Dimethyl Sulfoxide
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 PCI-24781 (CRA-024781) 783355-60-2 10mM (in 1mL DMSO)
PCI-24781 (CRA-024781 CAS 783355-60-2) is a histone deacetylase (HDAC) inhibitor targeting HDAC1 HDAC2 HDAC3 HDAC6 HDAC8 and HDAC10 with reported Ki values of 7 19 8 2 17 280 and 24 nM respectively HDAC enzymes catalyze the removal of acetyl groups from lysine residues on histone proteins thereby regulating chromatin structure and gene expression PCI-24781 induces dose-dependent hyperacetylation of histones and tubulin in human cancer cells (HCT116 DLD-1) leading to apoptosis via p21 upregulation PARP cleavage and H2AX accumulation PCI-24781 demonstrates antitumor activity against multiple tumor cell lines and in xenograft models highlighting its utility for oncology research
Apexbio Technology LLC LY2584702 1082949-67-4 10mM (in 1mL DMSO)
LY2584702 (CAS 1082949-67-4) is an orally bioavailable ATP-competitive inhibitor selectively targeting p70 S6 kinase (p70S6K) a serine/threonine kinase downstream of the PI3K/Akt/mTOR signaling cascade By inhibiting p70S6K activity LY2584702 effectively suppresses phosphorylation of ribosomal protein S6 (S6) thereby modulating protein translation LY2584702 exhibits potent inhibition of p70S6K (IC50 4 nM) and effectively reduces phosphorylated S6 levels in HCT116 colorectal cancer cells (IC50 between 0 1-0 24 M) Notably LY2584702 demonstrated anticancer activity in preclinical xenograft models supporting its role in targeted cancer research and therapeutic development
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 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 GDC-0994 1453848-26-4 10mM (in 1mL DMSO)
GDC-0994 (CAS 1453848-26-4) is a selective small-molecule inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2) components of the MAP kinase signaling cascade downstream of RAS/RAF/MEK ERK1/2 mediates cell proliferation and differentiation frequently activated due to oncogenic mutations in RAS and BRAF GDC-0994 shows inhibition of ERK1 and ERK2 with IC50 values of 1 1 and 0 3 nM respectively In preclinical models bearing KRAS or BRAF mutant tumor xenografts oral administration of GDC-0994 suppresses ERK phosphorylation and downstream signaling demonstrating significant anti-tumor activity GDC-0994 is a potent tool for studying ERK signaling in cancer research
Apexbio Technology LLC ML347 1062368-49-3 10mM (in 1mL DMSO)
ML347 (CAS 1062368-49-3) is a potent and selective inhibitor of bone morphogenetic protein (BMP) type I receptors specifically targeting ALK2 Mechanistically ML347 selectively inhibits ALK2 kinase activity with an IC50 of 32 nM while also inhibiting ALK1 with a comparable IC50 of 46 nM Notably ML347 displays approximately 300-fold selectivity for ALK2 over ALK3 and lacks inhibitory activity against closely related kinases such as ALK6 and KDR In the BMP4-induced C2C12BRA cell-based assay ML347 exhibits inhibitory activity with an IC50 of 152 nM As a selective ALK2 inhibitor ML347 serves as a valuable probe in BMP pathway research
Apexbio Technology LLC Z-Ligustilide 4431-01-0 10mM (in 1mL DMSO)
Ligustilide a bioactive compound purified from Angelica essential oil exhibits anti-inflammatory and anti-apoptotic properties and is commonly investigated for circulatory improvement and inflammation-related studies In vitro data demonstrate ligustilide s capability to interfere with apoptotic signaling pathways in neuronal cell models by modulating factors such as mitochondrial cytochrome C release Bcl-2/Bax ratios and Caspase-3 expression Additionally in animal models of ovariectomy-induced osteoporosis ligustilide administration reduces inflammatory markers including NF- B activation and production of cytokines (TNF- IL-1 ) and enzymes (COX-2 iNOS) suggesting potential therapeutic relevance in inflammation-associated conditions
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 PD 151746 179461-52-0 10mM (in 1mL DMSO)
PD 151746 is a cell-permeable inhibitor that selectively targets calpain a calcium-dependent cysteine protease involved in various cellular processes With a Ki value of 0 26 M against -calpain it prevents the proteolytic cleavage of substrates like neuronal nitric oxide synthase (nNOS) and calmodulin-dependent protein kinase II-alpha (CaMPK-II) particularly under stress In neuronal models PD 151746 inhibits apoptosis induced by serum/potassium withdrawal reduces MEF2 phosphorylation suppresses cdk5/p25 complex formation and decreases caspase-3 activation In HepG2 hepatoma cells it disrupts insulin-stimulated glycogen synthesis and affects protein tyrosine phosphatase-2 (PTP2) expression PD 151746 is used in research to study calpain-related signaling pathways apoptosis cell motility and metabolism
Apexbio Technology LLC GSK-923295 1088965-37-0 10mM (in 1mL DMSO)
GSK-923295 (CAS 1088965-37-0) is a highly potent inhibitor targeting the centromere-associated protein E (CENP-E) a kinesin motor protein essential for proper chromosome alignment and progression from metaphase to anaphase during cell division By blocking microtubule-stimulated ATPase activity of CENP-E GSK-923295 stabilizes an ATP-bound intermediate resulting in significantly reduced enzymatic function (IC50 3 2 nM) In cellular models GSK-923295 induces mitotic arrest with morphological changes similar to CENP-E knockdown In mouse xenograft models using Colo205 colon carcinoma cells administration of GSK-923295 leads to tumor growth inhibition and increased apoptosis supporting its utility in cancer research
Apexbio Technology LLC BV6 1001600-56-1 10mM (in 1mL DMSO)
BV6 (CAS 1001600-56-1) is a selective inhibitor targeting the inhibitor of apoptosis protein (IAP) family The IAP family includes proteins such as XIAP c-IAP1 and c-IAP2 that regulate programmed cell death pathways BV6 induces apoptosis and sensitizes cancer cells to chemotherapeutic agents and radiation by decreasing expression levels of IAPs including XIAP and c-IAP1 In vitro treatment with BV6 exhibited an IC50 of 7 2 M in H460 non-small cell lung carcinoma cells and enhanced their response to radiation BV6 is employed in research exploring cancer cell apoptosis modulation and therapeutic resistance
Apexbio Technology LLC Mupirocin 12650-69-0 10mM (in 1mL DMSO)
Mupirocin is an antibiotic targeting bacterial protein synthesis by inhibition of isoleucyl-tRNA synthetase Structurally analogous to isoleucine it binds the enzyme s active site blocking formation of isoleucyl-tRNA thus arresting bacterial protein production with reported MIC values around 0 05 g/ml for Staphylococcus aureus Primarily active against Gram-positive strains notably methicillin-resistant Staphylococcus aureus (MRSA) it is widely applied in biomedical research focused on antimicrobial resistance soft tissue infections biofilm studies and nasal colonization control strategies
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 Floxuridine 50-91-9 10mM (in 1mL DMSO)
Floxuridine is an antineoplastic antimetabolite compound functioning through inhibition of thymidylate synthase leading to interference with thymidine nucleotide biosynthesis This interruption induces DNA replication stress characterized by formation of double-strand DNA breaks Floxuridine exposure activates cellular DNA damage response pathways specifically ATR and ATM kinase signaling cascades and leads to the phosphorylation of checkpoint kinase 1 (Chk1) This compound has been widely utilized in oncology research to analyze DNA damage mechanisms cellular proliferation inhibition and apoptosis induction in human tumor cell lines Floxuridine demonstrates antiproliferative activity in cell-based assays with reported IC50 values typically ranging between 50 nM and 500 nM depending on cell line and experimental conditions