Search Result

Results for "

EGFR phosphorylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (85) Akt (23) AMPK (1) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (1) Apoptosis (41) Autophagy (4) Bacterial (2) Bcl-2 Family (1) Btk (3) c-Met/HGFR (1) Calcium Channel (2) Cannabinoid Receptor (1) Caspase (2) CDK (4) Cholecystokinin Receptor (2) COX (1) Endogenous Metabolite (1) Epigenetic Reader Domain (2) ERK (22) FABP (1) FAK (3) Ferroptosis (1) FGFR (4) GLUT (1) Glutathione Peroxidase (1) GSK-3 (2) Hedgehog (1) Histone Acetyltransferase (2) Histone Demethylase (1) HMG-CoA Reductase (HMGCR) (1) HSP (2) IAP (1) Interleukin Related (1) Itk (1) JAK (3) JNK (1) MDM-2/p53 (1) Microtubule/Tubulin (1) Mitosis (2) MMP (2) Monoamine Oxidase (1) mRNA (1) mTOR (3) Na+/K+ ATPase (2) NF-κB (1) NO Synthase (1) p38 MAPK (4) PACAP Receptor (2) PARP (3) PD-1/PD-L1 (1) PDGFR (1) PERK (3) Phosphatase (1) PhosTACs (1) PI3K (2) Reactive Oxygen Species (ROS) (4) Reference Standards (7) RET (1) Ribosomal S6 Kinase (RSK) (1) RSV (2) SOD (1) Src (5) STAT (4) Survivin (1) Syk (1) TGF-beta/Smad (2) TGF-β Receptor (1) Transmembrane Glycoprotein (1) Trk Receptor (2) TRP Channel (4) VEGFR (8)
By Research Areas:	Cancer (100) Cardiovascular Disease (4) Infection (8) Inflammation/Immunology (5) Metabolic Disease (6) Neurological Disease (10)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	mRNA (1)

108

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Targets Recommended: Oxidative Phosphorylation EGFR DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-50895

Gefitinib Maximum Cited Publications 200 Publications Verification ZD1839	EGFR Autophagy Apoptosis	Cancer
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

HY-13595

Chrysophanol 5+ Cited Publications Chrysophanic acid	EGFR	Cancer
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

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-P99275

Patritumab 1 Publications Verification AMG-888; U3-1287	EGFR Akt ERK PARP Survivin	Cancer
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of *EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis* and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .

HY-12283

Rostafuroxin 2 Publications Verification PST 2238	Na+/K+ ATPase RSV	Cardiovascular Disease
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na ⁺,K ⁺-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .

HY-17408

Mevastatin Maximum Cited Publications 7 Publications Verification Compactin; ML236B	HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic	Infection Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G₀/G₁ phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment .

HY-101084

NSC 228155 15+ Cited Publications	EGFR Histone Acetyltransferase Epigenetic Reader Domain	Cancer
NSC 228155 is an activator of *EGFR, binds to the extracellular region of EGFR* and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC₅₀ of 0.36 μM .

HY-19816

Avitinib 3 Publications Verification Abivertinib; AC0010	EGFR Btk Apoptosis	Cancer
Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective *EGFR* inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .

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-13302

CP-547632 1 Publications Verification	VEGFR FGFR	Cancer
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .

HY-116624

MAZ51 5+ Cited Publications	VEGFR Apoptosis	Cancer
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .

HY-19816A

Avitinib maleate 3 Publications Verification Abivertinib maleate; AC0010 maleate	EGFR Btk Apoptosis	Cancer
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective *EGFR* inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .

HY-P990957

Ficerafusp alfa BCA-101; FMAB2	EGFR TGF-beta/Smad	Inflammation/Immunology Cancer
Ficerafusp alfa (BCA-101) is a bispecific antibody targeting *EGFR* and TGFβ, with a K_d of 2.58 nM against *EGFR* and a K_d of 61.3 nM against TGFβ1. Ficerafusp alfa binds to EGFR, inhibits EGFR phosphorylation, blocks EGF-dependent cell proliferation, and mediates antibody-dependent cellular cytotoxicity against *EGFR*-positive tumor cells. Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizes the activity of TGFβ and TGFβ1, and blocks TGFβ-dependent processes, including epithelial-mesenchymal transition, cell invasion, and differentiation of inducible regulatory T cells. Ficerafusp alfa is applicable to research related to head and neck squamous cell carcinoma, advanced solid tumors, squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer .

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-P991558

RO-5429083 RG-7356	Transmembrane Glycoprotein	Cancer
RO-5429083 (RG-7356) is a humanized monoclonal antibody targeting CD44. RO-5429083 binds to the extracellular domain of CD44 and inhibits constitutive *EGFR* phosphorylation. RO-5429083 suppresses tumor growth in xenograft models and can be used in research related to head and neck squamous cell carcinoma and acute myeloid leukemia .

HY-W062835

CGP77675	Src	Cancer
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity .

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-12029

WZ8040	EGFR	Cancer
WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits **EGFR phosphorylation*. WZ8040 displays 100-fold greater activity against the mutated EGFR* than the normal .

HY-157229

STX-721 1 Publications Verification	EGFR ERK	Cancer
STX-721 is an orally active, irreversible, covalent *EGFR* exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of *EGFR* (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .

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-161408

GePhos1 1 Publications Verification	PhosTACs EGFR Apoptosis	Cancer
GePhos1, a *EGFR*-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis .

HY-103443

HKI-357	EGFR	Cancer
HKI-357 is an irreversible dual inhibitor of *EGFR* and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .

HY-134877

BAY 2476568	EGFR ERK Akt	Cancer
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC₅₀ values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits *EGFR* (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .

HY-115452

G5-7	JAK Apoptosis	Cancer
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr ¹⁰⁶⁸) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .

HY-20878

Tyrphostin AG 879 3 Publications Verification AG 879	Trk Receptor EGFR Apoptosis	Cancer
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC₅₀ of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC₅₀ of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .

HY-161275

BI-4732	EGFR Akt ERK Ribosomal S6 Kinase (RSK)	Cancer
BI-4732 is an orally active, reversible, ATP-competitive *EGFR* inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of *EGFR* L858R, T790M and C797S with IC₅₀ values of 1 nM while sparing *EGFR* wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring *EGFR*_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-137191

CH7233163	EGFR	Cancer
CH7233163 is a noncovalent ATP-competitive inhibitor for *EGFR*-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .

HY-150611

EGFR-IN-70	EGFR	Cancer
EGFR-IN-70 (compound 18j) is a potent *EGFR* inhibitor with IC₅₀ values of 23.6 and 307.5 nM for EGFR ^LR/TM/CS and EGFR ^WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .

HY-112474

Tyrphostin AG 112	EGFR	Cancer
Tyrphostin AG 112 is an **EGFR phosphorylation** inhibitor .

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-147183A

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

HY-147183B

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

HY-115605

CN009543V	EGFR p38 MAPK ERK Phosphatase	Cancer
CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research .

HY-124674A

CCT365623 hydrochloride 1 Publications Verification	Monoamine Oxidase EGFR Akt TGF-beta/Smad	Cancer
CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC₅₀ of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .

HY-13302B

CP-547632 hydrochloride 1 Publications Verification	VEGFR FGFR	Cancer
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .

HY-111553

TAS0728	EGFR	Cancer
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for *BMX、HER4、BLK、EGFR、JAK3、SLK* and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors .

HY-147183

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

HY-103441

JNJ28871063 hydrochloride	EGFR	Cancer
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC₅₀ values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .

HY-179143

EGFR-IN-185	EGFR Akt Apoptosis	Cancer
EGFR-IN-185 is a *EGFR* inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of NSCLC .

HY-175837

EGFR-IN-172	EGFR Apoptosis	Cancer
EGFR-IN-172 is a *EGFR* inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC .

HY-129510

4-Methyl erlotinib	EGFR Mitosis	Cancer
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

HY-13595R

Chrysophanol (Standard) Chrysophanic acid (Standard)	Reference Standards EGFR	Cancer
Chrysophanol (Standard) is the analytical standard of Chrysophanol. This product is intended for research and analytical applications. Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

HY-105226

CI-988 PD134308	Cholecystokinin Receptor	Neurological Disease Cancer
CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC₅₀ of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .

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-130616

EGFR-IN-11	EGFR Apoptosis	Cancer
EGFR-IN-11 is a fourth-generation *EGFR*-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR ^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-178283

EGFR-IN-177	EGFR	Cancer
EGFR-IN-177 is a potent *EGFR* inhibitor with IC₅₀s of 0.32, 1.04, 0.65, 0.67, 0.48, 0.55 and 0.38 nM against EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S, EGFR D746-750, EGFR D746-750/C797S, EGFR D770_N77linsNPG, and EGFR WT. EGFR-IN-177 inhibits lung cancer proliferation and EGFR phosphorylation. EGFR-IN-177 can be used for the study of cancers such as non-small cell lung cancer .

HY-175864

EGFR-IN-173	EGFR Apoptosis p38 MAPK ERK Akt STAT	Inflammation/Immunology Cancer
EGFR-IN-173 is an orally active, pan-mutant *EGFR* tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR ^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .

HY-164527

Si306	Src FAK EGFR	Cancer
Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM) .

HY-178448

EGFR-IN-178	EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase	Inflammation/Immunology Cancer
EGFR-IN-178 is an orally active *EGFR* mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the *EGFR* enzyme, including Del19 (IC₅₀ = 3.4 nM), L858R/T790 M (IC₅₀ = 2.9 nM), and Del19/T790 M (IC₅₀ = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC₅₀ = 55.6 nM) and JAK3 (IC₅₀ = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .

Cat. No.	Product Name

HY-L009

Kinase Inhibitor Library

3,849 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 3,849 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.

Cat. No.	Product Name	Target	Research Area

HY-P0221

PACAP (1-38), human, ovine, rat 5 Publications Verification Pituitary Adenylate Cyclase Activating Polypeptide 38	PACAP Receptor ERK EGFR Reactive Oxygen Species (ROS) Calcium Channel	Infection Neurological Disease
PACAP (1-38), human, ovine, rat is a PAC₁ receptor agonist. PACAP (1-38), human, ovine, rat binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC₅₀s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat increases the α-secretase activity. PACAP (1-38), human, ovine, rat elevates cytosolic Ca ²⁺, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat can be used for neurotrophic and neuroprotective research .

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-P0221A

PACAP (1-38), human, ovine, rat TFA Pituitary Adenylate Cyclase Activating Polypeptide 38 TFA	PACAP Receptor ERK EGFR Reactive Oxygen Species (ROS) Calcium Channel	Neurological Disease
PACAP (1-38), human, ovine, rat TFA is a PAC₁ receptor agonist. PACAP (1-38), human, ovine, rat TFA binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC₅₀s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat TFA increases the α-secretase activity. PACAP (1-38), human, ovine, rat TFA elevates cytosolic Ca ²⁺, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat TFA can be used for neurotrophic and neuroprotective research .

Cat. No.	Product Name	Target	Research Area	Image

HY-P99275

Patritumab 1 Publications Verification AMG-888; U3-1287	EGFR Akt ERK PARP Survivin	Cancer
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of *EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis* and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .

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-P990957

Ficerafusp alfa BCA-101; FMAB2	EGFR TGF-beta/Smad	Inflammation/Immunology Cancer
Ficerafusp alfa (BCA-101) is a bispecific antibody targeting *EGFR* and TGFβ, with a K_d of 2.58 nM against *EGFR* and a K_d of 61.3 nM against TGFβ1. Ficerafusp alfa binds to EGFR, inhibits EGFR phosphorylation, blocks EGF-dependent cell proliferation, and mediates antibody-dependent cellular cytotoxicity against *EGFR*-positive tumor cells. Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizes the activity of TGFβ and TGFβ1, and blocks TGFβ-dependent processes, including epithelial-mesenchymal transition, cell invasion, and differentiation of inducible regulatory T cells. Ficerafusp alfa is applicable to research related to head and neck squamous cell carcinoma, advanced solid tumors, squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer .

HY-P991558

RO-5429083 RG-7356	Transmembrane Glycoprotein	Cancer
RO-5429083 (RG-7356) is a humanized monoclonal antibody targeting CD44. RO-5429083 binds to the extracellular domain of CD44 and inhibits constitutive *EGFR* phosphorylation. RO-5429083 suppresses tumor growth in xenograft models and can be used in research related to head and neck squamous cell carcinoma and acute myeloid leukemia .

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 .

HY-P992341

D8P1C1	MMP	Cancer
D8P1C1 is a high-affinity ADAM17 inhibitor (with a K_d of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of *EGFR* ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. ⁸⁹Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13595

Chrysophanol 5+ Cited Publications Chrysophanic acid	Quinones Rheum palmatum L. Classification of Application Fields Anthraquinones Polygonaceae Phenols Polyphenols Plants Disease Research Fields Source Classification Cancer	EGFR
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

HY-17408

Mevastatin Maximum Cited Publications 7 Publications Verification Compactin; ML236B	Infection Cardiovascular Disease Natural Products Microorganisms Neurological Disease Classification of Application Fields Metabolic Disease Disease Research Fields Source Classification	HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic
Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G₀/G₁ phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment .

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-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-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-13595R

Chrysophanol (Standard) Chrysophanic acid (Standard)	Quinones Rheum palmatum L. Classification of Application Fields Polygonaceae Phenols Plants Disease Research Fields Source Classification Cancer	Reference Standards EGFR
Chrysophanol (Standard) is the analytical standard of Chrysophanol. This product is intended for research and analytical applications. Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

HY-N16557

(Rac)-8-Gingerol	Structural Classification Natural Products Phenols Plants Source Classification Zingiberaceae	Apoptosis EGFR STAT PERK
(Rac)-8-Gingerol is a non-volatile component. (Rac)-8-Gingerol can be extracted from ginger. (Rac)-8-Gingerol enhances Apoptosis. (Rac)-8-Gingerol decreases the level of phosphorylated *EGFR* and, accordingly, the phosphorylation levels of its downstream effectors, STAT3 and ERK. (Rac)-8-Gingerol exhibits anticancer activity against colorectal cancer .

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 .

Cat. No.	Product Name	Chemical Structure

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