Dimethyl Sulfoxide
Apexbio Technology LLC SB 431542 301836-41-9 10mM (in 1mL DMSO)
SB 431542 (CAS number 301836-41-9) is a selective ATP-competitive inhibitor targeting activin receptor-like kinase 5 (ALK5) a type I receptor within the transforming growth factor- (TGF- ) signaling pathway It inhibits ALK5 activity with an IC50 value of 94 nM thereby preventing phosphorylation of Smad2 proteins and their subsequent nuclear accumulation Additionally SB 431542 inhibits closely related receptors ALK4 and ALK7 while showing minimal or no significant activity against ALK1 ALK2 ALK3 and ALK6 at relevant concentrations Commonly utilized in cellular assays to investigate TGF- signaling this compound is valuable for studying associated cellular processes and diseases
Apexbio Technology LLC Epinephrine HCl 55-31-2 10mM (in 1mL DMSO)
Epinephrine hydrochloride is an adrenergic receptor agonist functioning as both a hormone and neurotransmitter Structurally epinephrine hydrochloride is the hydrochloride salt form of epinephrine facilitating receptor binding and signal transduction mediated by adrenergic receptor subtypes ( and ) Upon receptor activation it initiates downstream signaling pathways through G-protein-coupled mechanisms influencing intracellular second messengers such as cAMP calcium influx and protein kinase activity In biomedical research epinephrine hydrochloride serves as a pharmacological tool for investigating adrenergic receptor-mediated physiological responses including cardiac function modulation bronchodilation metabolic processes and vasoconstriction Its controlled application aids in studying sympathetic nervous system mechanisms cellular signaling cascades cardiovascular pharmacology and stress response frameworks
Apexbio Technology LLC Lomustine 13010-47-4 10mM (in 1mL DMSO)
Lomustine (CAS 13010-47-4) is an anticancer small molecule belonging to the nitrosourea class of alkylating agents It exerts its antitumor effects primarily by forming DNA cross-links leading to impaired replication and selective cytotoxicity in rapidly dividing tumor cells Lomustine shows inhibitory activity against various cancer cell lines including breast cancer (ZR-75-1 IC50 25 M) astrocytoma (U87MG IC50 8 8 M) and colon carcinoma (LS174T IC50 13 M) Due to its lipophilic nature lomustine efficiently crosses the blood-brain barrier facilitating its use in research involving central nervous system malignancies and related leukemia models
Apexbio Technology LLC Famprofazone 10mM (in 1mL DMSO)
A8431 is a small molecule that functions as a selective inhibitor of autophagy a conserved cellular pathway responsible for the lysosome-mediated degradation of intracellular components Acting primarily through interference with autophagosome formation or lysosomal fusion A8431 disrupts autophagic flux and thus influences cellular homeostasis and survival pathways It is widely utilized in biomedical research to dissect autophagy-mediated cellular mechanisms and has relevance in studies of cancer biology neurodegeneration and metabolic disorders where autophagy regulation is implicated
Apexbio Technology LLC ICG 001 847591-62-2 10mM (in 1mL DMSO)
ICG 001 is a small molecule inhibitor of the canonical Wnt/ -catenin signaling pathway Mechanistically it competes with -catenin for interaction with CREB-binding protein (CBP) thereby selectively disrupting CBP/ -catenin-mediated transcriptional activity driven by the TCF/ -catenin complex (IC50 3 M) Experimental studies demonstrated its use in assessing CBP-dependent biological functions regulated by Wnt signaling Research applications include investigating CBP/ -catenin roles in cancer cell proliferation such as colorectal cancer cells (HCT-116 SW480) glioblastoma stem cell growth and fibrotic responses in pulmonary and dermal experimental models Additionally ICG 001 is under evaluation in clinical studies aiming at treatment of colorectal cancer and leukemia
Apexbio Technology LLC Rucaparib (free base) 283173-50-2 10mM (in 1mL DMSO)
Rucaparib (free base) (CAS 283173-50-2) also known as AG014699 or PF-01367338 is a pharmacological inhibitor targeting poly(ADP-ribose) polymerase (PARP) a nuclear enzyme centrally involved in DNA damage signaling and base excision repair pathways By impeding PARP activity Rucaparib compromises DNA repair capacity leading to persistent DNA strand breaks as evidenced by increased gamma-H2AX and p53BP1 foci It has demonstrated radiosensitizing properties in prostate cancer cells notably those harboring PTEN deficiency or expressing ETS gene fusion proteins due partly to inhibition of non-homologous end-joining (NHEJ) DNA repair Rucaparib serves as a tool compound in oncology research to study chemosensitization and radiosensitization strategies
Apexbio Technology LLC Omecamtiv mecarbil 873697-71-3 10mM (in 1mL DMSO)
Omecamtiv mecarbil is a cardiac-specific myosin activator targeting the S1 domain of cardiac myosin It acts by accelerating the release of phosphate (Pi) from the cardiac myosin S1 domain upon actin binding thus facilitating transition from weak to strong actin-bound conformations This mechanistic action enhances cardiomyocyte contractility independent of calcium transient alterations In preclinical studies omecamtiv mecarbil enhances contraction force in isolated cardiomyocytes at submicromolar concentrations and improves cardiac function in animal models of systolic dysfunction without influencing myocardial oxygen consumption Researchers utilize omecamtiv mecarbil to investigate therapeutic approaches in treating systolic heart failure
Apexbio Technology LLC TG100-115 677297-51-7 10mM (in 1mL DMSO)
TG100-115 (CAS 677297-51-7) is a selective inhibitor targeting phosphoinositide 3-kinase isoforms PI3K and PI3K with IC50 values of 83 nM and 235 nM respectively exhibiting negligible inhibition towards PI3K and PI3K Research in murine models demonstrates that treatment with TG100-115 significantly reduces eosinophil accumulation bronchoalveolar IL-13 cytokine levels mucus deposition and leukocyte infiltration associated with allergic asthma decreasing airway hyperresponsiveness by approximately 50% Moreover this compound attenuates neutrophil infiltration and TNF induction following exposure to cigarette smoke and LPS suggesting its utility as an investigational tool for asthma and inflammatory pulmonary diseases
Apexbio Technology LLC Fludarabine(Synonyms: Fludarabine Phosphate, Fludara, Fludarabinum, 2-Fluoro-ara-AMP, 9H-Purin-6-amine), 10mM (in 1mL DMSO), CAS: 21679-14-1.
Fludarabine (CAS 21679-14-1) is a purine analog prodrug that inhibits DNA synthesis Upon cellular uptake it undergoes phosphorylation to its active triphosphate form (F-ara-ATP) disrupting DNA replication through inhibition of critical enzymes such as DNA primase DNA ligase I ribonucleotide reductase and DNA polymerases and In human myeloma RPMI8226 cell assays fludarabine suppressed cell growth reduced Akt phosphorylation and lowered anti-apoptotic proteins XIAP and Survivin In vivo studies demonstrated marked tumor growth inhibition in RPMI8226 xenograft models Fludarabine serves as a tool in oncology research particularly leukemia and multiple myeloma-related studies
Apexbio Technology LLC Nutlin-3a chiral 675576-98-4 10mM (in 1mL DMSO)
Nutlin-3a chiral (CAS 675576-98-4) is a small-molecule antagonist targeting mouse double minute 2 (MDM2) which functions as a negative regulator of the tumor suppressor TP53 By binding directly to the TP53-interacting pocket of MDM2 Nutlin-3a blocks the degradation of TP53 stabilizing the protein and activating TP53-dependent pathways Studies in solid tumors and lymphomas indicate that Nutlin-3a induces cell cycle arrest growth inhibition and apoptosis Research has demonstrated antitumor activity in vitro and in vivo highlighting its utility in studying TP53-related cell signaling pathways and its potential in cancer research applications
Apexbio Technology LLC Roscovitine (Seliciclib,CYC202) 186692-46-6 10mM (in 1mL DMSO)
Roscovitine (Seliciclib CYC202 CAS number 186692-46-6) is a selective inhibitor of cyclin-dependent kinases (CDKs) It targets cdc2 (CDK1/cyclin B) CDK2 (CDK2/cyclin A and CDK2/cyclin E) and CDK5 (CDK5/p35) with reported IC50 values of 0 65 M 0 7 M 0 7 M and 0 16 M respectively Additionally roscovitine inhibits extracellular signal-regulated kinases Erk1 and Erk2 displaying IC50 values of 34 M and 14 M respectively In cellular studies roscovitine has been shown to delay or halt transitions during early mitosis specifically preventing cell progression from prophase to metaphase as observed in Xenopus oocyte maturation induced by progesterone Due to its distinct inhibitory profile roscovitine is commonly utilized in research examining cell cycle regulation and kinase signaling pathways relevant to oncology
Apexbio Technology LLC Cinobufagin 470-37-1 10mM (in 1mL DMSO)
Cinobufagin (CAS 470-37-1) is a steroidal cardiac glycoside recognized for its inhibitory effect on the Na /K -ATPase pump Its inhibitory potency is approximately comparable to that of ouabain By impeding Na /K -ATPase activity cinobufagin disrupts ionic gradients altering intracellular calcium homeostasis and influencing cardiac and cellular functions In biomedical research cinobufagin serves as a valuable pharmacological tool to investigate ion transport mechanisms and explore related signaling pathways implicated in cellular physiology and pathology
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 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 Zebularine 3690-10-6 10mM (in 1mL DMSO)
Zebularine (CAS number 3690-10-6) is a chemically stable cytidine analog containing a 2-(1H)-pyrimidinone ring structure It acts primarily through inhibition of DNA methylation by forming covalent complexes with DNA methyltransferases Zebularine treatment leads to demethylation and reactivation of hypermethylation-mediated silenced genes exemplified by the p16 gene Additionally induced myogenic differentiation has been observed upon zebularine administration in 10T1/2 cells Zebularine displays minimal cytotoxicity in certain cell models such as T24 cells and retains stability in aqueous solutions across a broad pH range (up to pH 12) These properties make zebularine relevant for studies in epigenetic regulation and cellular differentiation