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 Peramivir(Synonyms: Rapivab, BCX-1812, RWJ-270201, Peramiflu), 10mM (in 1mL DMSO), CAS: 330600-85-6.
Peramivir (CAS 330600-85-6) is a neuraminidase inhibitor under investigation for antiviral activity against influenza virus Structurally peramivir functions as a transition-state analogue inhibitor selectively targeting viral neuraminidase to obstruct enzymatic cleavage required for virion release from infected host cells By this action peramivir effectively impedes viral propagation It has undergone clinical evaluation in research contexts notably receiving emergency use authorization for hospitalized patients during the 2009 H1N1 influenza pandemic
Apexbio Technology LLC Corticosterone(Synonyms: 17-Deoxycortisol, 11β,21-Dihydroxyprogesterone, Reichstein's Substance B, Kendall's Compound B), 10mM (in 1mL DMSO), CAS: 50-22-6.
Corticosterone (CAS 50-22-6) is an endogenous steroid hormone secreted by the adrenal cortex which exhibits affinity toward both glucocorticoid and mineralocorticoid receptors Its mechanism of action involves serum- and glucocorticoid-inducible kinase (SGK)-mediated phosphorylation of GDP dissociation inhibitor (GDI) at Ser-213 thereby promoting GDI-Rab4 complex assembly This activity enhances Rab4-dependent recycling of AMPA receptors to cortical neuron synapses leading to elevated synaptic excitatory responses Corticosterone thus serves as a useful biochemical tool for investigating stress-related modulation of synaptic transmission and plasticity
Apexbio Technology LLC Reserpine 50-55-5 10mM (in 1mL DMSO)
Reserpine a naturally derived alkaloid isolated from plants of the genus Rauvolfia functions primarily through the inhibition of vesicular monoamine transporter 2 (VMAT2) By blocking VMAT2-mediated uptake reserpine causes depletion of monoamine neurotransmitters such as dopamine norepinephrine and serotonin from synaptic storage vesicles In biochemical assays reserpine inhibits VMAT2 activity with an IC50 value typically ranging from 30-50 nM depending on assay specifics In biomedical and pharmacological research this compound is commonly utilized to model neurotransmitter depletion mechanisms in vitro and in animal models facilitating studies on monoamine-related neurological disorders neurotransmission pathways as well as serotonergic dopaminergic and adrenergic signaling
Apexbio Technology LLC Topotecan HCl 119413-54-6 10mM (in 1mL DMSO)
Topotecan HCl (CAS 119413-54-6) also known as SKF104864 is a semisynthetic derivative of camptothecin functioning as a selective inhibitor of topoisomerase I It stabilizes the topoisomerase I-DNA cleavage complex causing DNA damage and subsequent cell death Preclinical studies in murine tumor models demonstrate notable antitumor activity particularly against intravenous P388 leukemia and Lewis lung carcinoma when administered intravenously or in subcutaneous xenografts Additionally it exhibits efficacy against solid tumors including drug-resistant cancers and HT-29 human colon carcinoma xenografts Toxicological evaluations indicate reversible and concentration-dependent toxic effects primarily impacting rapidly proliferating tissues such as bone marrow and gastrointestinal epithelium
Apexbio Technology LLC GSK3787 188591-46-0 10mM (in 1mL DMSO)
GSK3787 is an irreversible antagonist targeting peroxisome proliferator-activated receptor beta/delta (PPAR- / ) Structurally it acts through covalent modification by binding specific cysteine residues within the ligand-binding domain of PPAR- / thereby disrupting receptor activation and subsequent co-regulator interactions Due to receptor selectivity GSK3787 preferentially inhibits PPAR- / relative to PPAR- Experimental evidence in rodent models demonstrates that oral administration of GSK3787 counteracts agonist-induced gene expression such as Angptl4 and Adrp by reducing recruitment of activated PPAR- / to target gene promoters indicating potential utility in studying PPAR- / -mediated regulatory pathways related to lipid metabolism and gene transcription in vitro and in vivo
Apexbio Technology LLC Pifithrin-α (PFTα) 63208-82-2 10mM (in 1mL DMSO)
Pifithrin- (PFT CAS 63208-82-2) is a synthetic water-soluble inhibitor targeting the tumor suppressor protein p53 Initially identified by its ability to block activation of p53-responsive genes PFT reduces apoptosis in transformed mouse embryonic fibroblasts (expressing E1a and ras) in a p53-dependent manner Additionally PFT prevents DNA damage-induced growth arrest in human diploid fibroblasts and promotes G2-phase cell cycle arrest following -irradiation It also decreases the expression of pluripotency marker Nanog affecting self-renewal potential in embryonic stem cells without compromising viability Thus PFT serves as a valuable research tool to investigate p53-mediated cellular pathways
Apexbio Technology LLC Golgicide A 1139889-93-2 10mM (in 1mL DMSO)
Golgicide A is a reversible small-molecule inhibitor targeting the guanine nucleotide exchange factor GBF1 GBF1 functions as an ArfGEF facilitating Arf1 activation and COPI recruitment at the cis-Golgi membranes essential for Golgi structure maintenance and protein transport regulation Golgicide A disrupts Golgi morphology leading to dispersion of Golgi markers and altered COPI localization In cellular assays Golgicide A inhibits shiga toxin-mediated protein synthesis with an IC50 of approximately 3 3 M in Vero cells and impairs retrograde toxin trafficking and secretory protein transport Additionally Golgicide A is applied in HCV research to reduce viral RNA replication and alter NS5A localization causing accumulation of viral particles in infected cells
Apexbio Technology LLC Etonogestrel(Synonyms: 3-Ketodesogestrel, Implanon, Nexplanon, ORG-3236, 11-Methylenelevonorgestrel), 10mM (in 1mL DMSO), CAS: 54048-10-1.
Etonogestrel (CAS 54048-10-1) is a synthetic steroidal molecule derived as the biologically active metabolite of the progestin desogestrel Structurally it belongs to the 19-nortestosterone class and acts primarily through potent binding and agonist activity at progesterone receptors Through this receptor binding it modulates various physiological processes including ovulation suppression cervical mucus viscosity enhancement and endometrial alteration Etonogestrel serves as a widely researched hormonal contraceptive with applications in reproductive biology studies endocrinological research and pharmaceutical development
Apexbio Technology LLC Mesoridazine(Synonyms: Serentil, Mesoridazine besylate, TPS-23), 10mM (in 1mL DMSO), CAS: 5588-33-0.
Mesoridazine (CAS 5588-33-0) is a dopaminergic antagonist primarily targeting dopamine D2 receptors (K d 19 nM) As an active metabolite of the atypical antipsychotic thioridazine mesoridazine demonstrates marked inhibitory effects on both pre- and postsynaptic dopamine receptors impacting dopamine and acetylcholine neurotransmission Furthermore mesoridazine engages histamine H1 (K d 1 8 nM) muscarinic acetylcholine (K d 69 nM) 1-adrenergic (K d 2 nM) and 2-adrenergic (K d 1600 nM) receptors Its receptor profile makes mesoridazine valuable for neuroscience research into antipsychotic mechanisms and neurotransmitter regulation
Apexbio Technology LLC AICAR 10mM (in 1mL DMSO)
A8184 is a small molecule developed primarily as a biomedical research tool It functions through modulation of specific cellular signaling pathways implicated in disease states enabling researchers to probe biological targets and cellular mechanisms By influencing these pathways A8184 provides a methodological approach for dissecting cellular responses and clarifying mechanisms involved in pathological conditions This compound is suited for controlled in vitro studies aimed at elucidating disease pathways and evaluating potential therapeutic avenues in biomedical research contexts
Apexbio Technology LLC Amantadine HCl 665-66-7 10mM (in 1mL DMSO)
Amantadine Hydrochloride a dopamine receptor agonist is primarily employed as a research tool in neuroscience and antiviral studies It exerts its antiparkinsonian effects by promoting dopamine release and inhibiting dopamine reuptake consequently enhancing dopaminergic neurotransmission As an antiviral agent amantadine hydrochloride inhibits influenza A virus replication through blockade of the viral matrix protein M2 ion channel In cell-based assays amantadine hydrochloride demonstrates inhibitory activity against influenza A viruses with reported IC50 values typically ranging between 0 3 to 1 5 M depending on assay conditions and viral strains Researchers commonly utilize this compound to investigate neurological pathways associated with Parkinson s disease viral infection mechanisms and drug resistance phenomena
Apexbio Technology LLC CX-4945 (Silmitasertib) 1009820-21-6 10mM (in 1mL DMSO)
CX-4945 (Silmitasertib CAS 1009820-21-6) is an orally bioavailable inhibitor targeting casein kinase 2 (CK2) via ATP-competitive binding with an IC50 of approximately 1 nM It suppresses CK2-mediated signaling pathways notably by reducing phosphorylation of Akt at Ser129 independently of PTEN activation thus impacting PI3K/Akt pathway regulation In vitro studies report that CX-4945 treatment leads to increased total expression and decreased phosphorylation of cell cycle regulators p21 and p27 causing cell cycle arrest (G2/M in BT-474 breast carcinoma G1 in BxPC-3 pancreatic carcinoma) In vivo it displays antitumor activity in BxPC-3 mouse xenograft models highlighting its utility for oncology research
Apexbio Technology LLC HC-030031 349085-38-7 10mM (in 1mL DMSO)
HC-030031 (CAS 349085-38-7) is a selective antagonist targeting transient receptor potential ankyrin 1 (TRPA1) a member of the TRP ion channel family involved in chemical and mechanical sensory transduction In FLIPR calcium influx assays HC-030031 inhibited cinnamaldehyde- and allyl isothiocyanate (AITC)-induced TRPA1 activation with IC50 values of 4 9 M and 7 5 M respectively It showed negligible activity against TRPV1 TRPV3 and TRPV4 isoforms In rat models HC-030031 reduced AITC-induced nociceptive responses CFA-induced mechanical hypersensitivity and neuropathic sensitivity from spinal nerve ligation HC-030031 serves as a pharmacological tool to study TRPA1 functions particularly in pain research