Catalog name Description price
R-C-1052 AMG-47a CAS No. 882663-88-9 AMG-47a is a potent,nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation.AMG-47a exhibit anti-inflammatory activity(ED50)of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2)in mice. price>
R-C-1077 PF-431396 CAS:717906-29-1 PF-431396 hydrate has been used as a dual inhibitor of proline-rich tyrosine kinase 2(PYK2)/focal adhesion kinase(FAK)inhibitor to study its effects on phosphorylation of Yes-associated protein(YAP)at Ser127 and steady state of transcriptional coactivator with PDZ-binding motif(TAZ).It has also been used as a PYK2/FAK inhibitor to study its effects on protein kinase A activation in human sperm samples. price>
R-C-1088 RN486 CAS:1242156-23-5 RN486 is a potently and selectively inhibitor.RN486 inhibited the Btk enzyme and displayed functional activities in human cell-based assays in multiple cell types.RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC(50)=2.9 nM),Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes(IC(50)=7.0 nM),and B cell antigen receptor-induced expression of an activation marker,CD69,in B cells in whole blood(IC(50)=21.0 nM).RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis(AIA) models.In the AIA model,RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate,reducing both paw swelling and inflammatory markers in the blood. price>
R-C-1118 Defactinib(VS6063,PF-04554878) CAS:1073154-85-4 Defactinib(VS-6063;PF-04554878)is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities. price>
R-C-1120 Radotinib(IY-5511) CAS:926037-48-1 Radotinib is a selective second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl,with an IC50 value of 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type form.Radotinib also inhibits platelet-derived growth factor receptors(PDGFRs)α and β with IC50 values of 75.5 and 130 nM,respectively.Binding of radotinib to Bcr-Abl in vitro inhibits the phosphorylation of the downstream signaling mediator CrkL.3 In acute myeloid leukemia cells,in vitro treatment with radotinib at doses of 10-100 µM reduces viability,activates the mitochondrial apoptosis pathway,and promotes expression of the differentiation marker CD11b. price>
R-C-1126 Molidustat(BAY85-3934) CAS:1154028-82-6 Molidustat,also known as BAY 85-3934,is a novel inhibitor of hypoxia-inducible factor(HIF)prolyl hydroxylase(PH)which stimulates erythropoietin(EPO)production and the formation of red blood cells.Phase I data have shown that inhibition of HIF-PH by Molidustat results in an increase in endogenous production of EPO. price>
R-C-1172 BLU-9931 CAS:1538604-68-0 BLU9931 is a potent,highly selective,and irreversible fibroblast growth factor receptor 4(FGFR4)inhibitor with an IC50 of 3 nM and a Kd of 6 nM.BLU9931 has significant antitumor activity. price>
R-C-1179 CGI-1746 CAS:910232-84-7 CGI1746 is a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. price>
R-C-1186 TAE226 (NVP-TAE226) CAS:761437-28-9 NVP-TAE 226(TAE226)is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM,respectively.NVP-TAE 226(TAE226) also effectively inhibits Pyk2 and insulin receptor(InsR)with IC50s of 3.5 nM and 44 nM,respectively. price>
R-C-1240 GSK2256098 CAS:1224887-10-8 GSK2256098,also known as GTPL7939,is a focal adhesion kinase-1(FAK)inhibitor with potential antiangiogenic and antineoplastic activities.FAK inhibitor GSK2256098 inhibits FAK,which may prevent the integrin-mediated activation of several downstream signal transduction pathways,including ERK,JNK/MAPK and PI3K/Akt,thereby inhibiting tumor cell migration,proliferation and survival,and tumor angiogenesis.The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix(ECM)but may be upregulated and constitutively activated in various tumor cell types. price>