Dimethyl Sulfoxide
Apexbio Technology LLC GW441756 504433-23-2 10mM (in 1mL DMSO)
GW441756 (CAS 504433-23-2) is a small-molecule inhibitor targeting TrkA kinase and LRRK2 It inhibits TrkA kinase activity with an IC50 of 320 nM potentially modulating downstream signaling involved in cellular proliferation differentiation and apoptosis Selectivity studies indicated limited inhibitory effects on other kinases such as cRaf1 and CDK2 with respective IC50 values above 12 M and 7 M GW441756 induced dose-dependent anti-proliferative and pro-apoptotic effects in the human sarcoma cell line HTB114 It also inhibited LRRK2-mediated phosphorylation at Ser935 (IC50 2 2 M) without significant cytotoxicity (IC50 20 M) GW441756 serves as a research tool in oncology and neurobiology
Apexbio Technology LLC OTX-015 202590-98-5 10mM (in 1mL DMSO)
OTX-015 (CAS 202590-98-5) is a selective inhibitor of BRD2 BRD3 and BRD4 proteins within the BET (bromodomain and extra-terminal) family involved in transcriptional regulation By disrupting the interaction between these BRD proteins and acetylated histone H4 OTX-015 exhibits inhibitory activity demonstrated by IC50 values between 92 and 112 nM and in vitro EC50 ranging from 10 to 19 nM OTX-015 treatment reduces proliferation (GI50 60 200 nM) induces G1 arrest and promotes apoptosis in various human cancer cell models In xenograft mouse studies of BRD-NUT midline carcinoma orally administered OTX-015 significantly suppresses tumor growth showing potential utility for cancer research
Apexbio Technology LLC Y-27632 dihydrochloride 129830-38-2 10mM (in 1mL DMSO)
Y-27632 dihydrochloride (CAS 129830-38-2) is a small-molecule inhibitor targeting ROCK kinases (Rho-associated protein kinases) specifically interacting with the catalytic domains of ROCK-1 and ROCK-2 It inhibits their kinase activity with an IC50 of approximately 140 nM By targeting ROCK signaling Y-27632 disrupts Rho-mediated formation of cellular stress fibers influences cell cycle progression from G1 to S phase and interferes with cytokinesis It is commonly utilized in studies investigating cell proliferation cytoskeletal organization and stem cell viability
Apexbio Technology LLC Zalcitabine 7481-89-2 10mM (in 1mL DMSO)
Zalcitabine is a nucleoside analog inhibitor targeting viral reverse transcriptase a key enzyme promoting viral replication By competitively binding to the active site of reverse transcriptase zalcitabine terminates DNA chain elongation effectively inhibiting viral DNA synthesis In vitro studies have demonstrated inhibitory activity against HIV-1 with reported IC50 values ranging approximately from 0 03 to 0 3 M Zalcitabine is frequently utilized in biomedical research as an antiviral reference molecule for studying HIV therapeutic targets antiviral drug resistance and mechanisms of reverse transcription inhibition
Apexbio Technology LLC Doxercalciferol 54573-75-0 10mM (in 1mL DMSO)
Doxercalciferol chemically known as 1 -Hydroxyvitamin D2 is a synthetic analog of vitamin D2 characterized by selective activation of the vitamin D receptor (VDR) Upon metabolic activation Doxercalciferol undergoes hepatic transformation to its biologically active form inducing gene transcription mediated via the VDR signaling pathway Central to its mechanism activated VDR regulates calcium and phosphate homeostasis influencing cellular differentiation proliferation and parathyroid hormone expression In biomedical research Doxercalciferol serves as a tool compound to investigate the molecular pathways regulated by vitamin D receptor activation particularly in renal insufficiency models bone metabolism studies and parathyroid physiology experiments
Apexbio Technology LLC Triapine 236392-56-6; 200933-27-3; 143621-35-6 10mM (in 1mL DMSO)
Triapine is a small molecule thiosemicarbazone derivative known to inhibit ribonucleotide reductase an enzyme essential for the conversion of ribonucleotides to deoxyribonucleotides thereby interfering with DNA synthesis and repair pathways Through this inhibition mechanism Triapine exhibits antitumor activity in a range of experimental cancer models including human ovarian carcinoma xenografts and murine leukemia models and inhibits proliferation across multiple tumor cell lines Due to its mechanistic specificity Triapine serves as a useful chemical tool for biomedical research into nucleic acid metabolism cancer cell replication and therapeutic resistance mechanisms
Apexbio Technology LLC Ronidazole 7681-76-7 10mM (in 1mL DMSO)
Ronidazole is a nitroimidazole compound exhibiting both antiprotozoal and antibacterial activities Its mechanism of action involves the generation of metabolites that interact with microbial DNA resulting in DNA damage and inhibition of nucleic acid synthesis Ronidazole is commonly employed in veterinary research settings to investigate therapeutic interventions against protozoan parasites such as Tritrichomonas foetus infections in feline models Histomonas meleagridis-mediated histomoniasis and Brachyspira hyodysenteriae-related swine dysentery It can be administered orally to experimental animal subjects for clarifying pathological mechanisms and therapeutic pathways in parasitic disease models Currently detailed IC50 data for Ronidazole remain underreported in literature
Apexbio Technology LLC Entinostat (MS-275,SNDX-275) 209783-80-2 10mM (in 1mL DMSO)
Entinostat (MS-275 SNDX-275 CAS 209783-80-2) is an orally bioavailable small molecule inhibitor targeting histone deacetylases (HDACs) a family of enzymes involved in transcriptional regulation by modifying histone acetylation Specifically entinostat exhibits inhibitory activity against class I HDAC enzymes HDAC1 HDAC3 and HDAC8 with reported IC50 values of 0 368 M 0 501 M and 63 4 M respectively In preclinical investigations entinostat demonstrates anti-proliferative effects in diverse human tumor cell lines including breast colon lung multiple myeloma ovarian pancreatic prostate cancers and leukemia Due to these properties entinostat is widely utilized in oncology research
Apexbio Technology LLC PF-8380 1144035-53-9 10mM (in 1mL DMSO)
PF-8380 (CAS 1144035-53-9) is a selective inhibitor of autotaxin (ATX) a secreted enzyme with lysophospholipase D activity that converts lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA) As increased local LPA production promotes tumor proliferation and invasion targeting ATX reduces LPA synthesis PF-8380 demonstrates potent ATX inhibition (IC50 2 8 nM) significantly lowering LPA in plasma and tissue in rodent models It reduces Akt activation enhances radiosensitivity and diminishes growth and invasion of glioblastoma cells indicating utility in oncology research focused on ATX-LPA signaling pathways
Apexbio Technology LLC Valganciclovir HCl 175865-59-5 10mM (in 1mL DMSO)
Valganciclovir hydrochloride is an antiviral prodrug that undergoes rapid enzymatic conversion to the active metabolite ganciclovir after oral administration Ganciclovir inhibits viral replication by selectively targeting viral DNA polymerase thereby interfering with viral DNA synthesis and slowing cytomegalovirus (CMV) proliferation Valganciclovir is commonly utilized in laboratory studies to evaluate antiviral activity against CMV and related herpesviruses and to investigate its therapeutic potential in CMV-associated infections including retinitis and organ transplant-associated CMV infections In vitro studies report an IC50 value for valganciclovir-derived ganciclovir ranging approximately from 0 2 to 2 8 M depending on experimental cell type and viral strain
Apexbio Technology LLC Latrepirdine 97657-92-6 10mM (in 1mL DMSO)
Latrepirdine (CAS 97657-92-6) is an orally bioavailable small molecule investigated for its neuroprotective properties in preclinical studies of neurodegenerative diseases including Alzheimer s and Huntington s diseases Although its precise mechanism remains under investigation latrepirdine has demonstrated the ability to inhibit neuronal cell death pathways in animal disease models Moreover preliminary evidence indicates potential cognitive enhancement in normal physiological conditions Latrepirdine serves as a relevant tool compound to study neuronal survival mechanisms and cognitive function regulation
Apexbio Technology LLC Lonafarnib 193275-84-2 10mM (in 1mL DMSO)
Lonafarnib (CAS 193275-84-2) also known as SCH66336 or Sarasar is a tricyclic orally bioavailable inhibitor of farnesyltransferase (FTase) functioning without peptide or sulfhydryl groups FTase mediates post-translational farnesylation of Ras proteins a modification required for their membrane localization and activation of downstream signaling pathways involved in cellular growth proliferation and survival By inhibiting this enzymatic activity Lonafarnib disrupts Ras translocation to the plasma membrane limiting Ras-mediated signaling Currently Lonafarnib is widely evaluated in preclinical and clinical investigations particularly in oncology contexts
Apexbio Technology LLC R406 (free base) 841290-80-0 10mM (in 1mL DMSO)
R406 (free base CAS 841290-80-0) is a small molecule inhibitor of spleen tyrosine kinase (SYK) a non-receptor kinase expressed predominantly within hematopoietic cells As an ATP-competitive inhibitor R406 selectively binds SYK s ATP-binding domain thereby suppressing its kinase activity and downstream phosphorylation events (IC50 41 nM) In mast cells R406 inhibits Fc receptor-driven degranulation with an EC50 value of 56-64 nM In diffuse large B-cell lymphoma models it blocks SYK-dependent B-cell receptor signaling through impaired autophosphorylation at sites Y525/Y526 resulting in apoptosis This compound is orally bioavailable and serves as a research tool for hematologic malignancies and autoimmune diseases