Dimethyl Sulfoxide
Apexbio Technology LLC Ivacaftor (VX-770)(Synonyms: Kalydeco, VX-770, Ivacaftor, CFTR Potentiator VX-770, Ivacaftor VX-770), 10mM (in 1mL DMSO), CAS: 873054-44-5.
Ivacaftor (VX-770 CAS 873054-44-5) is an orally bioavailable small molecule potentiator targeting the cystic fibrosis transmembrane conductance regulator (CFTR) Ivacaftor enhances CFTR-mediated chloride ion transport especially in cells expressing G551D- or F508del-CFTR mutations In vitro studies demonstrated that Ivacaftor in combination with forskolin significantly increased CFTR-dependent chloride secretion (EC50 100 nM in G551D- 25 nM in F508del-expressing cells) Similarly Ivacaftor reduced ENaC-mediated sodium reabsorption and increased airway surface liquid volume in human cystic fibrosis bronchial epithelial cells Ivacaftor is utilized in research to investigate CFTR function restoration and associated ion transport processes
Apexbio Technology LLC Tiplaxtinin(PAI-039)(Synonyms: Tiplaxtinin, PAI-039, Tiplaxtinin (PAI-039), Tiplaxitin, PAI1 inhibitor, PAI-1 antagonist, RWJ-676070), 10mM (in 1mL DMSO), CAS: 393105-53-8.
Tiplaxtinin (PAI-039 CAS 393105-53-8) is an orally bioavailable small molecule inhibitor targeting plasminogen activator inhibitor-1 (PAI-1) a physiological regulator of the plasminogen activation system Elevated PAI-1 levels stabilize thrombi by inhibiting tissue- and urokinase-type plasminogen activators Tiplaxtinin binds selectively to PAI-1 with a Kd of approximately 480 nM and inhibits its activity with an IC50 value around 2 7 M In animal models oral administration of Tiplaxtinin significantly delayed arterial thrombus-induced occlusion supporting its utility as a research tool for studying fibrinolytic pathways and thrombotic disorders
Apexbio Technology LLC vinblastine 865-21-4 10mM (in 1mL DMSO)
Vinblastine is a naturally-derived alkaloid isolated from Catharanthus roseus It functions as a microtubule inhibitor by binding specifically to tubulin disrupting microtubule polymerization and thereby arresting mitosis at metaphase Due to this mechanism vinblastine is widely investigated for antitumor activities and is commonly employed in biomedical research to study cell division cytoskeletal dynamics and therapeutic interventions in oncology Vinblastine should be stored under sealed dry and cool conditions to maintain molecular integrity and biological activity
Medchemexpress LLC Dimethyl sulfoxide | 67-68-5 | MFCD00002089 | 100.0% | 78.13 g/mol | C2H6OS | 10mL
Dimethyl sulfoxide (DMSO) meets analytical specification of Ch P is an aprotic solvent that dissolves polar and non-polar compounds including water-insoluble therapeutic and toxic agents Dimethyl sulfoxide (DMSO) has a strong affinity for water and can rapidly penetrate or enhance the penetration of other substances into biological membranes Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity Dimethyl sulfoxide also exhibits antifreeze and antibacterial properties[1][2][3] br/ MCE provides Dimethyl sulfoxide that complies with the inspection standards (Ch P) of Part 4 of the Chinese Pharmacopoeia (2020 Edition) Amicrobic low endotoxin can be used in various biochemical experiments such as drug dissolution
Apexbio Technology LLC GMX1778 (CHS828) 200484-11-3 10mM (in 1mL DMSO)
GMX1778 (CHS828 CAS 200484-11-3) is a small-molecule inhibitor targeting nicotinamide phosphoribosyltransferase (NAMPT) an enzyme crucial for NAD biosynthesis with a reported Kd value of 120 nM NAD functions as a cofactor essential for enzymatic oxidation-reduction processes and diverse cellular events including metabolism genomic integrity calcium signaling aging and apoptosis In cultured IM-9 cells exposure to GMX1778 substantially decreases NAD and NM levels in a time-dependent manner GMX1778 displays anti-tumor activity preferentially in NAPRT1-deficient cancer models highlighting its potential utility for investigating metabolic vulnerabilities and targeted cancer therapies
Apexbio Technology LLC R406 841290-81-1 10mM (in 1mL DMSO)
R406 (CAS 841290-81-1) is an orally active inhibitor targeting spleen tyrosine kinase (SYK) a non-receptor tyrosine kinase prominently expressed in hematopoietic cells SYK mediates essential signaling upon activation of immune receptors including Fc and B-cell receptors impacting immune responses platelet activation osteoclast differentiation and vascular development By competitively binding to SYK s ATP-binding pocket R406 disrupts SYK-mediated downstream substrate phosphorylation It potently inhibits IgE- and IgG-induced Fc receptor signaling (IC50 56 64 nM) and blocks SYK-dependent B-cell receptor activation (SYK IC50 41 nM) inducing apoptosis in diffuse large B-cell lymphoma cell lines R406 is utilized in research investigating hematologic malignancies and immune-mediated disorders
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 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 Oseltamivir 196618-13-0 10mM (in 1mL DMSO)
Oseltamivir is a neuraminidase inhibitor targeting influenza virus replication It functions as a prodrug metabolized into oseltamivir carboxylate by host esterases This active metabolite binds to viral neuraminidase thereby blocking cleavage of terminal -Neu5Ac residues and subsequent viral progeny release from infected host cells Oseltamivir has been widely employed in investigative studies addressing antiviral efficacy resistance mechanisms and clinical outcomes in influenza infection research The compound is frequently used in vitro to characterize neuraminidase activity inhibition typically reporting IC50 values in the low nanomolar range (approximately 0 1-5 nM) depending on the influenza viral strain and assay conditions influencing viral replication and transmission
Apexbio Technology LLC Pranlukast 103177-37-3 10mM (in 1mL DMSO)
Pranlukast (CAS 103177-37-3) is a selective antagonist of cysteinyl leukotriene (cysLT) receptors exhibiting its pharmacological action by competitively binding to targeted leukotriene receptor sites It specifically prevents the interaction of endogenous leukotrienes (LTC4 LTD4 LTE4) with corresponding receptors located on pulmonary cell membranes thus reducing leukotriene-driven airway inflammation and bronchoconstriction Binding experiments demonstrate that pranlukast possesses notably greater affinity for LTE4 and LTD4 compared to LTC4 In biomedical research pranlukast is frequently utilized for mechanistic studies and pharmacological modeling of asthma allergic rhinitis and related airway inflammatory conditions
Apexbio Technology LLC EPZ-6438 1403254-99-8 10mM (in 1mL DMSO)
EPZ-6438 is a selective inhibitor targeting EZH2 the catalytic subunit of polycomb repressive complex 2 (PRC2) By competitively binding to EZH2 s S-adenosylmethionine (SAM) pocket EPZ-6438 suppresses EZH2-driven trimethylation of histone H3 lysine 27 (H3K27me3) a key epigenetic modification implicated in transcriptional regulation and oncogenesis This selective inhibition of EZH2 exhibits reduced affinity for EZH1 In biological studies EPZ-6438 has demonstrated anti-tumor activity in preclinical malignant rhabdoid tumor models making it useful for examining EZH2-dependent cancer pathways and epigenetic research
Apexbio Technology LLC Fosaprepitant(Synonyms: Fosaprepitant dimeglumine, Emend IV, L-758298, MK-0517, Fosaprepitant meglumine, Ivemend), 10mM (in 1mL DMSO), CAS: 172673-20-0.
Fosaprepitant (CAS 172673-20-0) also known as MK-0517 or L-758 298 is a selective neurokinin-1 (NK-1) receptor antagonist exerting its pharmacological effects primarily through its active metabolite aprepitant This antagonism blocks substance P-mediated biological effects including vomiting responses In established preclinical models such as the cisplatin-triggered emesis in ferrets fosaprepitant demonstrated activity in mitigating chemotherapy-induced vomiting Given aprepitant s favorable penetration into the central nervous system fosaprepitant exhibits high NK-1 receptor affinity and potentiates antiemetic actions of agents such as dexamethasone and granisetron It is used in combination therapies with 5-HT3 antagonists and corticosteroids for chemotherapy-induced nausea and vomiting (CINV)
Apexbio Technology LLC LY2228820 862507-23-1 10mM (in 1mL DMSO)
LY2228820 (CAS 862507-23-1) is a potent selective ATP-competitive small-molecule inhibitor targeting the and isoforms of p38 mitogen-activated protein kinase (MAPK) with reported IC50 values of 5 3 nM and 3 2 nM respectively By suppressing p38 MAPK signaling LY2228820 decreases phosphorylation of heat shock protein 27 (HSP27) induced by Bortezomib thereby elevating cytotoxic effects in multiple myeloma (MM) models Additionally it inhibits secretion of IL-6 by bone marrow mononuclear cells and stromal cells as well as secretion of MIP-1 by patient-derived MM cell subsets and osteoclast precursors In melanoma (B16-F10) and NSCLC (A549) xenograft murine models LY2228820 reduces phosphorylation of MK2 and slows tumor progression respectively highlighting its potential utility in oncology research