erbb-2

EGFR ErbB-2 ErbB-4 inhibitor-2 (EGFR ErbB2 Inhibitor) is a cell-permeable compound that inhibits EGFR and c-ErbB2 with IC50 values of 20 nM and 79 nM, respectively.

EGFR ErbB-2 inhibitor-1 is a selective ErbB2 HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.

ErbB-2-binding peptide (HER2-binding peptide), a tumor-targeting peptide, shows significant potential for cancer research applications [1].

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.

ERBB agonist-1 (Compound EF-1) is an ERBB4 agonist that activates the ERBB4 signaling pathway by inducing ERBB4 receptor dimerization, with an EC50 of 10.5 μM. It promotes phosphorylation of Akt and ERK1 2, reduces collagen expression in cardiac fibroblasts, and inhibits H2O2-induced cardiomyocyte death and Ang II-induced cardiac hypertrophy. Furthermore, ERBB agonist-1 can prevent myocardial fibrosis and demonstrates cardioprotective effects in mouse models.

SU5204 (3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one), an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)

Lapatinib tosylate (GW572016), a robust and orally administered inhibitor specifically targeting the tyrosine kinase domains of ErbB-2 and EGFR, exhibits inhibitory concentration 50 (IC50) values of 10.2 nM and 9.8 nM against purified EGFR and ErbB-2, respectively.

2'-Thioadenosine (PD157432) serves as a selective and irreversible inhibitor of ErbB-1 and ErbB-2 tyrosine kinases, demonstrating an IC50 value of 45 µM against ErbB-2. It achieves covalent inactivation of ErbB-1 through modification of a cysteine residue within the enzyme's active site [1].

(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR HER2 inhibitor.

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

Sulforaphene is a natural product 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 signa