Dimethyl Sulfoxide
Apexbio Technology LLC Erlotinib Hydrochloride 183319-69-9 10mM (in 1mL DMSO)
Erlotinib hydrochloride (CAS 183319-69-9) is a small molecule inhibitor targeting the epidermal growth factor receptor (EGFR/HER-1) specifically blocking its tyrosine kinase activity By competitively inhibiting EGFR phosphorylation (IC50 2 nM) Erlotinib hydrochloride disrupts downstream signaling pathways involved in tumor cell proliferation apoptosis resistance migration and angiogenesis In vitro studies indicate this inhibitor induces G0/G1 cell cycle arrest and promotes apoptosis in cancer cell lines such as pancreatic (Bxpc-3 PANC-1) and hepatocellular carcinoma cells Erlotinib hydrochloride is widely studied in oncology research particularly in non-small cell lung cancer (NSCLC) and pancreatic cancer models
Apexbio Technology LLC K02288 1431985-92-0 10mM (in 1mL DMSO)
K02288 (CAS 1431985-92-0) is a highly selective small molecule inhibitor targeting activin receptor-like kinase 2 (ALK2) a type I receptor involved in BMP signaling Structurally classified as a 2-aminopyridine derivative K02288 demonstrates strong potency against ALK2 (IC50 1 1 nM) It exhibits selectivity across the ALK receptor family showing lower activity on ALK3 ALK6 and minimal inhibition against ALK4-5 In cell-based assays using C2C12 cells treated with BMP ligands K02288 dose-dependently reduces Smad phosphorylation It has utility in research elucidating ALK2-mediated signaling pathways and developmental processes exemplified by inducing dorsalized phenotypes in zebrafish embryos
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 ZM 447439 331771-20-1 10mM (in 1mL DMSO)
ZM 447439 (CAS 331771-20-1) is a selective inhibitor of Aurora kinases a subgroup within the serine/threonine kinase family involved in chromosome segregation during cell division It inhibits recombinant Aurora A and Aurora B kinases with IC50 values of approximately 110 nM and 130 nM respectively consequently reducing phosphorylation of histone H3 at serine 10 ZM 447439 demonstrates limited inhibitory activity towards other kinases with IC50 values above 10 M for CDK1/2/4 IKK1/2 PLK1 CHK1 cFLT2 KDR2 FAK and Zap-70 In biological research ZM 447439 is commonly employed to study mitotic regulation chromosomal alignment and apoptosis signaling pathways
Apexbio Technology LLC Tianeptine sodium(Synonyms: Stablon, Coaxil, Tatinol, Tianeurax, Salymbra, Tianeptine Sodium Salt), 10mM (in 1mL DMSO), CAS: 30123-17-2.
Tianeptine sodium (CAS 30123-17-2) is a small molecule known to selectively facilitate serotonin (5-HT) uptake in both in vitro and in vivo experimental models It exhibits minimal affinity toward various neurotransmitter receptors including serotonin and dopamine receptors (IC 10 M) and does not affect the uptake mechanisms of noradrenaline or dopamine Due to its distinct serotonergic modulation tianeptine sodium is extensively used in neuroscience research particularly in studies investigating the molecular basis and therapeutic potential of antidepressants
Apexbio Technology LLC VER 155008 1134156-31-2 10mM (in 1mL DMSO)
VER 155008 (CAS 1134156-31-2) is a small molecule inhibitor targeting members of the heat shock protein 70 (Hsp70) chaperone family It primarily inhibits Hsp70 by binding within its ATPase domain and suppressing its intrinsic ATPase activity thereby reducing chaperone-mediated cell survival functions VER 155008 demonstrates potent inhibition of Hsp70 (IC50 0 5 M) and exhibits moderate inhibitory action against related chaperones Hsc70 and glucose-regulated protein Grp78 In cancer cell models this compound diminishes cell proliferation and promotes apoptosis suggesting utility as a research tool in studying chaperone-dependent tumor cell survival pathways
Apexbio Technology LLC Penciclovir 39809-25-1 10mM (in 1mL DMSO)
Penciclovir is a selective inhibitor of herpes simplex virus 1 (HSV-1) DNA synthesis Structurally derived from guanine penciclovir undergoes phosphorylation within virus-infected cells forming penciclovir triphosphate the active antiviral metabolite Penciclovir triphosphate specifically targets viral DNA polymerase blocking HSV-1 DNA replication In vitro experiments using MRC-5 cells demonstrate inhibition of HSV-1 replication at an IC50 of 0 16 M without interfering with host cellular DNA synthesis This mechanism of action renders penciclovir suitable for antiviral research targeting HSV-1 replication as well as drug-resistance and mechanism-of-action studies involving HSV-2 and varicella-zoster virus (VZV)
Apexbio Technology LLC Pepstatin A 26305-03-3 10mM (in 1mL DMSO)
Pepstatin A is a pentapeptide functioning as an inhibitor targeting aspartic proteases including pepsin renin HIV protease and cathepsin D It inhibits human renin and HIV protease with IC50 values of approximately 15 M and 2 M respectively and shows inhibitory activity toward pepsin and cathepsin D at IC50 values below 5 M and 40 M Mechanistically Pepstatin A acts through binding to the catalytic site of aspartic proteases restricting proteolytic activity In biomedical research it is utilized to study viral protein processing osteoclast differentiation mediated by cathepsins and as a standard tool in enzyme inhibition assays examining aspartic protease function
Apexbio Technology LLC A939572 1032229-33-6 10mM (in 1mL DMSO)
A939572 (CAS 1032229-33-6) is an orally bioavailable small-molecule inhibitor targeting stearoyl-CoA desaturase 1 (SCD1) an enzyme that catalyzes the formation of monounsaturated fatty acids involved in lipid metabolism and body weight regulation A939572 selectively inhibits human and mouse SCD1 with IC50 values of 37 nM and 4 nM respectively exhibiting no inhibitory effect on associated cofactors cytochrome b5 or cytochrome b5 reductase By specifically interacting with SCD1 A939572 serves as a pharmacological tool in metabolic research particularly in studies focused on obesity and diabetes
Apexbio Technology LLC Simvastatin (Zocor) 79902-63-9 10mM (in 1mL DMSO)
Simvastatin (CAS 79902-63-9) marketed as Zocor is a synthetic lactone derived from fermented Aspergillus terreus metabolites Following oral administration the inactive lactone is hydrolyzed into an active -hydroxy acid metabolite which specifically inhibits HMG-CoA reductase the rate-limiting enzyme in cholesterol biosynthesis Simvastatin demonstrates antiproliferative effects in hepatocellular carcinoma cells (HepG2 Huh7) inducing apoptosis cell cycle arrest at G0/G1 reducing expression of cyclins (D1 E) and cyclin-dependent kinases (CDK1 2 4) while elevating CDK inhibitors p19 and p27 It is therefore utilized extensively for research in cancer biology cardiovascular pathology and lipid metabolism disorders
Apexbio Technology LLC Didanosine 69655-05-6 10mM (in 1mL DMSO)
Didanosine is a nucleoside analogue known to inhibit reverse transcriptase enzymes by acting as a competitive inhibitor and terminator of viral DNA elongation Mechanistically didanosine is phosphorylated intracellularly to its active metabolite dideoxyadenosine triphosphate (ddATP) an analog of dATP Incorporation of ddATP into viral DNA by viral reverse transcriptase causes premature termination of DNA synthesis thereby inhibiting retroviral replication Didanosine is frequently employed as an experimental tool in studies examining antiviral activity and resistance mechanisms in retroviral infection models particularly HIV research In vitro assays commonly report IC50 values for didanosine against HIV reverse transcriptase in the range of approximately 0 5 to 10 M varying according to experimental conditions and viral strain sensitivity evaluated
Apexbio Technology LLC Phenformin HCl 834-28-6 10mM (in 1mL DMSO)
Phenformin HCl (CAS 834-28-6) is the hydrochloride salt form of phenformin a biguanide-class compound exhibiting antidiabetic activity Phenformin acts primarily by reducing blood glucose levels and diminishing glycosuria as demonstrated in clinical studies with diabetic patients In an investigation involving five diabetic subjects treatment with phenformin led to notably decreased fasting blood glucose concentrations and urinary glucose excretion additionally cholesterol and total lipid levels reduced in four of the five patients studied Phenformin showed no measurable effect on glucose or insulin responses following intravenous glucose administration This biguanide derivative serves as an important pharmacological tool in diabetes-related biomedical research
Apexbio Technology LLC Marimastat 154039-60-8 10mM (in 1mL DMSO)
Marimastat (CAS 154039-60-8) also known as BB-2516 is an orally bioavailable inhibitor of matrix metalloproteases (MMPs) Structurally it contains a collagen-mimicking hydroxamate moiety that facilitates covalent binding to the zinc atom at MMP active sites Marimastat exhibits broad-spectrum inhibitory activity against MMP-1 MMP-2 MMP-7 MMP-9 and MMP-14 with IC50 values of 5 nM 6 nM 13 nM 3 nM and 9 nM respectively In animal models of metastatic cancers Marimastat reduces tumor dissemination and progression Clinically Marimastat is investigated for potential therapeutic effects against metastatic and non-metastatic solid tumors such as pancreatic and gastric cancers
Apexbio Technology LLC AG-1478 153436-53-4 10mM (in 1mL DMSO)
AG-1478 is a selective inhibitor of epidermal growth factor receptor (EGFR) a receptor tyrosine kinase involved in cellular proliferation and survival It inhibits EGFR-mediated Erk1/2 phosphorylation induced by EGF stimulation with an IC50 of approximately 10 M in Ishikawa ovarian cell lines In experimental cancer research AG-1478 has been applied to study EGFR signaling mechanisms by reducing receptor phosphorylation and downstream pathway activation Studies using diverse cancer cell lines including ovarian (CAOV-3 SKOV-3) colorectal (SW480) hepatocellular (HA22T/VGH) and lung (A549) carcinomas employ AG-1478 to investigate EGFR s role in tumor growth and chemoresistance Additionally AG-1478 is utilized in preclinical xenograft models to assess tumor growth modulation via EGFR inhibition
Apexbio Technology LLC TG100-115 677297-51-7 10mM (in 1mL DMSO)
TG100-115 (CAS 677297-51-7) is a selective inhibitor targeting phosphoinositide 3-kinase isoforms PI3K and PI3K with IC50 values of 83 nM and 235 nM respectively exhibiting negligible inhibition towards PI3K and PI3K Research in murine models demonstrates that treatment with TG100-115 significantly reduces eosinophil accumulation bronchoalveolar IL-13 cytokine levels mucus deposition and leukocyte infiltration associated with allergic asthma decreasing airway hyperresponsiveness by approximately 50% Moreover this compound attenuates neutrophil infiltration and TNF induction following exposure to cigarette smoke and LPS suggesting its utility as an investigational tool for asthma and inflammatory pulmonary diseases