Dimethyl Sulfoxide
Apexbio Technology LLC 17-AAG (KOS953) 75747-14-7 10mM (in 1mL DMSO)
17-AAG (KOS953) is a synthetic derivative of geldanamycin that inhibits heat shock protein 90 (HSP90) It acts by binding to HSP90 causing destabilization of client proteins including HER2 Raf-1 p53 and components of MAPK signaling pathways Reported IC50 for 17-AAG in BT474 cells is approximately 6 nM Its biological activity has been investigated broadly including in multiple myeloma breast cancer thyroid cancer Hodgkin lymphoma and melanoma cellular models Ongoing studies explore 17-AAG both as monotherapy and in combination with agents like bortezomib or trastuzumab for addressing treatment-resistant cancer cell lines Currently 17-AAG is evaluated in Phase II clinical trials
Apexbio Technology LLC Org 27569 868273-06-7 10mM (in 1mL DMSO)
Org 27569 (CAS 868273-06-7) is an allosteric modulator targeting the cannabinoid CB1 receptor It enhances the binding of the agonist CP55940 to purified CB1 receptors while simultaneously inhibiting receptor functionality In electrically-stimulated mouse vas deferens assays Org 27569 reduced WIN55212-induced contractions exhibiting a pEC50 of 8 24 0 12 and a maximal response (Emax) of approximately 45 4% Binding studies suggest its interaction at a putative allosteric site on CB1 receptors reflected by parameters such as a pKB of 5 67 0 23 and a Log of 1 14 0 17 Org 27569 serves as a tool compound for studying CB1 receptor allosteric modulation
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