HER

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

PF-04929113 Mesylate (SNX-5422 Mesylate), a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).

BMS 599626 2HCl (873837-23-1(HCl)) (AC480 dihydrochloride) is a selective inhibitor of HER1 and HER2 (IC50s: 20 nM and 30 nM), ~8-fold less potent to HER4, >100-fold to Lck, VEGFR2, c-Kit, MET, etc.

BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.

Panomifene HCl is a selective anti-estrogenic compound with antitumor activity for the treatment of breast cancer.

SYR127063 (BDBM-92454) (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.

Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

AG-1557 hydrochloride is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).

Sarizotan HCl (EMD 128130 HCl) is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinson's Dyskinesia.

EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.

AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.

Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).

Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

ARRY-380 analog (HER2-Inhibitor-1) is a potent and selective HER2 inhibitor.

Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-small cell lung cancer.

RG14620 (Tyrphostin RG14620) is an epidermal growth factor receptor (EGFR) inhibitor.

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.

HER2/neu (654-662) GP2 acetate is derived from the human epidermal growth factor receptor 2 (HER2-Neu, 654–662). HER2/neu (654-662) GP2 acetate induces HLA-A2-restricted cytotoxic T lymphocytes reactive to various epithelial cancers.

Epertinib hydrochloride (S-22611 hydrochloride) shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively.

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively.

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer.

1. Furanodienone has effects on MCF-7 cells are mediated, at least in part, by inhibiting ERα signaling. 2. Furanodienone inhibits EGFR/HER2 signaling pathway in BT474 and SKBR3 cells, the effect is specifically dependent on the expression of HER2 but not EGFR .

O-Nornuciferine reveals distinct in vitro hERG blockages measured in HEK293 cells with the IC50 value of 2.89 uM.

Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces Hsp90 expression and its interaction with hERG.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activity.

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

TAS0728 is a HER2 inhibitor, with antitumor activity

Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).

PF04929113 (SNX-5422) is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, PF04929113 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.

Tucatinib hemiethanolate (Irbinitinib hemiethanolate) is an orally active, selective and potent tyrosine kinase inhibitor targeting human epidermal growth factor receptor 2 (HER2) with anticancer activity for the study of metastatic HER2-positive breast and colorectal cancers.

AG1557 (AG-1557) is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).

AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM. AZD-5672 inhibits hERG cardiac ion channel binding and P-gp-mediated digoxin transport with IC50s of 7.3 μM and 32 μM. AZD-5672 can be used in studies about rheumatoid arthritis.

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

MCHR1 antagonist 2 is an antagonist of melanin-concentratin hormone receptor 1(MCH1-R, IC50 = 65 nM) and also inhibits hERG.

BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 Hydrochloride inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.