Dimethyl Sulfoxide
Apexbio Technology LLC Chlorpromazine HCl 69-09-0 10mM (in 1mL DMSO)
Chlorpromazine HCl (CAS 69-09-0) is a phenothiazine-based dopamine receptor antagonist with significant activity at G protein-coupled dopamine receptors in the central nervous system Mechanistically chlorpromazine directly binds to dopamine receptors competitively inhibiting receptor-ligand interactions as evidenced by its inhibition of [ H]spiperone binding in vitro In vivo studies indicate chronic chlorpromazine administration in rats induces behavioral sensitization and altered motor responses linked to DA and NMDA receptor function Clinically chlorpromazine is established as a conventional antipsychotic approved for schizophrenia treatment making it valuable in neuropharmacology research
Apexbio Technology LLC Clopidogrel 120202-66-6 10mM (in 1mL DMSO)
Clopidogrel (CAS 120202-66-6) is a selective antagonist targeting the platelet P2Y receptor thereby preventing ADP-mediated platelet activation and aggregation Through this mechanism clopidogrel exhibits pronounced antithrombotic properties reducing thrombus formation It is the pharmacologically active enantiomer derived from racemic ( )-clopidogrel hydrochloride Clopidogrel is widely employed in biomedical research examining platelet function thrombosis pathways and therapeutic interventions targeting cardiovascular disease
Apexbio Technology LLC SP 600125 129-56-6 10mM (in 1mL DMSO)
SP 600125 (CAS 129-56-6) is a selective reversible ATP-competitive inhibitor of c-Jun N-terminal kinase (JNK) with reported IC50 values of 40 nM for JNK1 and JNK2 and 90 nM for JNK3 Initially identified via GST-c-Jun substrate and recombinant human JNK2 screening assays SP 600125 demonstrates marked specificity being approximately 300-fold more selective toward JNK isoforms compared to ERK1 and p38-2 kinases In cellular assays SP 600125 effectively suppresses JNK-mediated phosphorylation of c-Jun and attenuates expression of IL-2 IFN- and TNF- It is widely utilized in inflammation and signal transduction research
Apexbio Technology LLC MDL 28170 88191-84-8 10mM (in 1mL DMSO)
MDL 28170 (CAS 88191-84-8) is a selective inhibitor of calpain and cathepsin B with Ki values of approximately 10 nM and 25 nM respectively It acts by directly blocking the catalytic site of these cysteine proteases without inhibiting serine proteases MDL 28170 readily penetrates the blood-brain barrier inhibiting protease activity in brain tissue and mitigating ischemia-induced neurological damage in animal models The compound reduces muscle fiber sensitivity to calcium influx post-ischemia and limits myocardial injury caused by calcium overload It also exhibits antiparasitic activity in vitro significantly lowering Trypanosoma cruzi survival in infected macrophages MDL 28170 is used in biomedical research to study protease-related pathology ischemic injury and parasite-host interactions
Apexbio Technology LLC WZ4002 1213269-23-8 10mM (in 1mL DMSO)
WZ4002 (CAS 1213269-23-8) is an irreversible EGFR tyrosine kinase inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants It potently inhibits autophosphorylation of EGFR mutants including T790M L858R/T790M delE746 A750/T790M L858R and delE746 A750 at low nanomolar Ki values Compared to wild-type EGFR mutant EGFR demonstrates greater sensitivity to WZ4002 at lower concentrations limiting off-target toxicity in normal tissues WZ4002 serves as a research tool for studying EGFR-driven tumorigenesis and therapeutic resistance in oncology models
Apexbio Technology LLC AS 602801 848344-36-5 10mM (in 1mL DMSO)
AS 602801 (CAS 848344-36-5) is a selective small-molecule inhibitor targeting c-Jun N-terminal kinase (JNK) a kinase implicated in immune and apoptotic signaling pathways Preclinical studies indicate that AS 602801 suppresses T-cell proliferation and promotes apoptosis altering gene expression in RRMS-derived CD4 and CD8 T-cells and innate receptor expression in RRMS-associated CD11b cells Animal models show beneficial effects in autoimmune disorders and neuronal apoptosis scenarios Thus AS 602801 is investigated primarily for therapeutic potential in multiple sclerosis and fibrotic conditions
Apexbio Technology LLC Tirapazamine(Synonyms: SR-4233, WIN 59075, Tirazone, TPZ, 3-Amino-1,2,4-benzotriazine 1,4-dioxide), 10mM (in 1mL DMSO), CAS: 27314-97-2.
Tirapazamine (CAS 27314-97-2) also known as SR259075 Win59075 or SR4233 is an investigational anticancer agent selectively activated under hypoxic conditions characteristic of solid tumors The compound is bioreduced in hypoxic tumor microenvironments to cytotoxic free radicals leading to cellular damage Tirapazamine downregulates hypoxia-inducible factor-1 (HIF-1 ) thereby influencing pathways associated with tumor adaptive mechanisms to hypoxia Combined treatment with tirapazamine and topoisomerase I inhibitors (such as SN-38 the active metabolite of irinotecan) enhances apoptosis via mitochondria-mediated caspase activation and weakened DNA repair signaling Preclinical investigations including hepatocellular carcinoma xenografts confirm this enhanced tumor suppression Clinical trials evaluating tirapazamine s anticancer efficacy are ongoing
Apexbio Technology LLC (+)-Bicuculline 485-49-4 10mM (in 1mL DMSO)
( )-Bicuculline is a competitive antagonist of gamma-aminobutyric acid type A (GABA A) receptors frequently employed as a pharmacological tool to elucidate the functional roles of inhibitory neurotransmission mediated by GABA A By antagonizing GABA binding this compound prevents chloride ion influx leading to reductions in neuronal inhibitory postsynaptic potentials (IPSPs) Additionally ( )-Bicuculline blocks small conductance calcium-activated potassium (SK) channels affecting neuronal excitability and firing patterns It is commonly utilized in electrophysiological studies such as patch-clamp or extracellular recordings to investigate synaptic transmission neuroplasticity mechanisms and epileptic activity models ( )-Bicuculline inhibits GABA A receptors with an IC 50 typically reported in the low micromolar range (approximately 2 5 M)
Apexbio Technology LLC Pirfenidone 53179-13-8 10mM (in 1mL DMSO)
Pirfenidone (CAS 53179-13-8) is a small molecule antifibrotic agent exhibiting anti-inflammatory properties Mechanistically pirfenidone reduces levels of pro-inflammatory mediators notably TNF- via translational regulation independent of MAPK pathway activation It suppresses TGF- -mediated signaling and extracellular matrix protein production contributing to decreased fibrotic responses in cellular and animal models In vivo pirfenidone administration mitigates fibrosis and inflammatory cytokine expression in tissues such as lung liver and kidney Clinically pirfenidone is investigated primarily for idiopathic pulmonary fibrosis demonstrating reductions in fibrosis progression and improved functional parameters
Apexbio Technology LLC Alexidine dihydrochloride 1715-30-6 10mM (in 1mL DMSO)
Alexidine dihydrochloride is a selective inhibitor targeting mitochondrial protein tyrosine phosphatase 1 (PTPMT1) exhibiting inhibitory activity with an IC50 value of approximately 1 08 M in vitro By inhibiting PTPMT1 Alexidine dihydrochloride modulates mitochondrial signaling pathways implicated in cellular metabolism Additionally this compound enhances insulin secretion in pancreatic -cells of rat islet models In cancer biology research Alexidine dihydrochloride demonstrates activity against FaDu cells providing a relevant tool for studying mitochondrial phosphatase-mediated mechanisms in oncology and diabetes-related research applications
Apexbio Technology LLC LY364947 396129-53-6 10mM (in 1mL DMSO)
LY364947 (CAS 396129-53-6) is a selective inhibitor targeting the kinase domain of transforming growth factor- (TGF- ) type I receptor TGF- signaling regulates crucial biological processes such as cell proliferation differentiation and tissue homeostasis In vitro studies demonstrated that LY364947 inhibits the receptor kinase activity with an IC50 of 51 nM effectively suppressing TGF- -dependent luciferase activity in mink lung epithelial cells (p3TP Lux assay) and growth of NIH 3T3 fibroblasts In vivo LY364947 showed protective effects against NMDA-induced retinal degeneration in rats attenuating retinal ganglion cell loss and capillary degradation Thus LY364947 serves as a valuable pharmacological tool in TGF- -related research and associated pathological conditions
Apexbio Technology LLC Acetaminophen 103-90-2 10mM (in 1mL DMSO)
Acetaminophen (paracetamol) is a cyclooxygenase-2 (COX-2) inhibitor widely employed in biomedical studies for investigating analgesic and antipyretic mechanisms Its inhibition of COX-2 enzyme activity occurs with an IC50 of approximately 25 8 M Experimental use includes inducing cellular hepatotoxicity models where acetaminophen exposure triggers glutathione depletion impaired glutathione peroxidase activity and ferroptosis-mediated cell death This makes acetaminophen useful in examining oxidative stress hepatic cell injury and associated cellular response mechanisms in vitro and in animal studies Additionally acetaminophen-mediated toxicity is applicable in screening protective agents or evaluating ferroptosis inhibitors in pharmacological research
Apexbio Technology LLC Kinetin 525-79-1 10mM (in 1mL DMSO)
Kinetin (N6-furfuryladenine) is a natural adenine derivative classified as a cytokinin originating from plant tissues and participates in diverse physiological processes including cell division and cellular differentiation Structurally kinetin contains an adenine core with a furfuryl substituent at position N6 Experimentally kinetin induces apoptosis-like morphological changes nuclear fragmentation and hypoploidy in vitro in various cell types Additionally kinetin contributes to modulation of RNA splicing patterns notably demonstrated through the promotion of exon 20 inclusion in familial dysautonomia models Due to these properties kinetin serves as an investigational tool in studies of RNA processing apoptosis mechanisms and is examined as a potential therapeutic agent in splicing-associated diseases
Selleck Chemical LLC UBCS039, Solution 10mM (1mL in DMSO)
UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.