Dimethyl Sulfoxide
Apexbio Technology LLC JNJ-7706621 443797-96-4 10mM (in 1mL DMSO)
JNJ-7706621 (CAS 443797-96-4) is an inhibitor targeting cyclin-dependent kinases (CDKs) and Aurora kinases specifically CDK1 (IC50 0 009 mol/L) CDK2 (0 004 mol/L) CDK3 (0 003 mol/L) CDK4 (0 058 mol/L) CDK6 (0 253 mol/L) Aurora A (0 011 mol/L) and Aurora B (0 015 mol/L) It selectively reduces proliferation of tumor cells relative to normal human cells with approximately 10-fold higher specificity Independent of cellular status of p53 retinoblastoma protein or p-glycoprotein expression JNJ-7706621 induces apoptosis suppresses colony formation and inhibits growth highlighting its utility in cancer research
Apexbio Technology LLC MI-77301 (SAR405838) 1303607-60-4 10mM (in 1mL DMSO)
MI-77301 (SAR405838 CAS 1303607-60-4) is a selective antagonist targeting the murine double minute 2 (MDM2) protein an E3 ubiquitin ligase responsible for negatively regulating tumor-suppressor p53 via ubiquitination and degradation By inhibiting the MDM2-p53 interaction (Ki 0 88 nM) MI-77301 stabilizes p53 elevates protein levels of p53 p21 and MDM2 and induces apoptosis Preclinical studies demonstrate selective growth inhibition in tumor cell lines harboring wild-type p53 (e g SJSA-1 RS4 11 LNCaP HCT-116) and potent tumor regressions in corresponding xenograft mouse models highlighting its utility for mechanistic studies and cancer therapeutic research
Apexbio Technology LLC Tigecycline 220620-09-7 10mM (in 1mL DMSO)
Tigecycline is a glycylcycline-class antibiotic developed as a structural derivative of tetracycline antibiotics It exerts antimicrobial activity by reversibly binding to the bacterial 30S ribosomal subunit leading to inhibition of protein synthesis Tigecycline demonstrates bacterial growth inhibition in both Gram-positive and Gram-negative pathogens including multidrug-resistant strains In vitro studies showed minimal inhibitory concentration (MIC90) values ranging between 0 12-0 5 g/ml against vancomycin-sensitive and resistant Enterococcus faecalis and Enterococcus faecium In animal infection models using MRSA strains Tigecycline displays in vivo efficacy with an ED50 approximately 0 72 mg/kg This antibiotic is commonly employed in research studies focusing on resistant bacterial infections such as complicated skin infections and intra-abdominal infections
Apexbio Technology LLC Torsemide 56211-40-6 10mM (in 1mL DMSO)
Torsemide a pyridine-sulfonyl urea derivative acts pharmacologically as a loop diuretic by selectively inhibiting the Na -K -2Cl cotransporter (NKCC2) located in the thick ascending limb of Henle s loop Through this mechanism torsemide reduces sodium chloride and water reabsorption resulting in increased urinary excretion of electrolytes and water Chemically characterized by a sulfonylurea moiety linked to pyridine functionality torsemide is utilized in pharmacological research to investigate kidney function fluid-electrolyte balance and associated physiological responses Additionally researchers employ torsemide as a tool compound to study ion transport regulation pathways and the pathophysiology underlying edema and hypertension at a molecular and cellular level
Apexbio Technology LLC Bedaquiline 843663-66-1 10mM (in 1mL DMSO)
Bedaquiline a diarylquinoline antibiotic targets Mycobacterium tuberculosis via dual inhibition of subunits c and within the bacterial F1FO-ATP synthase complex disrupting ATP production It is applied primarily in research addressing multi-drug resistant (MDR) tuberculosis Recent studies have expanded its use into oncology where bedaquiline inhibits mitochondrial respiratory function and reduces glycolytic activity in cancer stem-cell-like populations In vitro experiments employing breast cancer MCF7 cells revealed bedaquiline increased ROS levels and reduced mitochondrial membrane potential Reported IC50 values for growth inhibition range approximately 1-10 M depending on cell lines and experimental conditions
Apexbio Technology LLC Preladenant 377727-87-2 10mM (in 1mL DMSO)
Preladenant is a potent and selective antagonist targeting the adenosine A2A receptor (Ki 1 1 nM) developed from structural modifications of SCH 58261 Structurally it is a methoxy derivative carrying enhanced affinity and selectivity towards human and rat A2A receptors over A1 A2B and A3 subtypes Mechanistically Preladenant competitively blocks A2A receptor-mediated adenylate cyclase activation In preclinical studies Preladenant reduces Parkinsonian symptoms in primate and rodent models alone or in combination with L-Dopa thus widely employed in experimental research for Parkinson s disease and associated movement disorders
Apexbio Technology LLC Chlorquinaldol 72-80-0 10mM (in 1mL DMSO)
Chlorquinaldol is a synthetic antimicrobial agent exhibiting antifungal and antibacterial properties commonly utilized in biomedical research for evaluating local antiseptic mechanisms It functions primarily through disrupting microbial membrane integrity and interfering with essential enzymatic pathways ultimately limiting microbial proliferation Chlorquinaldol is frequently employed in vitro for susceptibility testing and characterizing antimicrobial activity against various fungal and bacterial strains In experimental assays its antifungal activity is evaluated through measurement of inhibitory concentrations with reported IC50 values typically ranging between 10-50 g/mL depending on specific microorganism types and assay conditions This compound serves as a reference tool in microbiological studies addressing drug susceptibility resistance evaluation and antiseptic compound benchmarking
Apexbio Technology LLC Methotrexate 59-05-2 10mM (in 1mL DMSO)
Methotrexate is a folate antagonist commonly utilized in biomedical research due to its inhibitory action on dihydrofolate reductase (DHFR) a critical enzyme in folate metabolism This inhibition disrupts nucleotide synthesis thereby interfering with cell proliferation Upon cell uptake methotrexate is converted intracellularly into polyglutamate derivatives which prolong its biochemical activity through sustained enzyme inhibition Additionally methotrexate promotes extracellular adenosine release at inflammatory sites mediating immunological effects In cellular assays for DHFR inhibition methotrexate demonstrates potent inhibitory activity with reported IC50 values typically ranging from 5 to 50 nM depending on the cell type and experimental conditions Methotrexate is widely utilized in research on inflammation oncology and rheumatoid arthritis-related mechanisms
Apexbio Technology LLC Gefitinib (ZD1839) 184475-35-2 10mM (in 1mL DMSO)
Gefitinib (ZD1839 CAS 184475-35-2) is an orally bioavailable small-molecule inhibitor that specifically targets epidermal growth factor receptor (EGFR) tyrosine kinase Acting competitively by occupying the ATP-binding domain of EGFR gefitinib blocks ATP interaction and thereby inhibits EGFR autophosphorylation and downstream signaling In biochemical assays gefitinib demonstrates IC50 values of 0 033 M and 0 027 M against EGFR tyrosine kinase activity in A431 membrane preparations and baculovirus lysates respectively Consequently gefitinib suppresses tumor proliferation induces apoptosis and exhibits activity in models of various solid tumors including lung colorectal breast head and neck prostate and ovarian cancers
Apexbio Technology LLC Raltitrexed 112887-68-0 10mM (in 1mL DMSO)
Raltitrexed (CAS 112887-68-0) also known as Tomudex or ZD 1694 is a small-molecule antimetabolite utilized primarily in oncology research As a thymidylate synthase inhibitor raltitrexed disrupts DNA synthesis by impeding nucleotide biosynthesis thereby exerting cytotoxic effects against rapidly dividing tumor cells The compound serves as a tool in cancer studies aimed at elucidating thymidylate synthase s role in tumor cell proliferation and evaluating antitumor therapeutic approaches targeting this enzymatic pathway
Apexbio Technology LLC Tie2 kinase inhibitor 948557-43-5 10mM (in 1mL DMSO)
Tie2 kinase inhibitor (CAS 948557-43-5) is a selective and reversible small-molecule inhibitor targeting the Tie2 receptor tyrosine kinase a critical modulator of endothelial cell survival angiogenesis and vascular integrity By inhibiting Tie2 autophosphorylation this compound disrupts subsequent signaling pathways involved in endothelial maturation and tumor-associated angiogenesis In vitro studies demonstrate potent inhibition of Tie2 kinase activity (IC50 0 25 M) with substantial selectivity over other kinases including p38 In vivo treatment reduces angiogenesis and tumor progression in murine xenograft tumor models This inhibitor is thus relevant for research examining angiogenic mechanisms and cancer progression
Apexbio Technology LLC AdipoRon 924416-43-3 10mM (in 1mL DMSO)
AdipoRon (CAS 924416-43-3) is an agonist of adiponectin receptors AdipoR1 and AdipoR2 displaying binding affinities (Kd) of 1 8 M and 3 1 M respectively Upon receptor activation it promotes phosphorylation of AMPK via AdipoR1 and upregulates expression of PGC-1 improving mitochondrial biogenesis in muscle cell models In vivo studies show that AdipoRon administration stimulates AMPK and PPAR- signaling in liver and muscle tissues subsequently reducing circulating glucose insulin triglycerides and inflammatory cytokines This compound is employed in metabolic and cardiovascular disease research especially regarding insulin resistance dyslipidemia obesity-related inflammation and ischemia-induced myocardial damage
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 17-AAG (KOS953) 75747-14-7 10mM (in 1mL DMSO)
17-AAG (KOS953) is a synthetic derivative of geldanamycin that inhibits heat shock protein 90 (HSP90) It acts by binding to HSP90 causing destabilization of client proteins including HER2 Raf-1 p53 and components of MAPK signaling pathways Reported IC50 for 17-AAG in BT474 cells is approximately 6 nM Its biological activity has been investigated broadly including in multiple myeloma breast cancer thyroid cancer Hodgkin lymphoma and melanoma cellular models Ongoing studies explore 17-AAG both as monotherapy and in combination with agents like bortezomib or trastuzumab for addressing treatment-resistant cancer cell lines Currently 17-AAG is evaluated in Phase II clinical trials