Dimethyl Sulfoxide
Apexbio Technology LLC PF-562271 HCl 939791-41-0 10mM (in 1mL DMSO)
PF-562271 HCl (CAS 939791-41-0) is a potent ATP-competitive reversible inhibitor targeting focal adhesion kinase (FAK) and its homolog proline-rich tyrosine kinase 2 (Pyk2) It inhibits FAK and Pyk2 enzymatic activity with reported IC50 values of 1 5 nmol/L and 14 nmol/L respectively FAK is a non-receptor tyrosine kinase regulating cell adhesion migration and growth while Pyk2 shares structural similarity to FAK In animal models of cancer PF-562271 reduces tumor progression and metastatic spread with dose-dependent suppression of FAK phosphorylation (EC50 93 ng/mL) Thus PF-562271 serves as an important tool for investigating FAK/Pyk2-mediated pathways in oncology research
Apexbio Technology LLC PTC124 (Ataluren) 775304-57-9 10mM (in 1mL DMSO)
PTC124 (Ataluren CAS 775304-57-9) is a small molecule modulator that selectively targets premature termination codons (nonsense mutations) which are point mutations causing early termination during translation By promoting ribosomal read-through of these mutations PTC124 enhances the synthesis of full-length functional proteins In vitro studies demonstrated its activity at IC50 of approximately 0 1 M Research in MDX mouse skeletal muscle cells and human induced pluripotent stem cell-derived retinal pigment epithelium cells confirmed its capacity to restore protein production Animal models of Duchenne muscular dystrophy and cystic fibrosis exhibited improved muscle and channel protein function upon oral or subcutaneous administration suggesting its potential for addressing genetic diseases associated with nonsense mutations
Apexbio Technology LLC Sephin1 13098-73-2 10mM (in 1mL DMSO)
Sephin1 (CAS 13098-73-2) is a selective inhibitor of PPP1R15A a regulatory subunit of protein phosphatase 1 involved in the regulation of stress-induced eIF2 dephosphorylation Under endoplasmic reticulum (ER) stress phosphorylated eIF2 attenuates protein synthesis preventing accumulation of misfolded proteins By inhibiting PPP1R15A Sephin1 sustains eIF2 phosphorylation extending translational attenuation during ER stress In cell assays Sephin1 selectively disrupts PPP1R15A-PP1c complexes without affecting PPP1R15B-mediated complexes In mouse models harboring misfolded protein mutations (e g MPZ or SOD1) Sephin1 administration mitigates molecular cellular and functional deficits thus relevant for proteostasis-related disease studies
Apexbio Technology LLC Levosimendan 141505-33-1 10mM (in 1mL DMSO)
Levosimendan (CAS 141505-33-1) is a small molecule calcium sensitizer that exerts its pharmacological action by binding selectively and in a calcium-dependent manner to cardiac troponin C (cTnC) Through this interaction levosimendan facilitates cardiac muscle contraction without significantly increasing intracellular calcium concentrations Research indicates utility in heart failure treatment where improved myocardial contractility is therapeutically desirable Currently levosimendan is evaluated extensively in Phase 4 clinical studies to explore its efficacy and therapeutic profile
Apexbio Technology LLC PD 173074 219580-11-7 10mM (in 1mL DMSO)
PD 173074 (CAS 219580-11-7) is a selective inhibitor targeting fibroblast growth factor receptors (FGFR) exerting its effects by suppressing FGFR tyrosine kinase phosphorylation It has demonstrated dose-dependent inhibitory activity against small cell lung cancer (SCLC) cell lines including H-510 and H-69 by reducing their proliferation colony formation and FGF-2 induced chemotherapy resistance in vitro In murine xenograft models of SCLC PD 173074 reduced tumor progression and significantly prolonged animal survival achieving durable complete responses in some cases PD 173074 represents an important tool compound for investigating the oncogenic role of FGFR signaling in cancer research
Apexbio Technology LLC Verteporfin 129497-78-5 10mM (in 1mL DMSO)
Verteporfin (CAS 129497-78-5) is a porphyrin-derived small molecule used as a photosensitizer in photodynamic therapy (PDT) Upon photoactivation verteporfin induces targeted vascular endothelial cytotoxicity through intravascular damage and thrombosis formation leading to selective vessel closure Experimental studies indicate verteporfin treatment triggers DNA fragmentation and enhances apoptotic events in vitro displaying potent cytotoxicity against HL-60 cells at concentrations around 100 ng/mL Independently of photoactivation verteporfin also directly modifies and inhibits the autophagy adaptor protein p62 impacting its binding to polyubiquitinated substrates Verteporfin is relevant to biomedical research involving PDT mechanisms autophagy pathways and angiogenesis
Apexbio Technology LLC Ezetimibe 163222-33-1 10mM (in 1mL DMSO)
Ezetimibe (CAS 163222-33-1) is a cholesterol absorption inhibitor that targets the intestinal cholesterol transporter Niemann-Pick C1 Like 1 (NPC1L1) It reduces intestinal uptake of cholesterol and dietary carotenoids including - and -carotene lycopene lutein and -cryptoxanthin through downregulating transport proteins such as SR-BI ABCA1 NPC1L1 and transcription factors including SREBP-1/-2 and LXR- In ApoE-deficient mouse models ezetimibe significantly decreases plasma cholesterol levels and attenuates atherosclerotic lesion formation Clinically it lowers LDL cholesterol total cholesterol and triglycerides while elevating HDL cholesterol
Apexbio Technology LLC AZD8931 (Sapitinib) 848942-61-0 10mM (in 1mL DMSO)
AZD8931 (Sapitinib CAS 848942-61-0) is a reversible small-molecule inhibitor that targets EGFR (HER1) HER2 (erbB2) and HER3 (erbB3) with similar potency It suppresses receptor phosphorylation with IC50 values of 4 nM (EGFR) 3 nM (HER2) and 4 nM (HER3) Preclinical studies using HER2-non-amplified inflammatory breast cancer (IBC) cell lines demonstrate reduced tumor cell proliferation and increased apoptosis upon AZD8931 administration In mouse xenograft models AZD8931 alone or combined with paclitaxel significantly delays tumor growth AZD8931 is under clinical evaluation as combination therapy in advanced breast cancer
Apexbio Technology LLC MK-1775 955365-80-7 10mM (in 1mL DMSO)
MK-1775 (CAS 955365-80-7) is a selective inhibitor targeting Wee1 kinase a nuclear Ser/Thr kinase involved in regulating entry into mitosis Mechanistically it inhibits Wee1-mediated Tyr15 phosphorylation of cyclin-dependent kinase 1 (CDC2) thus activating CDC2 and disrupting the G2 DNA damage checkpoint MK-1775 exhibits potent inhibition of Wee1 kinase with an in vitro IC50 of 5 2 nM and demonstrates substantial selectivity over related kinases including Myt1 In cell models harboring mutant p53 (e g WiDr) co-treatment with MK-1775 sensitizes tumor cells to DNA-damaging agents such as gemcitabine carboplatin and cisplatin highlighting its utility in cancer research
Apexbio Technology LLC HATU 148893-10-1 10mM (in 1mL DMSO)
HATU (1-[Bis(dimethylamino)methylene]-1H-1 2 3-triazolo[4 5-b]pyridinium 3-oxid hexafluorophosphate) is a peptide coupling reagent routinely employed for amide-bond formation in peptide synthesis and other biomolecular applications In solution HATU converts carboxylic acids into active ester intermediates (OAt esters) facilitating subsequent nucleophilic attack from amines or alcohols This reaction typically proceeds in presence of basic additives such as N N-Diisopropylethylamine (DIPEA) under anhydrous conditions in solvents like dimethylformamide (DMF) Its utility extends to synthesizing peptides and modifying biomolecules through ester or amide linkage formation widely applied in biomedical research and pharmaceutical laboratories
Apexbio Technology LLC Fluvastatin Sodium 93957-55-2 10mM (in 1mL DMSO)
Fluvastatin Sodium (CAS 93957-55-2) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase the rate-limiting enzyme in cholesterol biosynthesis By blocking HMG-CoA reductase activity fluvastatin reduces serum total cholesterol LDL-cholesterol and apolipoprotein B while increasing HDL-cholesterol and apolipoprotein A-I levels In research settings fluvastatin exhibits anti-atherosclerotic anti-thrombotic and antioxidant properties Studies have shown fluvastatin decreases platelet aggregation dose-dependently in vitro reducing platelet aggregation by approximately 10-15% at clinical doses (40 mg/day) Additionally fluvastatin inhibits inflammatory angiogenesis and NO production suggesting potential applications in inflammatory and cardiovascular 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 Mirabegron (YM178) 223673-61-8 10mM (in 1mL DMSO)
Mirabegron (YM178 CAS 223673-61-8) is a selective agonist targeting the -adrenergic receptor ( -AR) Activation of -AR influences physiological responses in tissues including adipose cells prostate gastrointestinal tract and primarily the urinary bladder In CHO cells expressing human -adrenergic receptor subtypes mirabegron demonstrated selective agonist properties at -AR (EC 22 4 nM) showing minimal activity at - and -AR subtypes Animal studies revealed mirabegron reduced rhythmic bladder contraction frequency without affecting amplitude Its selective -AR agonist profile makes mirabegron pertinent for research on bladder dysfunction particularly overactive bladder conditions
Apexbio Technology LLC Cefoperazone 62893-19-0 10mM (in 1mL DMSO)
Cefoperazone is a third-generation cephalosporin antibiotic with broad-spectrum antibacterial activity widely applied in biomedical research focused on transport-related mechanisms It exhibits inhibitory effects on rMrp2-mediated transport of [ 3H]estradiol-17 -glucuronide ([ 3H]E217 G) with a reported IC50 value of approximately 199 M Importantly the inhibitory profile of cefoperazone displays biphasic characteristics suggesting distinct binding sites the obtained IC50 values are 6 66 3 23 M (high-affinity component) and 3 88 1 32 mM (low-affinity component) These properties facilitate its use as a probe compound to assess transport pathways in pharmacokinetic and drug disposition studies
Apexbio Technology LLC Dofetilide 115256-11-6 10mM (in 1mL DMSO)
Dofetilide (CAS 115256-11-6) chemically designated as UK 68789 is a class III antiarrhythmic small molecule that selectively inhibits the rapid delayed rectifier potassium channel (IKr) This inhibition leads to prolonged ventricular action potential duration and extended effective refractory periods in cardiac cells Noted for favorable oral bioavailability Dofetilide is extensively utilized in cardiac electrophysiological research including studies aimed at elucidating arrhythmogenic mechanisms linked to IKr channel function assessing novel antiarrhythmic candidates and exploring physiological and pathological aspects of cardiac rhythm regulation