Dimethyl Sulfoxide
Apexbio Technology LLC Linifanib (ABT-869) 796967-16-3 10mM (in 1mL DMSO)
Linifanib (ABT-869 CAS 796967-16-3) is an ATP-competitive inhibitor of receptor tyrosine kinases targeting platelet-derived growth factor (PDGF) and vascular endothelial growth factor receptors (VEGFRs) as well as FMS-like tyrosine kinase 3 (FLT3) including its activating internal tandem duplication (ITD) mutations Linifanib selectively reduces cell growth in FLT3 ITD-expressing cell lines such as Ba/F3 FLT3 ITD cells inhibits phosphorylation of FLT3 and Akt and induces apoptosis preferentially in ITD mutant cells In vivo experiments with ITD-expressing leukemia xenografts show reduced leukemia progression and prolonged survival in mice treated orally with linifanib This compound is widely used in preclinical research for acute myeloid leukemia studies
Apexbio Technology LLC Epoxomicin 134381-21-8 10mM (in 1mL DMSO)
Epoxomicin (CAS 134381-21-8) is a naturally occurring proteasome inhibitor initially isolated from actinomycete cultures It acts primarily by forming covalent bonds through its -epoxyketone moiety with catalytic residues of the proteasome resulting in potent inhibition of the chymotrypsin-like (CTRL) activity of the 20S proteasome subunit Epoxomicin also inhibits proteasomal trypsin-like and peptidyl-glutamyl peptide hydrolysis activities albeit at significantly lower rates It exhibits anti-inflammatory and antitumor activities and is employed experimentally to study ubiquitin-proteasome-mediated cellular pathways bone formation regulation and Parkinson s disease model generation
Apexbio Technology LLC Calpain Inhibitor II, ALLM 136632-32-1 10mM (in 1mL DMSO)
Calpain inhibitor II (also termed ALLM or CPI-2) is a membrane-permeable inhibitor targeting calpain I calpain II as well as cathepsin L and B Calpain inhibition by this compound can activate apoptosis via caspase-mediated pathways Studies conducted in acute lymphoblastic leukemia (ALL) cell lines (such as ALL-1 RS4 11 JURKAT) and non-Hodgkin s lymphoma (NHL) cells (including RAMOS DAUDI) revealed apoptosis induction at concentrations of 50 100 M Additionally apoptosis triggered by calpain inhibitor II appears independent of tyrosine kinases BTK and LYN Unlike calpain inhibitor I calpain inhibitor II does not influence NF- B signaling nor sensitize tumor cells to TRAIL-induced apoptosis This inhibitor is widely employed in apoptosis-related research and studies exploring calpain-associated cellular pathways
Apexbio Technology LLC AVL-292 1202757-89-8 10mM (in 1mL DMSO)
AVL-292 (CAS 1202757-89-8) also known as CC-292 is an orally bioavailable irreversible small-molecule inhibitor targeting Bruton s tyrosine kinase (BTK) a member of the Tec kinase family crucial for B-cell receptor (BCR) signaling pathways AVL-292 covalently binds the cysteine residue (Cys481) within BTK suppressing its autophosphorylation and downstream signaling Reported IC50 and EC50 values in biochemical and cellular assays are 0 5 nM and 8 nM respectively AVL-292 has shown efficacy in preclinical models such as collagen-induced arthritis (CIA) mice and demonstrates therapeutic potential in clinical studies involving B-cell malignancies including CLL B-NHL and WM
Apexbio Technology LLC Topotecan HCl 119413-54-6 10mM (in 1mL DMSO)
Topotecan HCl (CAS 119413-54-6) also known as SKF104864 is a semisynthetic derivative of camptothecin functioning as a selective inhibitor of topoisomerase I It stabilizes the topoisomerase I-DNA cleavage complex causing DNA damage and subsequent cell death Preclinical studies in murine tumor models demonstrate notable antitumor activity particularly against intravenous P388 leukemia and Lewis lung carcinoma when administered intravenously or in subcutaneous xenografts Additionally it exhibits efficacy against solid tumors including drug-resistant cancers and HT-29 human colon carcinoma xenografts Toxicological evaluations indicate reversible and concentration-dependent toxic effects primarily impacting rapidly proliferating tissues such as bone marrow and gastrointestinal epithelium
Apexbio Technology LLC Y-27632 146986-50-7 10mM (in 1mL DMSO)
Y-27632 (CAS 146986-50-7) is a selective inhibitor of Rho-associated protein kinases (ROCK) specifically targeting ROCK1 and ROCK2 isoforms It competitively binds to the ATP-binding site inhibiting ROCK1 and ROCK2 with Ki values of 0 22 M and 0 30 M respectively Compared to other kinases such as citron kinase PKN and PKC Y-27632 exhibits significantly higher selectivity toward ROCK isoforms In cellular assays Y-27632 at 10 M concentration effectively disrupts stress fiber formation in Swiss 3T3 fibroblast cells It is widely used in cell biology research to study ROCK signaling pathways and cytoskeletal dynamics
Apexbio Technology LLC Purmorphamine 483367-10-8 10mM (in 1mL DMSO)
Purmorphamine (CAS 483367-10-8) is a synthetic small molecule agonist targeting the Smoothened (Smo) protein a critical component of the Hedgehog (Hh) signaling pathway By binding and activating Smo Purmorphamine induces downstream modulation of key pathway targets such as Gli1 and Patched In vitro studies demonstrated activation with an IC50 value of approximately 1 5 M during competitive assays with the antagonist cyclopamine and an EC50 of about 1 M for alkaline phosphatase (ALP) expression in C3H10T1/2 multipotent cells This agent has been applied in research contexts for inducing osteogenic differentiation with implications for studying bone regeneration and neural degeneration processes
Apexbio Technology LLC GSK3787 188591-46-0 10mM (in 1mL DMSO)
GSK3787 is an irreversible antagonist targeting peroxisome proliferator-activated receptor beta/delta (PPAR- / ) Structurally it acts through covalent modification by binding specific cysteine residues within the ligand-binding domain of PPAR- / thereby disrupting receptor activation and subsequent co-regulator interactions Due to receptor selectivity GSK3787 preferentially inhibits PPAR- / relative to PPAR- Experimental evidence in rodent models demonstrates that oral administration of GSK3787 counteracts agonist-induced gene expression such as Angptl4 and Adrp by reducing recruitment of activated PPAR- / to target gene promoters indicating potential utility in studying PPAR- / -mediated regulatory pathways related to lipid metabolism and gene transcription in vitro and in vivo
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 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
Apexbio Technology LLC GSK2636771 1372540-25-4 10mM (in 1mL DMSO)
GSK2636771 (CAS 1372540-25-4) is a selective inhibitor targeting the p110 isoform of class I phosphoinositide 3-kinase (PI3K) PI3Ks comprise catalytic subunits p110 and which mediate signaling cascades critical for cellular proliferation and survival Specifically GSK2636771 reduces AKT phosphorylation in breast cancer cell lines leading to diminished cellular viability In PTEN-deficient endometrioid endometrial cancer (EEC) cell lines combination with the p110 inhibitor A66 enhances inhibition of cell growth This compound serves as a research tool for investigating PI3K signaling and potential cancer therapeutic strategies
Apexbio Technology LLC TWS119 601514-19-6 10mM (in 1mL DMSO)
TWS119 (CAS 601514-19-6) is a selective inhibitor of glycogen synthase kinase-3 (GSK-3 ) exhibiting an IC50 of approximately 30 nM Originally identified from a library of pyrrolopyrimidine-based compounds TWS119 binds GSK-3 with a Kd value around 126 nM By inhibiting GSK-3 activity TWS119 modulates downstream transcriptional events promoting neuronal differentiation in murine embryonic carcinoma (P19) and mouse embryonic stem cells through mechanisms distinct from classical Wnt signaling Due to this property TWS119 serves as a useful tool for research in neural differentiation and regenerative medicine
Apexbio Technology LLC Bupivacaine HCl 18010-40-7 10mM (in 1mL DMSO)
Bupivacaine Hydrochloride (CAS 18010-40-7) is an amino amide-type local anesthetic compound that functions primarily through blockade of voltage-gated sodium channels By preventing sodium ion influx in neuronal membranes it reduces action potential propagation resulting in reversible inhibition of nerve conduction Due to its relatively rapid onset paired with prolonged anesthetic duration bupivacaine hydrochloride is frequently utilized experimentally to investigate neuronal signaling pain mechanisms and local anesthetic pharmacology in biomedical research
Cayman Chemical L-MethIonIn SulfoxIde 1g
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