Dimethyl Sulfoxide
Apexbio Technology LLC VER 155008 1134156-31-2 10mM (in 1mL DMSO)
VER 155008 (CAS 1134156-31-2) is a small molecule inhibitor targeting members of the heat shock protein 70 (Hsp70) chaperone family It primarily inhibits Hsp70 by binding within its ATPase domain and suppressing its intrinsic ATPase activity thereby reducing chaperone-mediated cell survival functions VER 155008 demonstrates potent inhibition of Hsp70 (IC50 0 5 M) and exhibits moderate inhibitory action against related chaperones Hsc70 and glucose-regulated protein Grp78 In cancer cell models this compound diminishes cell proliferation and promotes apoptosis suggesting utility as a research tool in studying chaperone-dependent tumor cell survival pathways
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 XL-888 1149705-71-4 10mM (in 1mL DMSO)
XL-888 (CAS 1149705-71-4) is an orally bioavailable small molecule inhibitor targeting heat shock protein 90 (HSP90) It selectively inhibits HSP90 and HSP90 with IC50 values of 22 nM and 44 nM respectively while exhibiting markedly weaker inhibition against a panel of other kinases Structural analyses indicated XL-888 binds HSP90 via hydrogen bonding interactions involving the Asp93 residue In tumor cell assays XL-888 potently suppresses proliferation with IC50 values in the range of 0 1-45 5 nM XL-888 is used in oncology research particularly for studying resistance mechanisms to targeted therapies
Apexbio Technology LLC SKI II 312636-16-1 10mM (in 1mL DMSO)
SKI II (CAS 312636-16-1) is a small-molecule inhibitor of sphingosine kinase (SK) an enzyme involved in converting sphingosine into sphingosine-1-phosphate (S1P) SKI II inhibits SK activity with an IC50 of 0 5 M through a mechanism independent of competition at the ATP-binding site Selectivity assessments showed no inhibitory effect against human kinases ERK2 PKC-I or PI3K Cellular assays demonstrate that SKI II effectively inhibits endogenous SK reducing S1P synthesis and subsequently suppressing proliferation and inducing apoptosis in various cancer cell lines including MDA-MB-231 T-24 MCF-7 and MCF-7/VP cells
Apexbio Technology LLC TIC10 41276-02-2 10mM (in 1mL DMSO)
TIC10 (TRAIL-inducing compound 10) is a small molecule inhibitor with oral bioavailability capable of penetrating the blood-brain barrier It functions primarily by simultaneously inhibiting Akt and ERK pathways resulting in Foxo3a nuclear translocation and transcriptional activation of TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) TRAIL is involved in apoptosis induction in cancer cells often compromised during tumor progression TIC10 triggers the expression of TRAIL independently of p53 status enabling apoptosis in diverse cancer cell types In preclinical xenograft models and orthotopic glioblastoma studies TIC10 has demonstrated TRAIL-mediated antitumor activity supporting its use in cancer biology research and therapeutic investigations
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 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 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 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 Etomidate 10mM (in 1mL DMSO)
A1958 is a small molecule utilized in biomedical research that acts primarily as an inhibitor targeting specific signaling pathways or protein interactions relevant to cellular processes The compound s mechanism typically involves selective modulation or inhibition of targeted biomolecules influencing downstream biological pathways A1958 serves as a research tool for studying cellular mechanisms underlying disease states aiding in cell-based assays to elucidate molecular function and clarify therapeutic targets in biomedical studies
Apexbio Technology LLC YM155 781661-94-7 10mM (in 1mL DMSO)
YM155 (Sepantronium Bromide CAS 781661-94-7) is a small-molecule inhibitor targeting survivin the smallest protein member of the inhibitor of apoptosis (IAP) gene family YM155 potently suppresses survivin expression while demonstrating minimal influence on other IAP family members or BCL-2-associated proteins Preclinical research shows YM155 inhibits proliferation and induces apoptosis across various human cancer cell lines including non-small cell lung cancer (NSCLC) melanoma bladder cancer aggressive non-Hodgkin lymphoma triple-negative breast cancer (TNBC) and Wilms tumor models In animal xenograft studies YM155 administration results in tumor regression reduces spontaneous metastasis and notably prolongs survival