Dimethyl Sulfoxide
Apexbio Technology LLC Moclobemide (Ro 111163) 71320-77-9 10mM (in 1mL DMSO)
Moclobemide (Ro 111163 CAS 71320-77-9) is a reversible inhibitor of monoamine oxidase A (MAO-A) with a reported IC50 of approximately 10 M In vitro studies using rat brain homogenate indicate that it selectively targets MAO-A over MAO-B though with moderate potency Animal experiments demonstrate up to 80% inhibition of MAO-A activity in brain and liver tissues upon administration Prolonged high-dose exposure to Moclobemide alters adrenergic receptor profiles by downregulating -adrenergic receptors and enhancing affinity of 1-adrenergic agonist binding Due to its MAO-A specificity this compound serves as a prototype reversible inhibitor (RIMA) with relevance in antidepressant drug research
Apexbio Technology LLC EPZ004777 1338466-77-5 10mM (in 1mL DMSO)
EPZ004777 (CAS 1338466-77-5) is a selective small-molecule inhibitor targeting DOT1L a histone H3K79 methyltransferase involved in leukemogenesis It inhibits DOT1L enzymatic activity with an IC50 of approximately 400 pM in radiometric assays EPZ004777 selectively reduces viability in leukemia cell lines harboring MLL rearrangements such as MV4-11 (MLL-AF4) and MOLM13 (MLL-AF9) Additionally treatment with EPZ004777 attenuates Hoxa9 and Meis1 mRNA expression and exhibits inhibitory activity (IC50 range 0 1 1 M) against cells transformed by MLL-AF10 and CALM-AF10 oncogenes Overall EPZ004777 serves as a valuable tool for studying DOT1L-mediated epigenetic regulation and leukemic pathogenesis
Apexbio Technology LLC BYL-719 1217486-61-7 10mM (in 1mL DMSO)
BYL-719 (CAS 1217486-61-7) is a selective inhibitor of PI3K demonstrating minimal activity against PI3K or isoforms Through targeting PI3K an essential node frequently dysregulated via PIK3CA mutations in various cancers BYL-719 effectively disrupts downstream proliferative signaling In biochemical assays BYL-719 shows potent inhibition of PI3K with an IC50 of 5 nM Preclinical evaluations indicate dose-dependent antitumor efficacy in xenograft tumor models and proliferation arrest and apoptosis induction in multiple myeloma cell lines exhibiting PIK3CA overexpression Clinically initial studies reveal manageable safety profiles and preliminary antitumor responses notably in PIK3CA-mutant malignancies supporting continued exploration in oncology research settings
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 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 Carvedilol 72956-09-3 10mM (in 1mL DMSO)
Carvedilol is an antagonist targeting 1- and -adrenergic receptors employed in research on cardiovascular diseases especially congestive heart failure and hypertension Mechanistically carvedilol blocks adrenergic receptor-mediated signaling influencing sympathetic nervous system activity Additionally carvedilol exhibits antioxidative properties in vitro studies demonstrate suppression of Fe2 -induced lipid peroxidation (IC50 8 1 M) protection of -tocopherol depletion due to Fe2 exposure (IC50 17 6 M) and reduction of hydroxyl radical-derived DMPO-OH signals (IC50 25 M) It also inhibits proliferation (IC50 0 3-2 0 M) and migration (IC50 3 M) in vascular smooth muscle cells induced by platelet-derived growth factor supporting investigation of vascular remodeling processes
Apexbio Technology LLC Prucalopride 179474-81-8 10mM (in 1mL DMSO)
Prucalopride (CAS 179474-81-8) is a selective serotonin 5-HT4 receptor agonist with high affinity for both 5-HT4A and 5-HT4B receptor subtypes demonstrating Ki values of 2 5 nM and 8 nM respectively It displays substantial selectivity exceeding 290-fold against other serotonin receptor classes By activating 5-HT4 receptors prucalopride promotes gastrointestinal motility making it a valuable tool compound for investigating serotonergic mechanisms underlying gastrointestinal disorders and motility regulation Currently prucalopride is evaluated in Phase 3 clinical trials
Apexbio Technology LLC K02288 1431985-92-0 10mM (in 1mL DMSO)
K02288 (CAS 1431985-92-0) is a highly selective small molecule inhibitor targeting activin receptor-like kinase 2 (ALK2) a type I receptor involved in BMP signaling Structurally classified as a 2-aminopyridine derivative K02288 demonstrates strong potency against ALK2 (IC50 1 1 nM) It exhibits selectivity across the ALK receptor family showing lower activity on ALK3 ALK6 and minimal inhibition against ALK4-5 In cell-based assays using C2C12 cells treated with BMP ligands K02288 dose-dependently reduces Smad phosphorylation It has utility in research elucidating ALK2-mediated signaling pathways and developmental processes exemplified by inducing dorsalized phenotypes in zebrafish embryos
Apexbio Technology LLC Propylthiouracil 51-52-5 10mM (in 1mL DMSO)
Propylthiouracil is a thioureylene derivative characterized by inhibitory effects on thyroid hormone synthesis through targeting thyroid peroxidase (TPO) and type 1 iodothyronine deiodinase (DIO1) Its mechanistic actions involve suppression of TPO activity disrupting iodine oxidation and subsequent thyroid hormone formation as well as inhibition of peripheral thyroid hormone conversion via decreased DIO1 enzymatic activity In biomedical research Propylthiouracil is commonly utilized to investigate molecular pathways underlying hyperthyroid conditions such as Graves disease as well as to experimentally explore metabolic regulation of thyroid hormones
Apexbio Technology LLC CX-4945 (Silmitasertib) 1009820-21-6 10mM (in 1mL DMSO)
CX-4945 (Silmitasertib CAS 1009820-21-6) is an orally bioavailable inhibitor targeting casein kinase 2 (CK2) via ATP-competitive binding with an IC50 of approximately 1 nM It suppresses CK2-mediated signaling pathways notably by reducing phosphorylation of Akt at Ser129 independently of PTEN activation thus impacting PI3K/Akt pathway regulation In vitro studies report that CX-4945 treatment leads to increased total expression and decreased phosphorylation of cell cycle regulators p21 and p27 causing cell cycle arrest (G2/M in BT-474 breast carcinoma G1 in BxPC-3 pancreatic carcinoma) In vivo it displays antitumor activity in BxPC-3 mouse xenograft models highlighting its utility for oncology research
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 Levonorgestrel 797-63-7 10mM (in 1mL DMSO)
Levonorgestrel is a synthetic progesterone analog structurally categorized as a progestin exhibiting agonistic activity primarily through progesterone receptor (PR) binding and also showing interaction with estrogen receptors (ER) Upon receptor binding levonorgestrel modulates transcriptional activity influencing downstream gene expression related to reproductive processes This molecular interaction reduces luteinizing hormone levels inhibits ovulation and induces alterations in uterine lining and cervical mucus thus contributing to contraceptive activity Biomedically levonorgestrel is widely utilized in research for studying progesterone receptor signaling pathways hormonal regulation mechanisms and contraceptive drug development
Apexbio Technology LLC Penciclovir 39809-25-1 10mM (in 1mL DMSO)
Penciclovir is a selective inhibitor of herpes simplex virus 1 (HSV-1) DNA synthesis Structurally derived from guanine penciclovir undergoes phosphorylation within virus-infected cells forming penciclovir triphosphate the active antiviral metabolite Penciclovir triphosphate specifically targets viral DNA polymerase blocking HSV-1 DNA replication In vitro experiments using MRC-5 cells demonstrate inhibition of HSV-1 replication at an IC50 of 0 16 M without interfering with host cellular DNA synthesis This mechanism of action renders penciclovir suitable for antiviral research targeting HSV-1 replication as well as drug-resistance and mechanism-of-action studies involving HSV-2 and varicella-zoster virus (VZV)
Apexbio Technology LLC Amantadine HCl 665-66-7 10mM (in 1mL DMSO)
Amantadine Hydrochloride a dopamine receptor agonist is primarily employed as a research tool in neuroscience and antiviral studies It exerts its antiparkinsonian effects by promoting dopamine release and inhibiting dopamine reuptake consequently enhancing dopaminergic neurotransmission As an antiviral agent amantadine hydrochloride inhibits influenza A virus replication through blockade of the viral matrix protein M2 ion channel In cell-based assays amantadine hydrochloride demonstrates inhibitory activity against influenza A viruses with reported IC50 values typically ranging between 0 3 to 1 5 M depending on assay conditions and viral strains Researchers commonly utilize this compound to investigate neurological pathways associated with Parkinson s disease viral infection mechanisms and drug resistance phenomena
Apexbio Technology LLC PF-477736 952021-60-2 10mM (in 1mL DMSO)
PF-477736 is an ATP-competitive small-molecule inhibitor of checkpoint kinase 1 (Chk1) It selectively inhibits Chk1 kinase activity demonstrating nanomolar inhibitory potency in kinase assays and exhibits lower affinity toward related kinases such as CDK1 and Chk2 In vitro studies utilizing human cancer cell lines show PF-477736 disrupts Chk1-dependent G2-phase cell-cycle arrest induced by DNA-damaging agents preferentially targeting tumor cells with compromised p53 function while minimizing cytotoxicity to normal cells PF-477736 is widely utilized experimentally to study DNA damage response mechanisms potential chemosensitizing effects and therapeutic implications for cancers harboring p53 mutations