Dimethyl Sulfoxide
Apexbio Technology LLC Go 6983(Synonyms: GO-6983, GO6983, PKC Inhibitor GO 6983, Pan-PKC Inhibitor GO-6983, PKC inhibitor GO6983, 133053-19-7), 10mM (in 1mL DMSO), CAS: 133053-19-7.
Go 6983 (CAS 133053-19-7) is a selective inhibitor of protein kinase C isoforms PKC PKC PKC PKC and PKC with reported IC50 values of approximately 7 nM 7 nM 6 nM 10 nM and 20 mM respectively Protein kinase C (PKC) isoforms act as receptors for tumor-promoting phorbol ester mediating various downstream cellular functions In cancer cell models Go 6983 suppresses PKC and PKC activation induced by phorbol esters and reduces PKC expression inhibiting cell survival pathways It is frequently employed in biomedical studies examining PKC-dependent signaling in cancer progression and epithelial-to-mesenchymal transition (EMT)
Apexbio Technology LLC Ambrisentan 177036-94-1 10mM (in 1mL DMSO)
Ambrisentan (CAS 177036-94-1) is an orally active selective endothelin receptor antagonist specifically targeting ETA receptors It exhibits strong selectivity towards ETA over ETB receptor subtypes shown by Ki values of approximately 1 nM for recombinant ETA receptors expressed in vitro versus 195 nM for ETB In recombinant human receptor assays using intact cells this selectivity is enhanced with reported Ki values of 0 63 nM (ETA) and 48 7 nM (ETB) Pharmacologically ambrisentan s selective ETA blockade preserves the ETB receptor s intrinsic vasodilatory and endothelin clearance functions making it useful in research involving pulmonary arterial hypertension cerebrovascular conditions and ischemia-reperfusion injury
Apexbio Technology LLC Triptolide 38748-32-2 10mM (in 1mL DMSO)
Triptolide (CAS 38748-32-2) is a biologically active diterpenoid originally isolated from the traditional Chinese herb Tripterygium wilfordii It exerts inhibitory effects by suppressing interleukin-2 expression in activated T cells and impeding NF- B-mediated transcriptional activation Triptolide inhibits invasion and migration of ovarian cancer cells via reducing matrix metalloproteinases MMP-7 and MMP-19 expression and enhancing E-cadherin expression Additionally it induces RNA polymerase II degradation leading to apoptosis and reduced proliferation in cancer cell lines and rheumatoid arthritis synovial fibroblasts Consequently triptolide serves as a valuable tool for immunology oncology and inflammation research
Apexbio Technology LLC Aprepitant 170729-80-3 10mM (in 1mL DMSO)
Aprepitant (MK-0869) is a highly selective antagonist of the neurokinin-1 (NK-1) receptor functioning by competitively inhibiting substance P (SP) an undecapeptide belonging to the tachykinin family from activating NK-1 receptors Its binding affinity for human NK-1 receptors is indicated by a dissociation constant (Kd) of approximately 86 pM In cellular models overexpressing NK-1 receptors including glioma (GAMG) neuroblastoma (SKN-BE2 IC50 19 6 M IMR-32 IC50 27 7 M KELLY IC50 30 4 M) retinoblastoma (Y-79 IC50 23 M WERI-Rb-1 IC50 31 2 M) pancreatic cancer (PA-TU-8902 IC50 27 4 M CAPAN-1 IC50 22 7 M) and colon cancer (SW-403 IC50 30 5 M) aprepitant application has been reported to inhibit tumor cell proliferation in vitro
Apexbio Technology LLC PCI-24781 (CRA-024781) 783355-60-2 10mM (in 1mL DMSO)
PCI-24781 (CRA-024781 CAS 783355-60-2) is a histone deacetylase (HDAC) inhibitor targeting HDAC1 HDAC2 HDAC3 HDAC6 HDAC8 and HDAC10 with reported Ki values of 7 19 8 2 17 280 and 24 nM respectively HDAC enzymes catalyze the removal of acetyl groups from lysine residues on histone proteins thereby regulating chromatin structure and gene expression PCI-24781 induces dose-dependent hyperacetylation of histones and tubulin in human cancer cells (HCT116 DLD-1) leading to apoptosis via p21 upregulation PARP cleavage and H2AX accumulation PCI-24781 demonstrates antitumor activity against multiple tumor cell lines and in xenograft models highlighting its utility for oncology research