Dimethyl Sulfoxide
Apexbio Technology LLC Riluzole 1744-22-5 10mM (in 1mL DMSO)
Riluzole (CAS 1744-22-5) is a small molecule modulator of glutamatergic neurotransmission exhibiting multiple mechanisms of neuroprotection Its action primarily involves inhibition of voltage-gated sodium channels modulation of high-voltage-activated calcium and potassium channels and interference with protein kinase C activity collectively mitigating neuronal excitotoxicity In cultured rat cortical neurons riluzole inhibits inward sodium currents with an IC50 of 51 M At submicromolar to micromolar concentrations riluzole enhances sodium-dependent glutamate uptake mediated by the GLAST GLT1 and EAAC1 transporters Owing to these properties riluzole is commonly utilized in neuroscience research on excitotoxicity neurodegeneration and related pathologies
Apexbio Technology LLC EPZ015666 1616391-65-1 10mM (in 1mL DMSO)
EPZ015666 (CAS 1616391-65-1) is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) an enzyme implicated in several cellular pathways including tumorigenesis EPZ015666 inhibits PRMT5 with an IC50 of 22 nM and displays a Ki value of approximately 5 nM It exhibits over 20 000-fold selectivity for PRMT5 relative to other protein methyltransferases tested In mantle cell lymphoma (MCL) cell lines treatment with EPZ015666 reduced methylation levels of the PRMT5 substrate SmD3 and exerted concentration-dependent anti-proliferative effects Additionally EPZ015666 demonstrated dose-dependent tumor growth inhibition in mouse xenograft models of MCL highlighting its potential utility as a molecular tool in cancer biology research
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 TMP269 1314890-29-3 10mM (in 1mL DMSO)
TMP269 (CAS 1314890-29-3) is a selective inhibitor of class IIa histone deacetylases (HDACs) specifically targeting HDAC isoforms 4 5 7 and 9 with IC50 values of 126 80 36 and 9 nM respectively HDACs catalyze removal of acetyl groups from histone lysine residues thereby condensing chromatin and repressing transcription TMP269 induces moderate cytotoxicity (IC50 22-38 M) in multiple myeloma cell lines correlating with cleavage of caspase-3 -8 -9 and PARP and enhances ER stress-induced apoptosis signaling pathways Additionally TMP269 inhibits PKD1-mediated proliferation in intestinal epithelial IEC-18 cells
Apexbio Technology LLC Ponatinib (AP24534) 943319-70-8 10mM (in 1mL DMSO)
Ponatinib (AP24534 CAS 943319-70-8) is a second-generation small molecule inhibitor targeting the BCR-ABL fusion kinase The BCR-ABL fusion arising from a t(9 22) chromosomal translocation encodes oncogenic tyrosine kinase variants implicated in chronic myeloid leukemia (CML) acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) Ponatinib inhibits both wild-type BCR-ABL (IC50 0 5 nM) and resistant mutants notably the T315I mutant (IC50 11 nM) Additionally it potently inhibits clinically relevant kinases such as RET FLT3 KIT PDGFR / and FGFR1 Ponatinib is utilized in cancer biology research pertaining to kinase-driven malignancies
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