Dimethyl Sulfoxide
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 Ondansetron hydrochloride dihydrate 103639-04-9 10mM (in 1mL DMSO)
Ondansetron hydrochloride dihydrate (CAS 103639-04-9) is a small molecule antagonist targeting the serotonin (5-HT3) receptor a ligand-gated ion channel prominent in the central and peripheral nervous systems Through blockade of 5-HT3 receptor signaling ondansetron inhibits serotonin-induced emetic responses Due to this mechanism it is widely utilized in biomedical research investigating serotonin-related signaling pathways and nausea mechanisms particularly in contexts involving chemotherapy-induced emesis
Apexbio Technology LLC (-)-MK 801 121917-57-5 10mM (in 1mL DMSO)
(-)-MK 801 (CAS 121917-57-5) is a small molecule serving as a non-competitive antagonist at the N-methyl-D-aspartate (NMDA) receptor It crosses the blood-brain barrier binding reversibly and with high affinity to cortical membranes in a saturable regionally specific manner notably within the hippocampus (-)-MK 801 selectively inhibits depolarization responses to NMDA receptor activation leading to suppression of seizure-like neuronal activity induced by neurotoxins such as tetrodotoxin Due to these properties it has widespread use as a research tool in neuroscience particularly in investigating excitotoxicity epilepsy and neurological disorders associated with NMDA receptor dysfunction
Apexbio Technology LLC GSK1904529A 1089283-49-7 10mM (in 1mL DMSO)
GSK1904529A (CAS 1089283-49-7) is a small-molecule inhibitor targeting insulin-like growth factor-I receptor (IGF-1R) Mechanistically it acts as a reversible ATP-competitive antagonist inhibiting IGF-1R kinase activity with an IC50 of approximately 27 nM and a Ki value of 1 6 nM In NIH-3T3/LISN cells it reduces IGF-1R phosphorylation at an IC50 of about 22 nM subsequently attenuating phosphorylation of downstream effectors such as AKT IRS-1 and ERK pathways GSK1904529A also suppresses proliferation in various tumor cell lines through cell-cycle arrest at the G1 phase and demonstrates tumor growth inhibition in xenograft mouse models It serves as a research tool for investigating IGF-1R signaling in oncology
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 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 Brassinolide 72962-43-7 10mM (in 1mL DMSO)
Brassinolide (CAS 72962-43-7) is a naturally occurring steroidal plant growth regulator It influences various physiological processes in plants including stem elongation leaf differentiation flower formation and fruit development In vitro studies indicated that brassinolide induces apoptosis in human prostate cancer PC-3 cells characterized by increased caspase-3 activity and decreased Bcl-2 protein expression In animal models brassinolide reduced blood glucose levels in diabetic rats demonstrating non-dose-dependent hypoglycemic effects without observed toxicity Brassinolide is valuable in research related to cancer cell apoptosis and glucose metabolism regulation
Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 10mM (in 1mL DMSO)
Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects
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 ML216 1430213-30-1 10mM (in 1mL DMSO)
ML216 (CAS 1430213-30-1) is a small molecule inhibitor targeting Bloom (BLM) helicase a DNA unwinding enzyme essential for homologous recombination-mediated DNA repair ML216 inhibits DNA unwinding activity of full-length BLM (IC50 3 0 M) and a truncated form BLM636-1298 (IC50 0 97 M) displaying sub-micromolar selectivity relative to other helicases such as RECQ1 RECQL5 and bacterial UvrD In cellular assays ML216 selectively suppresses proliferation in BLM-containing fibroblasts increasing sister chromatid exchange frequency consistent with BLM functional deficiency By inhibiting BLM helicase ML216 may sensitize tumor cells to conventional DNA-damaging therapeutics indicating potential application in cancer research and therapy development
Apexbio Technology LLC GM 6001 142880-36-2 10mM (in 1mL DMSO)
GM 6001 (Ilomastat Galardin CAS 142880-36-2) is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) including MMP-1 -2 -3 -8 and -9 with reported Ki values of 0 4 nM 0 5 nM 27 nM 0 1 nM and 0 2 nM respectively MMPs participate in extracellular matrix remodeling and mediate signaling events induced by GPCR agonists through EGFR transactivation GM 6001 suppresses EGFR phosphorylation ERK activation and subsequent DNA synthesis induced by stimuli such as bombesin and lysophosphatidic acid (LPA) Additionally this compound has potential applications in cartilage research facilitating meniscal repair under inflammatory conditions by dampening IL-1-mediated MMP activity
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