Dimethyl Sulfoxide
Apexbio Technology LLC XL-888 1149705-71-4 10mM (in 1mL DMSO)
XL-888 (CAS 1149705-71-4) is an orally bioavailable small molecule inhibitor targeting heat shock protein 90 (HSP90) It selectively inhibits HSP90 and HSP90 with IC50 values of 22 nM and 44 nM respectively while exhibiting markedly weaker inhibition against a panel of other kinases Structural analyses indicated XL-888 binds HSP90 via hydrogen bonding interactions involving the Asp93 residue In tumor cell assays XL-888 potently suppresses proliferation with IC50 values in the range of 0 1-45 5 nM XL-888 is used in oncology research particularly for studying resistance mechanisms to targeted therapies
Apexbio Technology LLC Vardenafil 224785-90-4 10mM (in 1mL DMSO)
Vardenafil (CAS 224785-90-4) is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) It inhibits PDE5 enzyme activity with an IC50 of approximately 0 7 nM in vitro Compared with other PDE isoforms (PDE1-4 and PDE6) vardenafil demonstrates superior selectivity toward PDE5 though moderate inhibition of PDE6 (IC50 11 nM) is observed Vardenafil enhances cGMP accumulation in human corpus cavernosum and significantly potentiates nitric oxide (SNP)- acetylcholine- and electrical field stimulation-induced relaxation in human trabecular smooth muscle Its vasodilatory effects render it suitable for research in erectile function and related vascular physiology
Apexbio Technology LLC CH5138303 959763-06-5 10mM (in 1mL DMSO)
CH5138303 (CAS 959763-06-5) is a potent inhibitor targeting Heat Shock Protein 90 (HSP90) exhibiting strong binding affinity with a Kd of 0 48 nM HSP90 a molecular chaperone regulates protein folding stability and degradation and maintains oncogenic proteins crucial to tumor cell proliferation CH5138303 effectively reduces protein levels and phosphorylation of HSP90 client proteins including Raf1 AKT EGFR and HER2 in NCI-N87 cancer cells In animal studies using human gastric cancer NCI-N87 xenografts oral administration of CH5138303 demonstrates significant antitumor activity achieving a tumor growth inhibition (TGI) rate of 136% at an ED of 3 9 mg/kg
Apexbio Technology LLC AM966 1228690-19-4 10mM (in 1mL DMSO)
AM966 (CAS 1228690-19-4) is an orally bioavailable small-molecule antagonist that selectively targets Lysophosphatidic acid type 1 receptor (LPA1) AM966 exhibits potent inhibitory activity against LPA1 receptors from humans and mice with IC50 values of approximately 17 nM and 19 nM respectively demonstrating selectivity over other LPA receptor subtypes (LPA2 5) In vitro AM966 blocks LPA-mediated chemotactic responses in IMR-90 human lung fibroblasts A2058 human melanoma cells and CHO cell lines In vivo AM966 effectively attenuates lung fibrosis inflammation and associated weight loss in bleomycin-induced murine pulmonary fibrosis models highlighting its utility in research on fibrotic diseases