Dimethyl Sulfoxide
Apexbio Technology LLC Roflumilast 162401-32-3 10mM (in 1mL DMSO)
Roflumilast is an orally available selective inhibitor of phosphodiesterase-4 (PDE-4) with an IC50 value of approximately 0 11 nM PDE-4 enzymes catalyze the hydrolysis of cyclic adenosine monophosphate (cAMP) and are predominantly expressed in various inflammatory and immune cells By selectively inhibiting PDE-4 activity Roflumilast elevates intracellular cAMP levels thus regulating cellular inflammatory signaling pathways This mechanism supports its use in the reduction of inflammatory responses associated with chronic obstructive pulmonary disease (COPD) Additionally Roflumilast has been investigated experimentally regarding its potential influence on glucose metabolism in early-stage type 2 diabetes mellitus
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 Wortmannin 19545-26-7 10mM (in 1mL DMSO)
Wortmannin is a selective inhibitor targeting phosphatidylinositol-3-kinase (PI3K) with reported IC50 of approximately 1 9 nM It inhibits PI3K through an ATP-noncompetitive binding mechanism interacting directly with the catalytic region Additionally wortmannin functions as a noncompetitive inhibitor of myosin light chain kinase (MLCK) with an IC50 around 1 9 M thus decreasing myosin light chain phosphorylation and associated smooth muscle contraction In biomedical research wortmannin is commonly employed to dissect the PI3K signaling pathway evaluate smooth muscle contractility and explore therapeutic potentials related to vascular dilation and inflammation modulation
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
Apexbio Technology LLC NSC23766 trihydrochloride 1177865-17-6 10mM (in 1mL DMSO)
NSC23766 trihydrochloride (CAS 1177865-17-6) is a selective inhibitor of the Rac1 GTPase It functions by binding specifically to guanine nucleotide exchange factors (GEFs) such as Trio and Tiam preventing their interaction with Rac1 and thus inhibiting Rac1 activation NSC23766 demonstrates an IC50 of approximately 50 M It has been used in various cellular models to study Rac1-dependent processes including endothelial barrier integrity and apoptosis regulation By modulating Rac1 activity NSC23766 serves as a tool compound for investigating the role of Rac signaling pathways in cellular apoptosis especially TNF- -induced JNK activation and barrier function dynamics
Apexbio Technology LLC SCH 527123 473727-83-2 10mM (in 1mL DMSO)
SCH 527123 (CAS 473727-83-2) is a selective antagonist of chemokine receptor 2 (CXCR2) It inhibits CXCR2-mediated signaling pathways by reducing phosphorylation events within the NF- B MAPK and AKT signaling cascades In colorectal cancer cell lines SCH 527123 suppresses cell growth in a dose-dependent manner with reported IC50 values ranging from approximately 18 to 40 mol/L after a 72-hour treatment Elevated IL-8 expression in cell lines such as HCT116 and Caco2 correlates with decreased sensitivity to SCH 527123 This compound is utilized in research investigating CXCR2 signaling in inflammation and tumor growth
Apexbio Technology LLC RGFP966 1357389-11-7;1396841-57-8 10mM (in 1mL DMSO)
RGFP966 is a selective inhibitor targeting histone deacetylase 3 (HDAC3) demonstrating an IC50 value of approximately 80 nM HDAC3 a Class I histone deacetylase regulates DNA transcription and influences chromatin structure replication and DNA repair It negatively regulates cognitive mechanisms such as learning and memory processes RGFP966 selectively inhibits HDAC3 without affecting other HDAC isoforms at concentrations up to 15 M as demonstrated by substrate-dependent assays In preclinical research RGFP966 has been utilized to investigate HDAC3 s role in neural functions particularly object recognition memory and to examine cellular effects including growth inhibition and apoptosis induction in models of cutaneous T-cell lymphoma
Apexbio Technology LLC Golgicide A 1139889-93-2 10mM (in 1mL DMSO)
Golgicide A is a reversible small-molecule inhibitor targeting the guanine nucleotide exchange factor GBF1 GBF1 functions as an ArfGEF facilitating Arf1 activation and COPI recruitment at the cis-Golgi membranes essential for Golgi structure maintenance and protein transport regulation Golgicide A disrupts Golgi morphology leading to dispersion of Golgi markers and altered COPI localization In cellular assays Golgicide A inhibits shiga toxin-mediated protein synthesis with an IC50 of approximately 3 3 M in Vero cells and impairs retrograde toxin trafficking and secretory protein transport Additionally Golgicide A is applied in HCV research to reduce viral RNA replication and alter NS5A localization causing accumulation of viral particles in infected cells
Apexbio Technology LLC Pacritinib (SB1518) 937272-79-2 10mM (in 1mL DMSO)
Pacritinib (SB1518) is a small molecule inhibitor targeting Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3) with IC50 values of 23 nM for wild-type JAK2 19 nM for JAK2V617F and 22 nM for FLT3 It inhibits phosphorylation of downstream effectors such as STAT5 and STAT3 mediated by JAK2 in Ba/F3 cells as well as phosphorylation of FLT3 and STAT5 in MV4-11 cells Pacritinib demonstrates good microsomal stability selectivity limited inhibitory activity toward CYP3A4 favorable permeability in cell permeability assays and oral bioavailability In preclinical studies treatment with pacritinib in Ba/F3-JAK2V617F murine allograft and MV4-11 xenograft models reduces disease progression and enhances survival These properties make pacritinib suitable for research concerning hematologic malignancies involving dysregulated JAK2 or FLT3 signaling pathways
Apexbio Technology LLC Enrofloxacin 93106-60-6 10mM (in 1mL DMSO)
Enrofloxacin a fluoroquinolone antibiotic exerts antibacterial activity by inhibiting bacterial DNA gyrase and topoisomerase IV enzymes essential for DNA replication and transcription This mechanism disrupts the DNA synthesis of pathogenic bacteria resulting in bacteriostatic outcomes In vitro experiments indicate that Enrofloxacin displays antimicrobial activity against Mycoplasma species such as Mycoplasma bovis with a minimum inhibitory concentration (MIC90) around 0 312 g/mL In biomedical research this compound is primarily utilized to establish microbial infection models and to study bacterial resistance mechanisms pharmaceutical efficacy and antibacterial pharmacodynamics
Apexbio Technology LLC Trifluoperazine 2HCl 440-17-5 10mM (in 1mL DMSO)
Trifluoperazine 2HCl is a dopamine D2 receptor antagonist extensively utilized in biomedical research for investigating dopaminergic signaling pathways It functions by selectively inhibiting the D2 subtype dopamine receptor exhibiting an IC50 value of approximately 1 1 nM Due to its receptor-blocking mechanism trifluoperazine is frequently employed to study dopamine-mediated neurotransmission receptor pharmacodynamics and neurological processes underlying disorders involving altered dopaminergic activity such as schizophrenia Additionally trifluoperazine serves as a tool compound for elucidating cellular responses linked to dopaminergic receptor modulation in in vitro receptor-binding assays and neuronal cell cultures
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