Dimethyl Sulfoxide
Apexbio Technology LLC ANA 12 219766-25-3 10mM (in 1mL DMSO)
ANA 12 (CAS 219766-25-3) is a potent and selective antagonist of tropomyosin receptor kinase B (TrkB) the receptor for neurotrophins BDNF and NT-4/5 It binds non-competitively to extracellular sites on TrkB exhibiting IC50 values of 45 6 nM (high-affinity site) and 41 1 M (low-affinity site) ANA 12 inhibits BDNF-induced TrkB activation effectively blocking downstream signaling pathways including PLC- PI3K and MAPK In mouse models ANA 12 administration reduces endogenous brain TrkB activity and demonstrates antidepressant and anxiolytic properties supporting its use for researching psychiatric disorders and neuronal signaling
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 UNC1999(Synonyms: UNC-1999, UNC 1999, EZH2 inhibitor UNC1999, EZH2-IN-UNC1999, EZH2-IN3), 10mM (in 1mL DMSO), CAS: 1431612-23-5.
UNC1999 (CAS 1431612-23-5) is a small molecule inhibitor targeting EZH2 and EZH1 enzymes responsible for methylating lysine 27 on histone H3 (H3K27me3) a modification associated with transcriptional suppression It inhibits EZH2 and EZH1 with IC50 values of 2 nM and 45 nM respectively binding at the enzyme s SAM cofactor binding site but not competing with histone substrate UNC1999 reduces cellular H3K27me3 levels (IC50 124 nM) and inhibits proliferation of DLBCL cells harboring EZH2 Y641N mutation (EC50 633 nM) It exhibits oral bioavailability in mouse studies supporting its utility as a research probe for investigating EZH-mediated epigenetic regulation
Apexbio Technology LLC A-803467 944261-79-4 10mM (in 1mL DMSO)
A-803467 (CAS 944261-79-4) is a potent selective blocker of the voltage-gated sodium channel subtype NaV1 8 It inhibits human and rat recombinant NaV1 8 channels with IC50 values of approximately 79 nM and 45 nM respectively Its selectivity for NaV1 8 over other sodium channel subtypes (e g NaV1 2 NaV1 3 NaV1 5 and NaV1 7) is 300 1000 fold By specifically reducing activity in tetrodotoxin-resistant sodium currents of dorsal root ganglion neurons A-803467 suppresses induced and spontaneous action potential firing exhibiting analgesic properties in animal models of neuropathic and inflammatory pain
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