Dimethyl Sulfoxide
Apexbio Technology LLC Aurora A Inhibitor I 1158838-45-9 10mM (in 1mL DMSO)
Aurora A Inhibitor I (CAS 1158838-45-9) is a selective and potent small-molecule inhibitor of Aurora A kinase exhibiting an IC50 of 3 4 nM Aurora kinases are serine/threonine kinases crucially involved in mitotic progression with Aurora A specifically implicated in centrosome maturation and spindle assembly Aurora A Inhibitor I exerts high specificity significantly favoring Aurora A over Aurora B or cyclin-dependent kinases (CDKs) in vitro Subtle amino acid changes within kinase active sites significantly impact inhibitor potency highlighting residue-dependent selectivity This compound represents a valuable research tool for investigating Aurora A-related signaling pathways and their roles in cell division and oncogenesis
Apexbio Technology LLC AMG-900 945595-80-2 10mM (in 1mL DMSO)
AMG-900 (CAS 945595-80-2) is a small-molecule inhibitor targeting Aurora kinases a group of serine/threonine kinases crucial for mitosis regulation It exhibits potent ATP-competitive inhibitory activity against all three Aurora kinase isoforms resulting in suppression of Aurora-A and Aurora-B autophosphorylation events AMG-900 induces disruption of cellular mitotic processes leading to cell cycle arrest and subsequent apoptotic cell death Preclinically AMG-900 demonstrates activity across multiple tumor cell lines including multidrug-resistant and taxane-resistant variants and inhibits tumor growth in mouse xenograft models suggesting utility for cancer research
Apexbio Technology LLC CUDC-907 1339928-25-4 10mM (in 1mL DMSO)
CUDC-907 (CAS 1339928-25-4) is a dual inhibitor targeting histone deacetylases (HDACs 1 2 3 10) and class I phosphatidylinositol 3-kinases (PI3K) It exhibits nanomolar inhibitory activity against these enzymes blocking PI3K-mediated Akt signaling and increasing acetylation of histones and non-histone substrates (e g tubulin p53) In cancer cell models CUDC-907 induces G2-M phase arrest and reduces phosphorylation of downstream proteins such as p70S6 4EBP-1 MEK STAT3 and SRC Preclinical studies demonstrate its anti-tumor activity in lymphoma and NSCLC xenografts making it relevant for oncology research
Apexbio Technology LLC Quizartinib (AC220) 950769-58-1 10mM (in 1mL DMSO)
Quizartinib (AC220) is a second-generation small molecule inhibitor specifically targeting FMS-like tyrosine kinase 3 (FLT3) It exhibits potent inhibitory activity against FLT3 kinases harboring internal tandem duplication (ITD) and wild-type forms with reported IC50 values around 1 1 nM and 4 2 nM respectively Quizartinib demonstrates selectivity for FLT3 with minimal inhibition toward other kinases such as KIT PDGFR / RET and CSF-1R In cell-based assays using MV4-11 AML cell lines that express FLT3-ITD quizartinib reduces FLT3 phosphorylation thus inhibiting downstream signaling pathways involved in tumor cell proliferation and survival Quizartinib is utilized primarily in leukemia research to examine FLT3 signaling dependency and resistance mechanisms providing a useful tool for investigating molecular pathways and therapeutic strategies in acute myeloid leukemia (AML)
Apexbio Technology LLC Nitrendipine 39562-70-4 10mM (in 1mL DMSO)
Nitrendipine (CAS number 39562-70-4) is a dihydropyridine derivative acting as a calcium channel antagonist that selectively inhibits L-type calcium channels By blocking calcium ion influx into vascular smooth muscle cells nitrendipine induces vasodilation and reduces peripheral vascular resistance thereby lowering arterial blood pressure Due to its vascular-selective calcium antagonism it serves as a pharmacological tool in cardiovascular research particularly for studying mechanisms of hypertension and calcium-dependent signaling pathways
Apexbio Technology LLC 3-Deazaneplanocin A (DZNep) hydrochloride 120964-45-6 10mM (in 1mL DMSO)
3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor targeting histone methyltransferase EZH2 exhibiting inhibitory activity with an IC50 range of 0 08-0 24 M Additionally DZNep inhibits S-adenosylhomocysteine hydrolase (SAHH) at a Ki of 50 pM EZH2 acts as a catalytic subunit of polycomb repressive complex 2 (PRC2) participating in modulation of gene expression via histone methylation Research demonstrates that DZNep suppresses EZH2-dependent gene regulation pathways in cancer cells leading to altered expression of cell-cycle and apoptosis-associated genes DZNep is commonly utilized in epigenetic studies of various tumors and metabolic dysfunction models including AML liver fibrosis and lipid accumulation studies
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
Apexbio Technology LLC Embelin 550-24-3 10mM (in 1mL DMSO)
Embelin (CAS 550-24-3) is a natural benzoquinone derivative isolated from plants of the genus Embelia functioning as an inhibitor of X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4 1 M XIAP negatively regulates apoptosis by inhibiting caspase activation Embelin promotes apoptosis by interrupting XIAP-caspase interaction activating apoptotic pathways in tumor cells expressing elevated XIAP levels Additionally embelin can inhibit the NF- B signaling cascade through suppression of IKK activation thereby downregulating NF- B-mediated anti-apoptotic and metastatic gene expression In animal models embelin demonstrates anti-tumor properties by attenuating tumorigenesis related to inflammation-driven colorectal cancer through modulation of IL-6/STAT3 pathway signaling
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 AG-1478 153436-53-4 10mM (in 1mL DMSO)
AG-1478 is a selective inhibitor of epidermal growth factor receptor (EGFR) a receptor tyrosine kinase involved in cellular proliferation and survival It inhibits EGFR-mediated Erk1/2 phosphorylation induced by EGF stimulation with an IC50 of approximately 10 M in Ishikawa ovarian cell lines In experimental cancer research AG-1478 has been applied to study EGFR signaling mechanisms by reducing receptor phosphorylation and downstream pathway activation Studies using diverse cancer cell lines including ovarian (CAOV-3 SKOV-3) colorectal (SW480) hepatocellular (HA22T/VGH) and lung (A549) carcinomas employ AG-1478 to investigate EGFR s role in tumor growth and chemoresistance Additionally AG-1478 is utilized in preclinical xenograft models to assess tumor growth modulation via EGFR inhibition
Apexbio Technology LLC Pralatrexate 146464-95-1 10mM (in 1mL DMSO)
Pralatrexate (CAS 146464-95-1) is a small molecule inhibitor targeting dihydrofolate reductase (DHFR) with a Ki value of 45 nM DHFR mediates the reduction of dihydrofolate to tetrahydrofolate a critical cofactor in purine thymidylate and amino acid biosynthesis Pralatrexate exhibits high affinity for folylpolyglutamate synthetase (FPGS) and reduced folate carrier-1 (RFC-1) facilitating intracellular accumulation It demonstrates notable antiproliferative activity against various human cancer cell lines in vitro and reduces tumor growth in NSCLC xenograft models indicating its suitability for oncology research
Apexbio Technology LLC INCB28060 1029712-80-8 10mM (in 1mL DMSO)
INCB28060 (CAS 1029712-80-8) also known as Capmatinib or INC280 is an ATP-competitive inhibitor of the receptor tyrosine kinase c-Met (HGFR) This receptor plays essential roles in cellular processes including embryogenesis healing proliferation invasion and angiogenesis and is frequently overexpressed or mutated in cancers INCB28060 blocks c-Met phosphorylation and downstream signaling exhibiting an IC50 of 0 13 nM In preclinical studies it suppresses proliferation in cancer cell lines (e g SNU-5 S114) and inhibits migration in U-87MG and H441 cells In mouse tumor models oral administration reduces c-Met activation and tumor progression INCB28060 serves as a tool compound for investigating c-Met function in cancer research
Apexbio Technology LLC Laquinimod (ABR-215062) 248281-84-7 10mM (in 1mL DMSO)
Laquinimod (ABR-215062 CAS 248281-84-7) is an orally bioavailable immunomodulatory small molecule Research studies demonstrate that in experimental autoimmune encephalomyelitis (EAE) a widely utilized rodent model for studying human multiple sclerosis (MS) laquinimod treatment suppresses disease progression in a dose-dependent manner Mechanistically the compound reduces inflammatory infiltration of CD4 T lymphocytes and macrophages into the central nervous system thereby modulating the Th1/Th2 immune response and inducing regulatory cytokines such as TGF- Clinical investigations into relapsing MS indicate that laquinimod administration correlates with reduced disease activity clinical relapse rate MRI-measured lesions and brain volume loss
Apexbio Technology LLC KU 55933 587871-26-9 10mM (in 1mL DMSO)
KU 55933 (CAS 587871-26-9) is a selective inhibitor of ATM kinase with an IC50 of 13 nM ATM kinase promotes insulin-induced Akt activation via phosphorylation of Akt at Ser473 KU 55933 inhibition of ATM significantly reduces Akt Ser473 phosphorylation in insulin- or IGF-I-treated MDA-MB-453 and PC-3 cells resulting in suppressed proliferation cell cycle arrest at G1 phase and decreased cyclin D1 levels KU 55933 serves as a tool for studying ATM-related signaling and Akt-driven cancer cell growth regulation
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