Dimethyl Sulfoxide
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
Cayman Chemical L-MethIonIn SulfoxIde 10g
A sulfoxide-modified methionine; increases weight gain in weanling mice in the diet at 6.3, 12.6, and 18.9 mmol/g; levels are decreased in patients with vitiligo
Apexbio Technology LLC TG003 300801-52-9 10mM (in 1mL DMSO)
TG003 (CAS 300801-52-9) is a selective inhibitor targeting the Cdc2-like kinase (Clk) family and casein kinase 1 (CK1) Specifically it demonstrates notable potency against mClk1 mClk2 and mClk4 with IC50 values of approximately 20 nM 200 nM and 15 nM respectively TG003 competitively binds with ATP at Clk1 modulating Clk-mediated phosphorylation of serine/arginine-rich (SR) proteins involved in alternative mRNA splicing Studies using HeLa cellular extracts and animal models have shown that TG003 alters splice site selection and pre-mRNA processing suggesting potential utility for investigating RNA splicing regulatory mechanisms
Apexbio Technology LLC VX-809 936727-05-8 10mM (in 1mL DMSO)
VX-809 (CAS 936727-05-8) is a small molecule CFTR corrector that partially restores the functional expression of F508del-CFTR the most common mutation associated with cystic fibrosis (CF) VX-809 stabilizes the misfolded CFTR protein by interacting with its membrane-spanning domain 1 (MSD1) thus facilitating proper maturation and membrane localization In F508del-CFTR-expressing Fischer rat thyroid (FRT) cells VX-809 enhanced CFTR protein processing (EC50 0 1 M) and improved chloride transport (EC50 0 5 M) VX-809 is utilized predominantly as a research tool in CF studies to understand and restore CFTR function often in combination with CFTR potentiators
Apexbio Technology LLC Romidepsin (FK228, depsipeptide) 128517-07-7 10mM (in 1mL DMSO)
Romidepsin (FK228 depsipeptide CAS 128517-07-7) is a small-molecule inhibitor targeting histone deacetylases (HDACs) Initially isolated from Chromobacterium violaceum romidepsin preferentially inhibits class I enzymes HDAC1 and HDAC2 over class II HDAC4 and HDAC6 Inhibition of HDAC activity by romidepsin results in increased histone acetylation promoting transcriptional activation of tumor suppressor genes Mechanistically this compound can trigger cellular differentiation cell-cycle arrest apoptosis and altered gene expression in various malignancies Romidepsin serves as a research tool to investigate epigenetic regulation and has notable anticancer properties in cell models such as neuroblastoma and cutaneous T-cell lymphoma
Apexbio Technology LLC LY2886721 1262036-50-9 10mM (in 1mL DMSO)
LY2886721 (CAS 1262036-50-9) is an orally bioavailable inhibitor of -site amyloid precursor protein cleaving enzyme 1 (BACE1) an aspartyl protease integral to amyloid precursor protein (APP) cleavage and amyloid- (A ) generation LY2886721 inhibits BACE1 activity with an IC50 of approximately 20 3 nM effectively reducing soluble APP and elevating soluble APP in human cell models (HEK293Swe) and neuronal cultures (PDAPP) at IC50 values of 18 7 nM and 10 7 nM respectively In animal models such as PDAPP mice oral LY2886721 administration dose-dependently reduces cerebral A C99 and sAPP levels Due to its BACE1 inhibitory action LY2886721 serves as a valuable tool in Alzheimer s disease research and therapeutic development
Apexbio Technology LLC CB-5083 1542705-92-9 10mM (in 1mL DMSO)
CB-5083 (CAS 1542705-92-9) is an orally bioavailable small-molecule inhibitor targeting the AAA ATPase p97 (also termed valosin-containing protein VCP) P97 functions in diverse cellular processes related to protein homeostasis including membrane fusion intracellular trafficking and degradation pathways CB-5083 selectively inhibits the second ATPase domain of p97 (IC50 15 4 nM) promoting cytoplasmic protein degradation and triggering apoptosis in cultured cancer cell lines such as A549 and HCT116 In vivo orally administered CB-5083 demonstrates significant reduction of tumor growth in xenograft models The compound is being investigated clinically for treatment of solid tumors and multiple myeloma
Apexbio Technology LLC JSH-23 749886-87-1 10mM (in 1mL DMSO)
JSH-23 (CAS 749886-87-1) is a small-molecule inhibitor of NF- B transcriptional activity exhibiting an IC50 of approximately 7 1 M Mechanistically JSH-23 prevents NF- B-mediated gene transcription by reducing nuclear localization and DNA binding activity of the NF- B p65 subunit without interfering with I B degradation In LPS-stimulated RAW 264 7 macrophages JSH-23 decreases expression of pro-inflammatory mediators including IL-6 IL-1 COX-2 and TNF- and inhibits apoptotic chromatin condensation This compound serves as a research tool for studying NF- B signaling and related inflammatory processes
Apexbio Technology LLC OTX-015 202590-98-5 10mM (in 1mL DMSO)
OTX-015 (CAS 202590-98-5) is a selective inhibitor of BRD2 BRD3 and BRD4 proteins within the BET (bromodomain and extra-terminal) family involved in transcriptional regulation By disrupting the interaction between these BRD proteins and acetylated histone H4 OTX-015 exhibits inhibitory activity demonstrated by IC50 values between 92 and 112 nM and in vitro EC50 ranging from 10 to 19 nM OTX-015 treatment reduces proliferation (GI50 60 200 nM) induces G1 arrest and promotes apoptosis in various human cancer cell models In xenograft mouse studies of BRD-NUT midline carcinoma orally administered OTX-015 significantly suppresses tumor growth showing potential utility for cancer research
Apexbio Technology LLC Vinorelbine 71486-22-1 10mM (in 1mL DMSO)
Vinorelbine is a semisynthetic vinca alkaloid derived from the plant Catharanthus roseus (L ) G Don Structurally characterized by its ability to bind selectively to tubulin this compound inhibits microtubule polymerization and disrupts mitotic spindle function leading to cell cycle arrest in metaphase and subsequent apoptosis Due to these antimitotic properties vinorelbine is extensively employed in biomedical research focused on investigating cell proliferation mechanisms understanding tumor biology and evaluating cytotoxicity profiles in vitro and in vivo Commonly utilized as a chemotherapy agent it serves as a research tool in studies of cancer pharmacology and drug resistance modeling Vinorelbine must be stored in a properly sealed container under cool dry conditions to maintain its chemical stability and biological activity for experimental use
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 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 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
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