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A431

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By Targets:	5-HT Receptor (1) ADC Cytotoxin (1) Akt (4) Apoptosis (11) Autophagy (6) Bacterial (4) Btk (1) c-Kit (2) c-Met/HGFR (5) EGFR (30) ERK (1) Estrogen Receptor/ERR (1) FAK (1) FLT3 (2) Fungal (1) Glutathione Peroxidase (1) Necroptosis (1) p38 MAPK (3) Piezo Channel (1) PKA (1) Potassium Channel (1) Proton Pump (3) STING (1) TAM Receptor (2) VEGFR (2) Wnt (1)
By Research Areas:	Cancer (44) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (4) Neurological Disease (1)

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153697

FAK-IN-10	FAK	Cancer
FAK-IN-10 is an inhibitor of FAK with an IC₅₀ of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC₅₀s of 4.23 and 0.78 μM,respectively .

HY-115963

Anticancer agent 38	Others	Cancer
Anticancer agent 38 (compound 19), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 38 inhibits A431 cell growth with an IC₅₀ of 5.2 µg/mL .

HY-157503

Photosensitizer-3	Others	Cancer
Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEK cells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation .

HY-142517

EGFR-IN-25

EGFR Cancer

EGFR-IN-25 is a potent EGFR inhibitor with IC₅₀s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .

EGFR-IN-25	EGFR	Cancer
EGFR-IN-25 is a potent EGFR inhibitor with IC₅₀s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .

HY-144872

RJ-34	Others	Cancer
RJ-34, an aristolactam analogue, exhibits potent antitumor activities against a broad array of cancer cell lines with GI₅₀ values in the subnanomolar range (GI₅₀ <0.1 nM for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells) .

HY-115960

Anticancer agent 35	Others	Cancer
Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 35 inhibits A549, A431, PACA2 cell growth with IC₅₀s of 18.1 µg/mL, 4.0 µg/mL, 18.9 µg/mL, respectively .

HY-160682

EGFR/HER2-IN-12	EGFR	Others
EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .

HY-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 has IC₅₀ value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .

HY-N12606

Neodidymelliosides A	Fungal	Infection
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .

HY-132842

Sunvozertinib 1 Publications Verification DZD9008	EGFR Btk	Cancer
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC₅₀s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .

HY-156912

Tyrosine kinase-IN-7	EGFR	Cancer
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC₅₀s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC₅₀s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .

HY-147826

EGFR-IN-60	EGFR Apoptosis	Cancer
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR ^WT, EGFR ^T790M, EGFR ^L858R and JAK3 with IC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR ^T790M mutation (IC₅₀=1.32 µM) over A431 cells overexpressing EGFR ^WT (IC₅₀=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .

HY-143729

EGFR-IN-29

EGFR Inflammation/Immunology Cancer

EGFR-IN-29 is a potent EGFR inhibitor, example J-022, extracted from Patent WO2021160087 .

EGFR-IN-29	EGFR	Inflammation/Immunology Cancer
EGFR-IN-29 is a potent EGFR inhibitor, example J-022, extracted from Patent WO2021160087 .

HY-128481

SB24011	STING	Cancer
SB24011 is a STING-TRIM29 interaction inhibitor with a IC₅₀ value of 3.85 μM. SB24011 enhances STING immunity by upregating STING protein levels, thereby enhancing the immunotherapy effect of STING agonists and anti-PD-1 antibodies through systemic anticancer immunity .

HY-144044

EGFR-IN-30	EGFR	Cancer
EGFR-IN-30 is a potent EGFR inhibitor with IC₅₀s of 1-10 nM, <1 nM for EGFR (WT), EGFR (L858R/T790M/C797S), respectively. EGFR-IN-30 has potential for cell proliferative diseases, such as cancer research .

HY-138556

GPX4-IN-2

Glutathione Peroxidase Cancer

GPX4-IN-2 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-2 has the potential for the research of cancer .

GPX4-IN-2	Glutathione Peroxidase	Cancer
GPX4-IN-2 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-2 has the potential for the research of cancer .

HY-149846

SIQ17	EGFR	Cancer
SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC₅₀ of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC₅₀ of ∼20 nM). SIQ17 can be used for cancer research

HY-101820

Simotinib

EGFR Cancer

Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC₅₀ of 19.9 nM. Antineoplastic activities .

Simotinib	EGFR	Cancer
Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC₅₀ of 19.9 nM. Antineoplastic activities .

HY-144053

EGFR-IN-36	EGFR	Cancer
EGFR-IN-36 is a potent EGFR inhibitor with IC₅₀s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .

HY-146132

EGFR-IN-55	EGFR	Cancer
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC₅₀ values of 70 nM and 3.9 nM against EGFR ^WT and EGFR ^L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .

HY-119944

JND3229	EGFR	Cancer
JND3229 is a reversible EGFR ^C797S inhibitor with IC₅₀ values of 5.8, 6.8 and 30.5 nM for EGFR ^{L858R/T790M/C797S}, EGFR ^WT and EGFR ^L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .

HY-13016

Cabozantinib 35+ Cited Publications XL184; BMS-907351	VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis	Cancer
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .

HY-135815

Mobocertinib 5+ Cited Publications TAK-788; AP32788	EGFR	Cancer
Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .

HY-135815A

Mobocertinib succinate 5+ Cited Publications TAK-788 succinate; AP32788 succinate	EGFR	Cancer
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .

HY-117152

L-threo-Sphingosine L-threo-Sphingosine C-18	p38 MAPK Apoptosis	Cancer
L-threo-Sphingosine is a potent MAPK inhibitor. L-threo-Sphingosine induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine shows anticancer effect .

HY-13016A

Cabozantinib hydrochloride XL184 hydrochloride; BMS-907351 hydrochloride	VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis	Cancer
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .

HY-135815B

Mobocertinib mesylate TAK-788 mesylate; AP32788 mesylate	EGFR	Cancer
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research .

HY-146210

EGFR-IN-50	EGFR	Cancer
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI₅₀=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI₅₀=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .

HY-P99155

Zalutumumab	EGFR	Cancer
Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC₅₀s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .

HY-157413

YS-67	EGFR	Cancer
YS-67 is a potent inhibitor of EGFR with an IC ₅₀ of 5.2 nM. YS-67 significantly inhibits p-EGFR and p-AKT. YS-67 inhibits the proliferation of A549, PC-9, and A431cells with IC ₅₀s of 4.1, 0.5, and 2.1 μM, respectively .

HY-18723

Yoda 1 20+ Cited Publications	Piezo Channel Akt ERK Potassium Channel	Cardiovascular Disease
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca ²⁺ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .

HY-135901

Py-MPB-amino-C3-PBD	ADC Cytotoxin Bacterial	Cancer
Py-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Py-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity .

HY-150610

EGFR-IN-69	EGFR	Cancer
EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC₅₀ values of 4.3, 6.6 and 25.6 nM against EGFR ^{L858R/T790M/C797S}, EGFR ^L858R/T790M, and EGFR ^{19del/T790M/C797S}, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .

HY-14933

Prinaberel 2 Publications Verification ERB-041	Estrogen Receptor/ERR Wnt Apoptosis	Cancer
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC₅₀s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .

HY-32721

Neratinib 15+ Cited Publications HKI-272	EGFR	Cancer
Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively .

HY-146782

EGFR-IN-49	EGFR	Cancer
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC₅₀s of 65.0 nM and 13.6 nM for EGFR ^T790M and EGFR ^T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .

HY-32721B

Neratinib maleate 15+ Cited Publications HKI-272 maleate	EGFR	Cancer
Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively .

HY-149401

EGFR-IN-82	EGFR	Cancer
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC₅₀ values of 0.09 and 0.06 nM for EGFR ^{L858R/T790M/C797S} and EGFR ^{Del19/T790M/C797S}, respectively. EGFR-IN-82 has no significant effect on EGFR ^WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .

HY-17507

Pantoprazole 3 Publications Verification BY1023; SKF96022	Proton Pump Autophagy Apoptosis Bacterial	Inflammation/Immunology Cancer
Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H ⁺/K ⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) .

HY-17507A

Pantoprazole sodium 3 Publications Verification BY1023 sodium; SKF96022 sodium	Proton Pump Autophagy Apoptosis Bacterial	Inflammation/Immunology Cancer
Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole sodium, a substituted benzimidazole, is a potent H ⁺/K ⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142) .

HY-17507B

Pantoprazole sodium hydrate 3 Publications Verification BY1023 sodium hydrate; SKF96022 sodium hydrate	Proton Pump Autophagy Apoptosis Bacterial	Inflammation/Immunology Cancer
Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H ⁺/K ⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142) .

HY-100923

H-9 Dihydrochloride	PKA 5-HT Receptor EGFR	Neurological Disease
H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines .

HY-116107

AG311

Necroptosis Cancer

AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .

AG311	Necroptosis	Cancer
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on 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-10261

Afatinib Maximum Cited Publications 53 Publications Verification BIBW 2992	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-10261A

Afatinib dimaleate Maximum Cited Publications 53 Publications Verification BIBW 2992MA2	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-10261D

Afatinib oxalate BIBW 2992 oxalate	EGFR Autophagy Apoptosis c-Met/HGFR Akt	Cancer
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

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A431

Inhibitors & Agonists

Inhibitory Antibodies

NaturalProducts

Natural
Products