Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of ofEGFR and ErbB2by inducing internalization of the receptors.
Khellin, a compound isolated from the seeds of Ammi Visnaga Lam (Umbelliferae), is used to treat a variety of maladies.
Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50...
Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.
Sulforaphene, isolated from radish seeds, exhibits an ED50against velvetleaf seedlings approximately 2 x 10-4M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibitingEGFR,p-ERK1/2,NF‐κB and ot...
ZM 449829 is a potent, selective and ATP competitive inhibitor ofJAK3, with apIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of theJAK3.
Beta-hydroxyisovalerylshikonin is a natural product isolated fromLithospermium radix, acts as a potent inhibitor ofprotein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. B...
Cyasterone, a natural EGFR inhibitor, can inhibit the growth of A549 and MGC823 cells, via regulating EGFR signaling pathway, it may be a promising anti-cancer agent. Cyasterone has antifeeding activity.
EMI48, the derivative of EMI1, displays greater potency toward mutantEGFRthan EMI1. EMI48 inhibitsEGFRtriple mutants.
NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.
Tyrphostin AG30 (AG30) is a potent and selectiveEGFR tyrosine kinaseinhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in p...
Lavendustin A (RG-14355), isolated fromStreptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor oftyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEG...
Lavendustin C is a potentCa2+calmodulin-dependent kinase II (CaMK II)inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibitsEGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+)kinase (IC50=0.5 µM).
AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
AG-555 is an inhibitor of tyrosine kinase , interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.
AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM).
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