Dimethyl Sulfoxide
Apexbio Technology LLC AGI-5198 1355326-35-0 10mM (in 1mL DMSO)
AGI-5198 (CAS 1355326-35-0) is a selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) harboring the R132H substitution Identified via high-throughput screening AGI-5198 blocks mutant IDH1-mediated formation of the oncometabolite R-2-hydroxyglutarate (R-2-HG) in a dose-dependent manner Mechanistically inhibition of mutant IDH1 by AGI-5198 induces expression of differentiation-associated zinc finger and BTB domain-containing protein 16 (ZBTB16 also termed PLZF) decreasing histone H3 lysine 9 trimethylation (H3K9me3) and promoting glioma cell differentiation In experimental glioma models AGI-5198 reduces tumor cell proliferation underscoring its utility for investigating differentiation therapy strategies targeting IDH1-mutant cancers
Apexbio Technology LLC Empagliflozin (BI 10773) 864070-44-0 10mM (in 1mL DMSO)
Empagliflozin (BI 10773 CAS 864070-44-0) is a potent selective inhibitor targeting sodium-glucose cotransporter 2 (SGLT-2) a transmembrane protein primarily expressed in the kidneys and responsible for glucose reabsorption Empagliflozin inhibits SGLT-2 with an IC50 of 3 1 nM demonstrating high selectivity relative to related transporters (SGLT-1 4 5 and 6) In vitro studies using HK2 human proximal tubular cells showed that empagliflozin suppresses high glucose-induced pro-inflammatory signaling pathways including TLR4 NF- B AP-1 and IL-6 secretion Empagliflozin has been widely studied in diabetic animal models such as Zucker diabetic obese rats effectively reducing blood glucose and increasing urinary glucose excretion supporting its application in diabetes research
Apexbio Technology LLC Tivozanib (AV-951) 475108-18-0 10mM (in 1mL DMSO)
Tivozanib (AV-951 CAS 475108-18-0) is a quinoline-urea derivative functioning as a potent inhibitor of vascular endothelial growth factor receptors (VEGFR) It primarily targets VEGFR-2 kinase demonstrating significant inhibitory activity in picomolar ranges (IC50 of approximately 160 pM) Additionally Tivozanib displays considerable selectivity causing minimal off-target interaction with c-kit In cellular assays it inhibits PDGFR and c-kit phosphorylation at nanomolar levels Preclinical evaluations revealed antitumor activity across multiple solid tumor xenograft models particularly renal cell carcinoma (RCC) Its mechanism and selectivity profile render it valuable for cancer research clinical investigation and preclinical efficacy assessments
Apexbio Technology LLC AZD1208 1204144-28-4 10mM (in 1mL DMSO)
AZD1208 (CAS 1204144-28-4) is a selective orally bioavailable pan-Pim kinase inhibitor targeting Pim-1 Pim-2 and Pim-3 kinases with IC50 values of 0 4 nM 5 nM and 1 9 nM respectively Pim kinases are implicated in proliferative and anti-apoptotic signaling downstream of cytokines and growth factors frequently overexpressed in leukemia and lymphoma In vitro AZD1208 inhibits growth induces cell cycle arrest apoptosis and reduces phosphorylation of the anti-apoptotic protein Bcl-2 in AML cell lines Preclinically this compound suppresses tumor growth in AML xenograft models supporting its current clinical evaluation in AML and solid tumor trials
Apexbio Technology LLC LCL161 1005342-46-0 10mM (in 1mL DMSO)
LCL161 (CAS 1005342-46-0) is a small-molecule antagonist targeting inhibitor of apoptosis (IAP) proteins specifically designed as a mimetic of the endogenous second mitochondria-derived activator of caspase (SMAC) LCL161 binds to and inhibits XIAP and cIAP1/2 proteins frequently overexpressed in malignant cells It demonstrates antiproliferative activity in vitro against selected hepatocellular carcinoma cell lines (Hep3B PLC5) and hematologic cancer models (ALL) with IC50 values in the micromolar range In in vivo tumor xenograft studies oral administration of LCL161 has led to significant growth delays across various malignancies including osteosarcoma and glioblastoma Its combination with AAVP-delivered TNF- results in synergistic antitumor effects indicating its utility in oncology research
Apexbio Technology LLC Anacetrapib (MK-0859) 875446-37-0 10mM (in 1mL DMSO)
Anacetrapib (MK-0859 CAS 875446-37-0) is a selective inhibitor of cholesteryl ester transfer protein (CETP) an enzyme involved in mediating the transfer of cholesteryl esters and triglycerides between lipoproteins In biochemical assays anacetrapib exhibits potent inhibition of CETP-driven lipid transfer with reported IC50 values of 16 nM for cholesteryl ester transfer and 29 nM for triglyceride transfer Metabolically it undergoes oxidation via CYP3A4 to form metabolites M1 M2 and M3 Due to its effect of significantly lowering LDL cholesterol and elevating HDL cholesterol anacetrapib is studied in research related to primary hypercholesterolemia and mixed dyslipidemia
Apexbio Technology LLC Dihydromyricetin 27200-12-0 10mM (in 1mL DMSO)
Dihydromyricetin also termed Ampelopsin is a natural flavanonol compound frequently investigated for its antioxidant and anticancer properties It exerts biological effects primarily through modulation of molecular pathways involving oxidative stress responses apoptosis regulation and GABA-A receptor enhancement at benzodiazepine binding sites Studies indicate dihydromyricetin acts as a positive allosteric modulator on GABA-A receptors suggesting potential for research related to alcohol intoxication and associated neural mechanisms In cellular assays dihydromyricetin demonstrates antiproliferative activity against various cancer cell lines typically exhibiting IC50 concentrations in the micromolar range Thus this compound is widely utilized in biomedical research including cell signaling pathway analysis antioxidant mechanism exploration and studies examining potential therapeutic roles in oncology and neuropharmacology
Apexbio Technology LLC BPTES 314045-39-1 10mM (in 1mL DMSO)
BPTES (CAS 314045-39-1) is a selective inhibitor of kidney-type glutaminase (GLS) an enzyme responsible for converting glutamine to glutamate and ammonia It exhibits inhibitory activity against GLS with a reported Ki of approximately 3 M GLS-mediated glutamine metabolism is particularly essential in proliferating and malignant cells BPTES reduces glutamine-to-glutamate conversion in tumor cells diminishing the transamination of pyruvate to alanine as observed in decreased alanine-to-pyruvate ratios in animal models In vitro BPTES inhibits growth by approximately 50% of IDH1-mutant AML cells at 20 M concentration but does not significantly affect wild-type AML cells highlighting its relevance for cancer metabolism research
Apexbio Technology LLC CPI-169 1450655-76-1 10mM (in 1mL DMSO)
CPI-169 is a selective small-molecule inhibitor targeting enhancer of zeste homolog 2 (EZH2) a catalytic component of polycomb repressive complex 2 (PRC2) By inhibiting EZH2 enzymatic activity CPI-169 suppresses methylation at histone H3 lysine 27 (H3K27me3) thereby altering chromatin structure and gene expression profiles Pharmacological experiments demonstrate inhibition of EZH2 with subnanomolar IC50 values and cellular studies indicate reductions of H3K27 trimethylation at nanomolar concentrations CPI-169 has been utilized experimentally to investigate EZH2-dependent epigenetic processes cell proliferation apoptosis pathways and therapeutic potential particularly in lymphoma and cancer biology studies employing in vitro and in vivo models
Apexbio Technology LLC XL019 945755-56-6 10mM (in 1mL DMSO)
XL019 (CAS 945755-56-6) is a selective inhibitor targeting Janus kinase 2 (JAK2) with an IC50 of 2 2 nM JAK2 regulates signaling pathways controlling erythroid granulocytic and megakaryocytic lineage differentiation via cytokine and hematopoietic growth factor receptors including erythropoietin and thrombopoietin receptors XL019 demonstrates high selectivity for JAK2 over related kinases (e g JAK1 TYK2) In mouse models bearing HEL 92 1 7 xenografts oral administration of XL019 significantly reduced tumor growth XL019 is evaluated clinically as a candidate for treating primary myelofibrosis and secondary myelofibrosis associated with polycythemia vera or essential thrombocythemia