Dimethyl Sulfoxide
Apexbio Technology LLC GM 6001 142880-36-2 10mM (in 1mL DMSO)
GM 6001 (Ilomastat Galardin CAS 142880-36-2) is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) including MMP-1 -2 -3 -8 and -9 with reported Ki values of 0 4 nM 0 5 nM 27 nM 0 1 nM and 0 2 nM respectively MMPs participate in extracellular matrix remodeling and mediate signaling events induced by GPCR agonists through EGFR transactivation GM 6001 suppresses EGFR phosphorylation ERK activation and subsequent DNA synthesis induced by stimuli such as bombesin and lysophosphatidic acid (LPA) Additionally this compound has potential applications in cartilage research facilitating meniscal repair under inflammatory conditions by dampening IL-1-mediated MMP activity
Apexbio Technology LLC CGP 57380 522629-08-9 10mM (in 1mL DMSO)
CGP 57380 (CAS 522629-08-9) is a specific and selective inhibitor targeting the serine/threonine kinase MNK1 an enzyme implicated in translation regulation via phosphorylation of the eukaryotic initiation factor 4E (eIF4E) It inhibits MNK1 activity in vitro with an IC50 of approximately 2 2 M CGP 57380 suppresses stimulus-induced phosphorylation of eIF4E in various cellular contexts including 293 cells vascular smooth muscle cells and macrophages reducing translation of mRNAs encoding proinflammatory mediators such as TNF- IL-6 and monocyte chemoattractant protein-1 (MCP-1) Hence CGP 57380 is valuable for investigating MNK1-mediated translational control in inflammation and cell signaling
Apexbio Technology LLC Irinotecan(Synonyms: CPT-11, Campto, Camptosar, irinotecan hydrochloride, Irinotecan HCl, irinotecan hydrochloride trihydrate), 10mM (in 1mL DMSO), CAS: 97682-44-5.
Irinotecan (CAS 97682-44-5) also known as CPT-11 is an anticancer prodrug that acts as an inhibitor of topoisomerase I Upon enzymatic activation by carboxylesterase (CCE) to its potent metabolite SN-38 it stabilizes the DNA-topoisomerase I cleavable complex causing DNA damage and apoptosis In vitro studies show Irinotecan inhibits various colorectal cancer cell lines including LoVo (IC50 15 8 M) and HT-29 (IC50 5 17 M) Additionally xenograft models such as COLO 320 demonstrate pronounced tumor growth suppression Irinotecan is widely utilized in research to investigate DNA damage mechanisms and therapeutic efficacy in colorectal cancer
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
Sigma Aldrich Fine Chemicals Biosciences Dimethyl sulfoxide, 67-68-5, MFCD00002089, 1L
Molecular Formula: (CH3)2SO, Molecular Weight: 78.13, Beilstein Registry Number: 506008, Assay: ≥99.5% (GC)
Apexbio Technology LLC Lonidamine 50264-69-2 10mM (in 1mL DMSO)
Lonidamine (AF-1890) is a cell metabolism inhibitor targeting mitochondrial pyruvate carrier and hexokinase exhibiting inhibitory activity with a Ki value of approximately 2 5 M Through these targets it disrupts glycolytic metabolism by impairing aerobic glycolysis processes common in tumor cells Researchers utilize Lonidamine primarily to investigate metabolic pathways implicated in cancer cell energy production alterations in mitochondrial functions and related metabolic disorders Additionally Lonidamine is employed experimentally in studies examining mitochondrial dysfunction-associated conditions and inflammatory responses including pulmonary fibrosis
Apexbio Technology LLC XL019 945755-56-6 10mM (in 1mL DMSO)
XL019 (CAS 945755-56-6) is a selective inhibitor targeting Janus kinase 2 (JAK2) with an IC50 of 2 2 nM JAK2 regulates signaling pathways controlling erythroid granulocytic and megakaryocytic lineage differentiation via cytokine and hematopoietic growth factor receptors including erythropoietin and thrombopoietin receptors XL019 demonstrates high selectivity for JAK2 over related kinases (e g JAK1 TYK2) In mouse models bearing HEL 92 1 7 xenografts oral administration of XL019 significantly reduced tumor growth XL019 is evaluated clinically as a candidate for treating primary myelofibrosis and secondary myelofibrosis associated with polycythemia vera or essential thrombocythemia
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 Corticosterone(Synonyms: 17-Deoxycortisol, 11β,21-Dihydroxyprogesterone, Reichstein's Substance B, Kendall's Compound B), 10mM (in 1mL DMSO), CAS: 50-22-6.
Corticosterone (CAS 50-22-6) is an endogenous steroid hormone secreted by the adrenal cortex which exhibits affinity toward both glucocorticoid and mineralocorticoid receptors Its mechanism of action involves serum- and glucocorticoid-inducible kinase (SGK)-mediated phosphorylation of GDP dissociation inhibitor (GDI) at Ser-213 thereby promoting GDI-Rab4 complex assembly This activity enhances Rab4-dependent recycling of AMPA receptors to cortical neuron synapses leading to elevated synaptic excitatory responses Corticosterone thus serves as a useful biochemical tool for investigating stress-related modulation of synaptic transmission and plasticity
Apexbio Technology LLC PLX-4720 918505-84-7 10mM (in 1mL DMSO)
PLX-4720 (CAS 918505-84-7) is a selective inhibitor of the oncogenic kinase B-RafV600E a frequently observed activating mutation in cancer Structurally derived from a 7-azaindole scaffold PLX-4720 inhibits B-RafV600E with an IC50 of 13 nM exhibiting marked selectivity in comparison to wild-type B-Raf (IC50 160 nM) and other kinases such as FRK CSK SRC FAK FGFR and Aurora A (IC50 1000 nM) PLX-4720 decreases ERK phosphorylation in B-RafV600E-containing cells induces growth arrest and apoptosis in B-RafV600E melanoma lines and delays tumor progression in xenograft models harboring this mutation It represents a valuable tool in cancer research targeting B-Raf signaling pathways
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 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