Dimethyl Sulfoxide
Apexbio Technology LLC Darifenacin HBr 133099-07-7 10mM (in 1mL DMSO)
Darifenacin HBr (CAS 133099-07-7) known as UK88525 is a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR M3) It demonstrates high binding affinity (pKi 8 9) toward M3 receptors which mediate smooth muscle contraction and glandular secretion in various tissues In vitro studies reveal that darifenacin acts as a substrate of the P-gp efflux transporter at the blood-brain and blood-ocular barriers In animal models darifenacin modulates bladder contractility and reduces bladder afferent nerve activity Clinically it is employed in research focusing on disorders involving abnormal detrusor muscle activity such as overactive bladder syndrome
Apexbio Technology LLC BI 2536(Synonyms: BI-2536, BI2536, Plk1 inhibitor BI 2536), 10mM (in 1mL DMSO), CAS: 755038-02-9.
BI 2536 (CAS number 755038-02-9) is an ATP-competitive inhibitor selectively targeting human polo-like kinase 1 (PLK1) exhibiting an IC50 value of approximately 0 83 nM Comparatively BI 2536 shows substantially less affinity towards other kinases In vitro studies demonstrate that BI 2536 inhibits proliferation of various human tumor cell lines (EC50 values ranging from 2 to 25 nM) and induces G2/M cell cycle arrest accompanied by apoptosis as evidenced in HeLa cervical cancer cells In vivo data from xenograft tumor models indicate that BI 2536 administered intravenously on a weekly or biweekly schedule possesses antitumor efficacy
Apexbio Technology LLC SB 203580 hydrochloride 869185-85-3 10mM (in 1mL DMSO)
SB 203580 hydrochloride (CAS 869185-85-3) is a selective inhibitor targeting the p38 mitogen-activated protein kinases (MAPKs) specifically isoforms p38-MAPK and p38-MAPK It prevents the downstream phosphorylation and activation of MAP kinase-activated protein kinase 2 (MAPKAPK2) exhibiting an IC50 around 70 nM in neonatal myocytes Additionally SB 203580 hydrochloride inhibits MAPKAPK2 activation and heat shock protein 27 (HSP27) phosphorylation induced by IL-1 osmotic stress or arsenite in KB cells with IC50 values below 1 M It also reduces JNK-mediated activation of c-Jun in neonatal rat cardiac myocytes This compound is widely utilized in research into cellular stress responses inflammation pathways and cardiac signal transduction
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC Carfilzomib (PR-171) 868540-17-4 10mM (in 1mL DMSO)
Carfilzomib (PR-171 CAS 868540-17-4) is a derivative of the natural product epoxomicin and functions as an irreversible inhibitor of the chymotrypsin-like activity within the 20S proteasome Proteasomes play a critical role in intracellular protein degradation thus inhibition results in accumulation of polyubiquitinated proteins Through this mechanism Carfilzomib induces cell cycle arrest and apoptosis consequently suppressing tumor cell growth Research applications primarily involve exploration of its antitumor efficacy and mechanisms in oncology models
Sigma Aldrich Fine Chemicals Biosciences Methyl phenyl sulfoxide >=97% | 1193-82-4 | MFCD00002088 | 25G
Methyl phenyl sulfoxide >=97% | Purity: >=97% | Mol Wt: 140.2 | 1193-82-4 | MFCD00002088 | 25G
Apexbio Technology LLC ANA 12 219766-25-3 10mM (in 1mL DMSO)
ANA 12 (CAS 219766-25-3) is a potent and selective antagonist of tropomyosin receptor kinase B (TrkB) the receptor for neurotrophins BDNF and NT-4/5 It binds non-competitively to extracellular sites on TrkB exhibiting IC50 values of 45 6 nM (high-affinity site) and 41 1 M (low-affinity site) ANA 12 inhibits BDNF-induced TrkB activation effectively blocking downstream signaling pathways including PLC- PI3K and MAPK In mouse models ANA 12 administration reduces endogenous brain TrkB activity and demonstrates antidepressant and anxiolytic properties supporting its use for researching psychiatric disorders and neuronal signaling
Apexbio Technology LLC Disulfiram 97-77-8 10mM (in 1mL DMSO)
Disulfiram (CAS 97-77-8) is a small molecule compound recognized as a copper ionophore facilitating intracellular transport of Cu ions It inhibits inflammasome-dependent pyroptotic cell death IL-1 secretion and gasdermin D (GSDMD)-mediated pore formation in liposomes within human and murine cellular models Mechanistically disulfiram elevates intracellular reactive oxygen species (ROS) concentrations in the presence of copper initiating copper-dependent cell death Additionally disulfiram disrupts the ubiquitin-proteasome protein degradation pathway in tumor cells impairing cellular waste clearance and inducing apoptosis Research demonstrates its potential anti-cancer activity particularly synergistically enhanced by copper supplementation and cardioprotective effects against ischemia-reperfusion-induced damage
Apexbio Technology LLC AZD7762(Synonyms: AZD-7762, AZD 7762, 860352-01-8), 10mM (in 1mL DMSO), CAS: 860352-01-8.
AZD7762 (CAS No 860352-01-8) is an ATP-competitive inhibitor targeting the checkpoint kinases Chk1 and Chk2 regulatory enzymes activated upon DNA damage that control cell-cycle progression through phosphorylation of CDC25 phosphatases By competitively binding the ATP-binding pocket of Chk1 AZD7762 blocks Chk1-mediated phosphorylation of CDC25C exhibiting an IC50 of approximately 5 nM and Ki of 3 6 nM This inhibition prevents DNA damage-induced cell cycle arrest and interrupts DNA repair mechanisms promoting apoptosis in tumor cells Consequently AZD7762 acts as a chemosensitizing agent enhancing the cytotoxic effects of DNA-damaging therapies in oncology research
Apexbio Technology LLC Cobimetinib 934660-93-2 10mM (in 1mL DMSO)
Cobimetinib (CAS 934660-93-2) is a selective small molecule inhibitor targeting mitogen-activated protein kinase kinase (MEK) MEK functions as a kinase that specifically phosphorylates serine/threonine and tyrosine residues playing a critical role in the MAPK signaling cascade and modulating cell proliferation survival migration differentiation and angiogenesis Cobimetinib effectively inhibits MEK with an IC50 value of 0 9 nM demonstrating potent activity in various experimental cancer models including breast cancer cells harboring KRAS and B-RAF mutations In xenograft mouse models it exhibits dose-dependent tumor growth suppression and sustained inhibition of ERK phosphorylation Cobimetinib is currently evaluated in phase I clinical trials as an anticancer therapeutic candidate
Apexbio Technology LLC Epirubicin HCl 56390-09-1 10mM (in 1mL DMSO)
Epirubicin HCl is an anthracycline antibiotic with antitumor activity targeting DNA topoisomerase II (TOPII) It functions by stabilizing TOPII-DNA cleavable complexes resulting in increased DNA double-strand breaks subsequent activation of DNA damage responses and initiation of apoptosis pathways Consequently epirubicin is frequently utilized in anticancer research particularly against osteosarcoma cells Studies demonstrate epirubicin induces apoptosis in osteosarcoma models yet it can also activate resistance pathways such as NF- B affecting therapeutic efficacy The reported IC50 values of epirubicin in osteosarcoma cell lines typically range between approximately 0 1 to 2 M based on experimental conditions This compound is thus actively employed in oncology research exploring DNA-damaging agents or combination therapy strategies in cell-based assays and animal models
Apexbio Technology LLC Elvitegravir (GS-9137) 697761-98-1 10mM (in 1mL DMSO)
Elvitegravir (GS-9137) is an integrase inhibitor targeting HIV-1 which impedes viral DNA integration during the replication cycle of human immunodeficiency virus type 1 (HIV-1) Its mechanism involves inhibition of the integrase enzyme-mediated DNA strand transfer reaction thereby preventing the insertion of viral genetic material into host genomic DNA and subsequently decreasing viral replication Reported inhibitory concentrations (IC50) against HIV-1 integrase range approximately from 7 to 8 nM Besides its application in HIV-1 research Elvitegravir demonstrates inhibitory effects against other retroviral integrases such as murine leukemia virus (MLV) and simian immunodeficiency virus (SIV) making it suitable for broader antiviral research use
Apexbio Technology LLC ABT-737 852808-04-9 10mM (in 1mL DMSO)
ABT-737 (CAS 852808-04-9) is a small molecule inhibitor targeting the BCL-2 protein family exhibiting high binding affinity toward the anti-apoptotic proteins BCL-2 BCL-X L and BCL-w ABT-737 disrupts BCL-2/BAX protein interactions leading to apoptosis primarily via the BAK-mediated intrinsic pathway independent of BIM In preclinical studies ABT-737 demonstrated single-agent antitumor activity in lymphoma multiple myeloma and small-cell lung cancer models Additionally research indicates activity against acute myeloid leukemia (AML) cells progenitor cells and leukemia stem cells while sparing normal hematopoietic populations highlighting its potential for therapeutic research in hematologic malignancies