cancer cell migration ability. (Rac)-AAA also abolishes the 20-HETE-induced upregulation of HIC-5 expression and anchorage-independent growth, and modulates the subcellular localization of PKC-α and phosphorylated AKT. (Rac)-AAA is investigated in androgen-independent prostate cancer (castration-resistant prostate cancer) .

HY-N6577

Astragaloside VI	EGFR	Neurological Disease Inflammation/Immunology
Astragaloside VI could activate *EGFR/ERK* signalling pathway to improve wound healing.

HY-U00002

ZD-4190	VEGFR EGFR	Cancer
ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.

HY-P991571

GC1118 GC-1118A	EGFR PERK Akt	Cancer
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (K_D) to *EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR* ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .

HY-176279

Hsp90-IN-42	HSP	Cancer
Hsp90-IN-42 (Compound 13l) is a potent heat shock protein 90 (Hsp90) inhibitor (IC₅₀=15.65 nM). Hsp90-IN-42 reduces the stability of the epidermal growth factor receptor (EGFR), suppressing the activation of the EGFR-Akt signaling pathway, inducing G0/G1 phase arrest in colorectal cancer cells (such as HT-29 cells), and slightly triggering apoptosis. Hsp90-IN-42 also inhibits cell proliferation and migration by down-regulating the expression of CDK12, CDK13, and Bcl-2 proteins, and up-regulating the expression of Bax protein. Hsp90-IN-42 is promising for research of colorectal cancer .

HY-164548

WK88-1	HSP Apoptosis PI3K Akt NF-κB	Inflammation/Immunology Cancer
WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various *EGFR* mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .

HY-117852

CGP-59326 TRX-13	EGFR Tyrosinase	Cancer
CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC₅₀=0.027 μM). CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers .

HY-P10994

Eps8 peptide 327 Eps8(327-335)	EGFR IFNAR Interleukin Related TNF Receptor Complement System Apoptosis	Inflammation/Immunology Cancer
Eps8 peptide 327 is an HLA-A2402-restricted peptide antigen derived from Eps8 protein. Eps8 peptide 327 has potent antitumor activity with significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cells proliferation, induces apoptosis* and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the *Eps8/EGFR* interaction. Eps8 peptide 327 significantly inhibits tumor growth in HT-29 xenograft mcie models .

HY-123952

RTC-5 TRC-382	EGFR	Cancer
RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an *EGFR* driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling .

HY-123823

Nitroaspirin NCX 4016	COX Apoptosis	Cancer
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins .

HY-178955

EGFR-IN-182	EGFR HSP PI3K Caspase Apoptosis CDK ERK Akt	Cancer
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC₅₀ value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC₅₀ values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .

HY-178057

EGFR-IN-176	EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
EGFR-IN-176 is an orally active and ATP-competitive *EGFR* mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-178939

EGFR-IN-181	EGFR Akt PERK Apoptosis	Neurological Disease Cancer
EGFR-IN-181 is an orally active, potent, brain-penetrant EGFR^{L858R/T790M/C797S} triple mutations inhibitor (IC₅₀ = 1.32 nM). EGFR-IN-181 can inhibit *EGFR* phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .

HY-P991572

MM-151	EGFR	Cancer
MM-151 is a humanized IgG1 monoclonal antibody targeting *EGFR. MM-151 binds multiple regions of the EGFR* extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .

HY-174415

ZSH-2117	PROTACs EGFR Akt ERK	Cancer
ZSH-2117 is a covalent and selective *EGFR* PROTAC degrader with a DC₅₀ of 45 nM in Ba/F3-EGFR ^{L858R/T790M/C797S} cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR ^{L858R/T790M/C797S} xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker

HY-P991092

IBI-334	EGFR CD276/B7-H3	Cancer
IBI-334 is a bispecific B7-H3 and *EGFR* antibody. IBI-334 has an EGFR arm for signal blockage and is coupled with a fine-tuned B7-H3 arm with optimal affinity and binding domain. IBI-334 shows antibody-mediated cell cytotoxicity (ADCC) effects. IBI-334 has a wide range of applications in many EGFR-driven solid tumors .

HY-137433A

Befotertinib mesylate D-0316 mesylate	EGFR P-glycoprotein Apoptosis	Inflammation/Immunology Cancer
Befotertinib (D-0316) mesylate is an orally active *EGFR* inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR ^T790M, EGFR ^L858R and delE746-A750, forms covalent bonds with EGFR ^C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .

HY-120412

SKLB188	EGFR Apoptosis	Cancer
SKLB188 is an orally active and potent epidermal growth factor receptor (EGFR) inhibitor (IC₅₀=5 nM). SKLB188 suppresses MEK/Erk and Akt/mTOR signaling pathways to inhibit head and neck squamous cell carcinoma (HNSCC) proliferation and induce caspase-dependent apoptosis. SKLB188 is promising for research of EGFR-overexpressing solid tumors .

HY-164392

TAS-121	EGFR Apoptosis	Cancer
TAS-121 is an orally active, selective, covalent, third-generation mutant **EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC₅₀=1.7 nM), Ex19del mutation (IC₅₀=2.7 nM), L858R/T790M mutation (IC₅₀=0.56 nM) and Ex19del/T790M mutation (IC₅₀*=1.1 nM) and wild-type EGFR* (IC₅₀=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC₅₀s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .

HY-N2409R

Delphinidin chloride (Standard)	Apoptosis EGFR JAK STAT Reference Standards	Cardiovascular Disease Cancer
Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades .

HY-N2450R

Sulforaphene (Standard)	Reference Standards 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 .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,586 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,586 compounds that act as a useful tool for PTKs-related drug screening and disease research.

HY-L008

JAK/STAT Compound Library

709 compounds

The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokine receptors, a superfamily of more than 30 transmembrane proteins that recognize specific cytokines, and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). Since the JAK/STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK/STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder (SCID).

MCE provides 709 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

HY-L196

Protein Kinase Compound Library

4,400 compounds

Protein Kinases (PTKs) are a class of phosphotransferases that phosphorylate proteins. Protein kinases participate in many signal transduction pathways including those involved with growth, differentiation, and cell division. Protein kinase not only plays an important role in the process of cell activation, but also its abnormal expression is closely related to the pathogenesis of many diseases. So far, the protein kinase family has become one of the most important drug targets. The most common drug targets include ALK, B-Raf, BCR-Abl, EGFR, and VEGFR.

MCE designs a unique collection of 4,400 bioactive compounds targeting protein kinases, which is an important tool for the development of drug targeting protein kinases.

HY-L009

Kinase Inhibitor Library

3,886 compounds

Kinase is an enzyme that adds phosphate groups to other molecules. This process is known as phosphorylation. Protein phosphorylation is a key aspect in the regulation of a large number of cellular processes including cellular division, metabolism, signal transduction, and so on. There are over 500 kinases encoded by the human genome and it has been estimated that kinases regulate approximately 50% of cellular functions. Kinases are a large group of drug targets in drug discovery. Kinase inhibitors are an important class of drugs that block certain enzymes involved in diseases such as cancer and inflammatory disorders.

Kinase inhibitor library designed by MCE contains 3,886 kinase inhibitors and regulators mainly targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.) and carbohydrate kinases (Hexokinase), and is a useful tool for kinase drug discovery and related research.

HY-L009M

Kinase Inhibitor Library Mini

270 compounds

Kinases is a class of enzymes that adds chemicals called phosphates to other molecules, such as sugars or proteins. Protein phosphorylation serves as a critical regulatory mechanism for numerous cellular processes including cell division, metabolism, and signal transduction, with approximately 50% of cellular functions in humans being regulated by kinase activity. In drug discovery, kinases represent a major category of therapeutic targets, and kinase inhibitors constitute an important class of pharmaceuticals that block the activity of specific disease-associated enzymes, particularly in cancer and inflammatory disorders. Small molecule kinase inhibitors represent one of the fastest-growing drug categories, having received U.S. Food and Drug Administration (FDA) approval for both oncological and non-oncological indications. As of September 2023, over 70 FDA-approved small molecule kinase inhibitors are commercially available.

The MCE Kinase Inhibitor Library Mini contains 270 kinase inhibitors primarily targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.), and carbohydrate kinases. This collection includes 1-3 highly specific representative compounds per target, optimized for screening of kinase-related drug targets in pharmaceutical research.

HY-L075

Anti-Lung Cancer Compound Library

2,926 compounds

Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.

As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.

MCE offers a unique collection of 2,926 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Cat. No.	Product Name	Target	Research Area

HY-P10408

Candidalysin	EGFR MMP Calcium Channel NOD-like Receptor (NLR) ERK p38 MAPK	Infection Inflammation/Immunology
Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the *EGFR-MAPK* signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity

HY-P10994

Eps8 peptide 327 Eps8(327-335)	EGFR IFNAR Interleukin Related TNF Receptor Complement System Apoptosis	Inflammation/Immunology Cancer
Eps8 peptide 327 is an HLA-A2402-restricted peptide antigen derived from Eps8 protein. Eps8 peptide 327 has potent antitumor activity with significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cells proliferation, induces apoptosis* and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the *Eps8/EGFR* interaction. Eps8 peptide 327 significantly inhibits tumor growth in HT-29 xenograft mcie models .

HY-P10995

TAT-327	EGFR IFNAR Interleukin Related TNF Receptor Complement System Apoptosis	Inflammation/Immunology Cancer
TAT-327 is cell-penetrating peptide. TAT-327 selectively inserts into cancer cell membranes and shows potent antitumor activity. TAT-327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the *Eps8/EGFR* interaction. TAT-327 significantly inhibits tumor growth in HT-29 xenograft mcie models .

Cat. No.	Product Name	Target	Research Area	Image

HY-P99406

Petosemtamab MCLA 158	EGFR	Cancer
Petosemtamab (MCLA 158) is an anti- EGFR (K_d: 0.22 nM) and anti-LGR5 (K_d: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .

HY-P9964

Necitumumab 11F8; IMC-11F8; LY3012211	EGFR	Cancer
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against *EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR* phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .

HY-P99866

Duligotuzumab MEHD-7945A; RG 7597	EGFR Akt p38 MAPK Apoptosis	Cancer
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting *EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT* and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .

HY-P9969

Matuzumab EMD 72000	EGFR	Cancer
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth. Deglycosylation and the possible elimination of ADCC activity can reduce the in vivo anti-tumor activity of Mattuzumab .

HY-P99406A

Petosemtamab (FUT8-KO)	EGFR	Cancer
Petosemtamab (FUT8-KO) is an anti-EGFR and anti-LGR5 monoclonal antibody expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucosyl loss enhances the ADCC effect of the antibody. Petosemtamab (FUT8-KO) leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab (FUT8-KO) can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC) .

HY-P991571

GC1118 GC-1118A	EGFR PERK Akt	Cancer
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (K_D) to *EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR* ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .

HY-P991572

MM-151	EGFR	Cancer
MM-151 is a humanized IgG1 monoclonal antibody targeting *EGFR. MM-151 binds multiple regions of the EGFR* extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .

HY-P991092

IBI-334	EGFR CD276/B7-H3	Cancer
IBI-334 is a bispecific B7-H3 and *EGFR* antibody. IBI-334 has an EGFR arm for signal blockage and is coupled with a fine-tuned B7-H3 arm with optimal affinity and binding domain. IBI-334 shows antibody-mediated cell cytotoxicity (ADCC) effects. IBI-334 has a wide range of applications in many EGFR-driven solid tumors .

HY-P991234

COVA208	EGFR p38 MAPK PI3K Akt	Cancer
COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer .

HY-P991092A

IBI-334 (FUT8-KO)	EGFR CD276/B7-H3	Cancer
IBI-334 (FUT8-KO) is a bispecific B7-H3 and *EGFR* antibody that has knocked out the fucosyltransferase 8 gene (FUT8). IBI-334 (FUT8-KO) has an EGFR arm for signal blocking and is coupled with a fine-tuned B7-H3 arm with the best affinity and binding domain. IBI-334 (FUT8-KO), compared to IBI-334 (HY-P991092), has enhanced antibody-mediated cytotoxicity (ADCC) effect. IBI-334 (FUT8-KO) has wide applications in many EGFR-driven solid tumors .

HY-P991977

BSI-001 5G9	EGFR Apoptosis PARP Akt ERK	Cancer
BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of *EGFR, HER3, AKT* and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2409

Delphinidin chloride 2 Publications Verification	Cardiovascular Disease Classification of Application Fields Plants Anthocyans Flavonoids Microorganisms other families Solanum melongena L. Phenols Polyphenols Solanaceae Disease Research Fields Source Classification Cancer	Apoptosis EGFR JAK STAT
Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC₅₀: 1.3 μM), shutting down downstream signaling cascades .

HY-N1988

Cucurbitacin IIa 1 Publications Verification Hemslecin A	Triterpenes Structural Classification Classification of Application Fields Terpenoids Cucurbitaceae Plants Hemsleya chinensis Cogn. ex Forbes et Hemsl. Disease Research Fields Source Classification Cancer	Survivin Apoptosis EGFR Caspase p38 MAPK Autophagy MEK Raf ERK STAT CaMK
Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable *EGFR* inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the *EGFR-MAPK* signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer .

HY-N1073

Wighteone 1 Publications Verification 6-Isopentenylgenistein; Erythrinin B	Leguminosae Genista ephedroides DC. Plants Isoflavones Source Classification	Apoptosis EGFR HSP ERK Akt
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR ^L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of *EGFR, and thereby inhibits the downstream ERK* and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR ^L858R/T790M mutation, and fungal infections .

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-N2510

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

HY-N0616

Trifolirhizin	Structural Classification Flavonoids Classification of Application Fields Leguminosae Trifolium pratense Linn. Sophora flavescens Aiton Plants Other Flavonoids Inflammation/Immunology Disease Research Fields Source Classification Cancer	Tyrosinase TNF Receptor Bacterial Apoptosis Autophagy AMPK mTOR ERK NF-κB
Trifolirhizin is a pterocarpan flavonoid found in the roots of Sophora flavescens. Trifolirhizin is a tyrosinase inhibitor with an IC₅₀ value of 506.77 μM. Trifolirhizin reduces intracellular melanin production and modulates multiple signaling pathways including NFκB-MAPK, AMPK/mTOR, PI3K/Akt, MAPK-NFATc1 and EGFR-MAPK. Trifolirhizin targets biological molecules including PTK6 and COX-2, inhibits the activities of hyaluronidase, collagenase and elastase, induces apoptosis, autophagy and cell cycle arrest, and suppresses the proliferation, migration and invasion of cancer cells. Trifolirhizin exerts diverse pharmacological effects including anti-inflammatory, anti-asthmatic, bone-protective, renoprotective, antibacterial, antifungal, hepatoprotective, antiplatelet, estrogenic and wound-healing activities. Trifolirhizin can be used to investigate a broad range of malignant, inflammatory, metabolic and infectious disorders .

HY-N2445

Flavokawain C 4 Publications Verification	Structural Classification Classification of Application Fields Piperaceae Plants Chalcones Flavonoids other families Phenols Polyphenols Piper methysticum G.Forst. Disease Research Fields Source Classification Cancer	Apoptosis Akt JNK PERK Caspase PARP MDM-2/p53 IAP Reactive Oxygen Species (ROS) SOD FABP Autophagy AMPK mTOR GLUT EGFR PI3K HSP VEGFR FAK
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the *EGFR/PI3K/Akt/mTOR* signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .

HY-N0891

Tubeimoside II Tubeimoside-B	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Plants Disease Research Fields Source Classification Cancer	EGFR TGF-β Receptor RIG-I-like receptor (RLR) SARS-CoV
Tubeimoside II is an orally active triterpenoid saponin and antiviral agent that binds to PACT/PRKRA with K_d values of 5.37 μM and 133.1 μM, respectively. Tubeimoside II inhibits oxidase-dependent *EGFR* activation and reduces TGF-β1-induced oxidative stress. Tubeimoside II activates the RIG-I signaling pathway and increases IFN-β secretion. Tubeimoside II suppresses TPA-induced ear edema, mouse sarcoma 180 growth, and TPA-induced skin tumor formation. Tubeimoside II exerts broad-spectrum antiviral activity against SARS-CoV-2, HCoV-OC43, and IAV-H1N1/FM1. Tubeimoside II can be used in research related to retinoblastoma, respiratory viral infections, skin tumors, and sarcoma 180 .

HY-N12445

Quercetin-3'-O-glucoside 1 Publications Verification	Malvaceae Structural Classification Flavonols Flavonoids Abelmoschus manihot (Linn.) Medicus Plants Source Classification	Topoisomerase Caspase Apoptosis SOD
Quercetin-3'-O-glucoside is an orally active flavonoid glycoside. Quercetin-3'-O-glucoside reduces liver glucose-6-phosphatase activity, alters serum insulin and glucose levels, and regulates the activities of antioxidant enzymes in the liver and kidney. Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest and caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Quercetin-3'-O-glucoside selectively inhibits EGFR-mediated signaling pathways targeting AKT, ERK1/2, FAK and MEK1/2. Quercetin-3'-O-glucoside inhibits growth factor-induced migration and invasion in pancreatic cancer cells. Quercetin-3'-O-glucoside exerts free radical scavenging effects. Quercetin-3'-O-glucoside is applicable to research related to pancreatic cancer, diabetes, hepatocellular carcinoma and malignant tumors .

HY-N3000

6-Methoxydihydrosanguinarine	Alkaloids Structural Classification Classification of Application Fields Quinoline Alkaloids Macleaya cordata (Willd.) R. Br. Plants Disease Research Fields Papaveraceae Source Classification Cancer	JNK IRE1 Akt mTOR YAP Reactive Oxygen Species (ROS) Autophagy Apoptosis Ferroptosis Fungal
6-Methoxydihydrosanguinarine is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .

HY-113599

Isoprocurcumenol	Classification of Application Fields Terpenoids Sesquiterpenes Other Diseases Cosmetic Research Plants Disease Research Fields Source Classification Curcuma comosa Roxb. Zingiberaceae	EGFR ERK Akt
Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate *EGFR* signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .

HY-N4309

Lotusine	Cardiovascular Disease Alkaloids Structural Classification other families Classification of Application Fields Phenols Polyphenols Plants Isoquinoline Alkaloids Disease Research Fields Source Classification	Amylases Glycosidase
Lotusine is an orally active signaling pathway modulator and enzyme inhibitor, with an IC₅₀ of 30.60 μg/mL against α-amylase and an IC₅₀ of 36.15 μg/mL against α-glucosidase. Lotusine inhibits the EGFR-Akt-ERK signaling pathway by reducing the levels of phosphorylated EGFR, Akt and ERK. Lotusine induces apoptosis, triggers G₀/G₁ cell cycle arrest and inhibits cancer cell proliferation. Lotusine reduces lipid peroxidation and increases the activities of SOD, CAT and GPx. Lotusine is applicable to researches related to non-small cell lung cancer, type 2 diabetes and autism spectrum disorder .

HY-N6932

Voacamine	Alkaloids other families Classification of Application Fields Metabolic Disease Plants Disease Research Fields Indole Alkaloids Source Classification	Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits *EGFR* to exert oncogenic activity against colorectal cancer .

HY-N6577

Astragaloside VI	Triterpenes other families Leguminosae Terpenoids Astragalus membranaceus var. mongholicus (Bunge)P.K.Hsiao Plants Source Classification	EGFR
Astragaloside VI could activate *EGFR/ERK* signalling pathway to improve wound healing.

HY-N2409R

Delphinidin chloride (Standard)	Structural Classification Anthocyans Flavonoids Microorganisms other families Solanum melongena L. Phenols Polyphenols Solanaceae Plants Source Classification	Apoptosis EGFR JAK STAT Reference Standards
Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades .

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-N2510R

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

HY-N4309A

Lotusine hydroxide	Cardiovascular Disease Alkaloids Classification of Application Fields Phenols Polyphenols Nelumbo nucifera Gaertn. Plants Isoquinoline Alkaloids Nymphaeaceae Disease Research Fields Source Classification	Amylases Glycosidase
Lotusine hydroxide is an orally active signaling pathway modulator and enzyme inhibitor, with an IC₅₀ of 30.60 μg/mL against α-amylase and an IC₅₀ of 36.15 μg/mL against α-glucosidase. Lotusine hydroxide inhibits the EGFR-Akt-ERK signaling pathway by reducing the levels of phosphorylated EGFR, Akt and ERK. Lotusine hydroxide induces apoptosis, triggers G₀/G₁ cell cycle arrest and inhibits cancer cell proliferation. Lotusine hydroxide reduces lipid peroxidation and increases the activities of SOD, CAT and GPx. Lotusine hydroxide is applicable to researches related to non-small cell lung cancer, type 2 diabetes and autism spectrum disorder .

HY-N1988R

Cucurbitacin IIa (Standard) Hemslecin A (Standard)	Triterpenes Structural Classification Terpenoids Cucurbitaceae Plants Hemsleya chinensis Cogn. ex Forbes et Hemsl. Source Classification	Reference Standards Apoptosis EGFR Autophagy MEK Caspase ERK STAT Survivin Raf p38 MAPK CaMK
Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating *EGFR* inhibitor with an IC₅₀ of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the *EGFR-MAPK* signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.

HY-N9684

Degalactotigonin	Plantaginaceae Digitalis purpurea L. Structural Classification Natural Products Plants Source Classification	EGFR GSK-3 Hedgehog Akt ERK Apoptosis
Degalactotigonin is a saponin-selective inhibitor targeting the *EGFR, GSK3β* and Hedgehog/Gli1 pathways and can be isolated from Solanum nigrum (Solanum nigrum). Degalactotigonin inhibits *EGFR* phosphorylation and the downstream Akt/ERK signaling pathway, and at the same time inhibits the Hedgehog/Gli1 pathway through GSK3β inactivation, thereby inducing cancer cell apoptosis, arresting the cell cycle, and inhibiting migration and invasion. Degalactotigonin can be used in targeted research on malignant tumors such as pancreatic cancer and osteosarcoma .

HY-N3000A

6-Methoxydihydrosanguinarine hydrochloride	Structural Classification Alkaloids Meconopsis simplicifolia (D. Don) Walp. Quinoline Alkaloids Plants Papaveraceae Source Classification	JNK IRE1 Akt mTOR YAP Reactive Oxygen Species (ROS) Autophagy Apoptosis Ferroptosis Fungal Caspase DNA/RNA Synthesis
6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .

Cat. No.	Product Name	Chemical Structure

HY-155227S

ALK/EGFR-IN-1-d5

ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC₅₀ of 1.08 nM for EGFR and an IC₅₀ of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment

HY-168968S

ZJY-54
ZJY-54 is an orally active dual-target inhibitor of *EGFR/LSD1, with IC₅₀* values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the *EGFR* signaling pathway. ZJY-54 has anti-tumor activity .

Cat. No.	Product Name		Classification