Dimethyl Sulfoxide
Apexbio Technology LLC GW9662(Synonyms: GW-9662, GW 9662, 2-Chloro-5-nitro-N-phenylbenzamide, PPAR gamma antagonist GW9662), 10mM (in 1mL DMSO), CAS: 22978-25-2.
GW9662 (CAS 22978-25-2) is an antagonist of peroxisome proliferator-activated receptor gamma (PPAR ) a nuclear receptor involved in various biological processes including tumor growth and inflammation GW9662 irreversibly blocks PPAR activity by covalently modifying cysteine residues at its ligand-binding site (IC50 3 3 M) In cellular assays GW9662 inhibits proliferation of breast cancer cell lines (MCF7 MDA-MB-231 MDA-MB-468 IC50 20 30 M) Additionally GW9662 reverses the protective impact of lipopolysaccharide on kidney ischemia/reperfusion injury demonstrating its utility for studying PPAR -mediated pathways in oncology and inflammation models
Apexbio Technology LLC ASC-J9(Synonyms: Dimethylcurcumin, GO-Y025, AR degrader enhancer ASC-J9), 10mM (in 1mL DMSO), CAS: 52328-98-0.
ASC-J9 (CAS 52328-98-0) is a small-molecule degrader targeting androgen receptor (AR) By promoting degradation of full-length AR and splice variants such as AR3/fAR ASC-J9 inhibits androgen receptor signaling pathways involved in castration-resistant prostate cancer (CRPC) progression and metastatic behavior ASC-J9 interferes with AR-dependent transcriptional modulation and AR-independent signaling pathways notably inhibiting STAT3 phosphorylation and CCL2 chemokine secretion thus reducing macrophage infiltration and prostate cancer invasiveness Research indicates ASC-J9 may represent an alternative therapeutic strategy for CRPC treatment and metastasis prevention
Apexbio Technology LLC Meropenem 96036-03-2 10mM (in 1mL DMSO)
Meropenem is a broad-spectrum -lactam antibiotic within the carbapenem subclass characterized by bactericidal activity against both gram-positive and gram-negative organisms It primarily acts by binding to penicillin-binding proteins (PBPs) mainly PBP2 of Escherichia coli and Pseudomonas aeruginosa and PBP1 of Staphylococcus aureus thus disrupting cell wall synthesis and bacterial growth In vitro studies indicate Meropenem inhibition is effective at MIC 4 mg/L (susceptible strains) intermediate at 8 mg/L and resistant at 16 mg/L Meropenem demonstrates greater potency against gram-negative bacteria compared to Imipenem with typical IC50 values around 0 25 mg/L for anaerobic strains It is typically used in microbiological research to investigate antibiotic susceptibility bacterial resistance mechanisms and interactions with drug metabolism
Apexbio Technology LLC Mitomycin C 10mM (in 1mL DMSO)
Mitomycin C (CAS 50-07-7) is an antibiotic compound derived from Streptomyces caespitosus or Streptomyces lavendulae exhibiting anti-cancer properties by interfering with DNA synthesis Its mode of action involves direct formation of covalent adducts with DNA impeding DNA replication In PC3 cells mitomycin C presents an EC50 of approximately 0 14 M Moreover it can potentiate apoptosis induced by TRAIL (TNF-related apoptosis-inducing ligand) through mechanisms independent of p53 modulating apoptosis-related protein expression and caspase activation Due to its cytotoxic mechanism mitomycin C continues to serve as a useful compound in cancer research particularly in apoptosis signaling studies
Apexbio Technology LLC Bexarotene 153559-49-0 10mM (in 1mL DMSO)
Bexarotene is a synthetic selective agonist for retinoid X receptors (RXRs) a subclass of nuclear hormone receptors involved in the regulation of gene transcription Upon binding to RXRs Bexarotene modulates the expression of target genes associated with cell differentiation proliferation and apoptosis Due to this mechanism Bexarotene is commonly employed in research investigating tumor growth inhibition cellular differentiation pathways and apoptosis induction Researchers also frequently utilize this retinoid derivative to elucidate RXR-mediated signaling pathways in oncology and to explore potential therapeutic applications for various malignancies
Apexbio Technology LLC XL-888 1149705-71-4 10mM (in 1mL DMSO)
XL-888 (CAS 1149705-71-4) is an orally bioavailable small molecule inhibitor targeting heat shock protein 90 (HSP90) It selectively inhibits HSP90 and HSP90 with IC50 values of 22 nM and 44 nM respectively while exhibiting markedly weaker inhibition against a panel of other kinases Structural analyses indicated XL-888 binds HSP90 via hydrogen bonding interactions involving the Asp93 residue In tumor cell assays XL-888 potently suppresses proliferation with IC50 values in the range of 0 1-45 5 nM XL-888 is used in oncology research particularly for studying resistance mechanisms to targeted therapies
Apexbio Technology LLC MK-5108 (VX-689) 1010085-13-8 10mM (in 1mL DMSO)
MK-5108 (VX-689 CAS 1010085-13-8) is a selective inhibitor targeting Aurora A kinase (AAK) functioning through competitive interaction with its ATP-binding pocket It exhibits sub-nanomolar inhibition of Aurora A kinase (IC50 0 064 nM) and displays additional inhibitory activity against Aurora B and Aurora C kinases (IC50 14 nM and IC50 12 nM respectively) MK-5108 has been extensively studied in cancer research contexts demonstrating antiproliferative activity across various tumor types including breast cervical colorectal ovarian and pancreatic cancers
Apexbio Technology LLC DMXAA (Vadimezan) 117570-53-3 10mM (in 1mL DMSO)
DMXAA (Vadimezan AS-1404) is a tumor vascular disrupting and apoptosis-inducing agent functioning primarily through inhibition of DT-diaphorase (DTD) It acts by suppressing DTD enzymatic activity showing an IC50 of approximately 62 5 M Additionally DMXAA inhibits various kinases notably VEGFR2 disrupting endothelial cells and blood vessel formation to induce tumor cell apoptosis and vascular necrosis Experimentally DMXAA demonstrates activity in murine tumor models including induction of apoptosis in endothelial cells and tumor vasculature promoting necrosis and tumor regression Therefore DMXAA is commonly used in oncology research focused on anti-angiogenesis and tumor vascular disruption mechanisms
Apexbio Technology LLC ABT-199 1257044-40-8 10mM (in 1mL DMSO)
ABT-199 (CAS 1257044-40-8) is a selective small-molecule inhibitor targeting BCL-2 developed through structure-guided drug design By specifically interfering with the mitochondrial apoptotic pathway regulated by BCL-2 ABT-199 induces apoptosis predominately in cells dependent on BCL-2 signaling rather than BCL-XL In preclinical assessments ABT-199 exhibited antitumor activity against hematologic malignancies including BCL-2-dependent non-Hodgkin lymphoma (NHL) and acute myeloid leukemia (AML) cell lines and xenograft models while demonstrating minimal platelet toxicity
Apexbio Technology LLC Simvastatin (Zocor) 79902-63-9 10mM (in 1mL DMSO)
Simvastatin (CAS 79902-63-9) marketed as Zocor is a synthetic lactone derived from fermented Aspergillus terreus metabolites Following oral administration the inactive lactone is hydrolyzed into an active -hydroxy acid metabolite which specifically inhibits HMG-CoA reductase the rate-limiting enzyme in cholesterol biosynthesis Simvastatin demonstrates antiproliferative effects in hepatocellular carcinoma cells (HepG2 Huh7) inducing apoptosis cell cycle arrest at G0/G1 reducing expression of cyclins (D1 E) and cyclin-dependent kinases (CDK1 2 4) while elevating CDK inhibitors p19 and p27 It is therefore utilized extensively for research in cancer biology cardiovascular pathology and lipid metabolism disorders
Apexbio Technology LLC Q-VD(OMe)-OPh 10mM (in 1mL DMSO)
Q-VD(OMe)-OPh is a pan-caspase inhibitor structurally identified as quinolyl-valyl-O-methylaspartyl-[2 6-difluorophenoxy]-methyl ketone As a broad-spectrum inhibitor Q-VD(OMe)-OPh reversibly targets multiple caspases involved in apoptotic signaling including initiator caspases (such as caspases 8 9 10 and 12) and executioner caspases (such as caspase 3) thereby blocking intrinsic extrinsic and endoplasmic reticulum-mediated apoptotic pathways In recombinant enzyme assays this inhibitor displays nanomolar-range IC values against caspases 1 3 8 and 9 Due to minimal cytotoxicity at tested concentrations Q-VD(OMe)-OPh serves as a tool compound in apoptosis-related biomedical research applied broadly for dissecting caspase-dependent apoptotic mechanisms and evaluating cytoprotective strategies
Apexbio Technology LLC Axitinib (AG 013736) 319460-85-0 10mM (in 1mL DMSO)
Axitinib (CAS 319460-85-0) also known as AG 013736 is an orally bioavailable selective inhibitor targeting vascular endothelial growth factor receptor (VEGFR) tyrosine kinases 1 2 and 3 It inhibits VEGFR phosphorylation with IC50 values of approximately 0 1 nM (VEGFR-1) 0 2 nM (VEGFR-2) and 0 1 0 3 nM (VEGFR-3) and demonstrates significantly higher selectivity relative to FGFR-1 Axitinib reduces phosphorylation of VEGF-mediated intracellular signaling proteins Akt eNOS and ERK1/2 and exhibits in vivo suppression of VEGFR-2 activation (EC50 0 49 nM) Its antiangiogenic action results in tumor growth delay in human xenograft models (e g HCT-116 SN12C) highlighting its utility in cancer research
Apexbio Technology LLC PTC-209 315704-66-6 10mM (in 1mL DMSO)
PTC-209 (CAS 315704-66-6) is a small-molecule inhibitor targeting BMI-1 identified through Gene Expression Modulation by Small molecules (GEMS) technology It acts by suppressing BMI-1 expression at the transcriptional level displaying an IC50 of approximately 0 5 M In HCT116 cells PTC-209 reduces both UTR-mediated and endogenous BMI-1 expression It selectively restricts cell proliferation in certain tumor and stem cell types including U937 HT1080 and human hematopoietic stem cells without affecting viability in cell lines such as HEK293 and HT1080 Thus PTC-209 is primarily utilized in studies exploring cancer stem cell growth and oncogenesis involving BMI-1 and the PRC1 complex
Apexbio Technology LLC HC-030031 349085-38-7 10mM (in 1mL DMSO)
HC-030031 (CAS 349085-38-7) is a selective antagonist targeting transient receptor potential ankyrin 1 (TRPA1) a member of the TRP ion channel family involved in chemical and mechanical sensory transduction In FLIPR calcium influx assays HC-030031 inhibited cinnamaldehyde- and allyl isothiocyanate (AITC)-induced TRPA1 activation with IC50 values of 4 9 M and 7 5 M respectively It showed negligible activity against TRPV1 TRPV3 and TRPV4 isoforms In rat models HC-030031 reduced AITC-induced nociceptive responses CFA-induced mechanical hypersensitivity and neuropathic sensitivity from spinal nerve ligation HC-030031 serves as a pharmacological tool to study TRPA1 functions particularly in pain research
Apexbio Technology LLC Ketoprofen 22071-15-4 10mM (in 1mL DMSO)
Ketoprofen (CAS 22071-15-4) is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase enzymes (COX) reducing prostaglandin synthesis and subsequent inflammation In biochemical assays using human recombinant enzymes ketoprofen demonstrates non-selective COX inhibition with reported IC50 values of approximately 0 5 M for COX-1 and 2 33 M for COX-2 Widely utilized in biomedical research ketoprofen serves as a pharmacological tool to investigate inflammatory signaling pathways and evaluate COX-dependent processes