Dimethyl Sulfoxide
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 CO-1686 (AVL-301) 1374640-70-6 10mM (in 1mL DMSO)
CO-1686 (AVL-301 CAS 1374640-70-6) is an orally delivered irreversible small molecule inhibitor targeting mutated epidermal growth factor receptor (EGFR) It functions by forming a covalent bond at cysteine 797 in the ATP-binding domain of EGFR selectively inhibiting mutant variants such as L858R/T790M with reported IC50 values below 0 51 nM CO-1686 preferentially targets mutant EGFR over wild-type demonstrating approximately 22-fold selectivity Preclinical studies using non-small cell lung cancer (NSCLC) cell lines and xenograft models carrying EGFR mutations showed potent anti-proliferative and tumor regression effects Thus CO-1686 represents a valuable research tool in studying mutant EGFR-mediated oncogenesis
Gold Biotechnology Inc DMSO, ACS Grade 10 mL
Dimethylsulfoxide (DMSO) is a very polar organic compound that is useful in organic chemistry for solubilizing organic and inorganic compounds. DMSO is also used as a cryoprotectant for cell media, preventing the formation of ice crystals, which would otherwise damage cells. DMSO can be used in PCR reactions to inhibit the self-complementation of DNA or PCR primers and increase amplification, especially for DNA sequences, which have GC rich sequences.
Apexbio Technology LLC DMXAA (Vadimezan) 117570-53-3 10mM (in 1mL DMSO)
DMXAA (Vadimezan AS-1404) is a tumor vascular disrupting and apoptosis-inducing agent functioning primarily through inhibition of DT-diaphorase (DTD) It acts by suppressing DTD enzymatic activity showing an IC50 of approximately 62 5 M Additionally DMXAA inhibits various kinases notably VEGFR2 disrupting endothelial cells and blood vessel formation to induce tumor cell apoptosis and vascular necrosis Experimentally DMXAA demonstrates activity in murine tumor models including induction of apoptosis in endothelial cells and tumor vasculature promoting necrosis and tumor regression Therefore DMXAA is commonly used in oncology research focused on anti-angiogenesis and tumor vascular disruption mechanisms
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 PF-562271 HCl 939791-41-0 10mM (in 1mL DMSO)
PF-562271 HCl (CAS 939791-41-0) is a potent ATP-competitive reversible inhibitor targeting focal adhesion kinase (FAK) and its homolog proline-rich tyrosine kinase 2 (Pyk2) It inhibits FAK and Pyk2 enzymatic activity with reported IC50 values of 1 5 nmol/L and 14 nmol/L respectively FAK is a non-receptor tyrosine kinase regulating cell adhesion migration and growth while Pyk2 shares structural similarity to FAK In animal models of cancer PF-562271 reduces tumor progression and metastatic spread with dose-dependent suppression of FAK phosphorylation (EC50 93 ng/mL) Thus PF-562271 serves as an important tool for investigating FAK/Pyk2-mediated pathways in oncology research
Apexbio Technology LLC THZ1 1604810-83-4 10mM (in 1mL DMSO)
THZ1 (CAS 1604810-83-4) is a covalent inhibitor of cyclin-dependent kinase 7 (CDK7) targeting specifically the cysteine residue C312 outside its kinase domain It exhibits potent inhibition with an IC50 of 3 2 nM against CDK7 in kinase binding assays In cellular studies THZ1 suppresses proliferation of Jurkat and Loucy T-cell acute lymphoblastic leukemia (T-ALL) cell lines (IC50 50 nM and 0 55 nM respectively) by disrupting CDK7-mediated signaling transcriptional regulation mediated by RUNX1 and RNA polymerase II CTD phosphorylation Thus THZ1 is utilized in cancer research to investigate transcriptional dysregulation in malignancies
Apexbio Technology LLC Thioridazine HCl 130-61-0 10mM (in 1mL DMSO)
Thioridazine HCl is a pharmacological inhibitor targeting dopamine receptor subtypes D2 and D4 as well as a calcium channel blocker It modulates dopaminergic neurotransmission by interfering with receptor-mediated signaling and reduces intracellular calcium influx via calcium channel inhibition (IC50 approximately 1 0 M) Thioridazine is frequently utilized in research contexts involving dopaminergic signaling pathways calcium-related cellular processes and investigations of pharmacological sensitivity shifts following prolonged receptor modulation Specifically it is employed experimentally to examine receptor-mediated cardiovascular responses such as hypotension and to assess alterations in dopamine receptor responsiveness induced by chronic exposure regimens
Apexbio Technology LLC Salubrinal 405060-95-9 10mM (in 1mL DMSO)
Salubrinal is a cell-permeable inhibitor of eukaryotic translation initiation factor 2 alpha (eIF2 ) dephosphorylation exhibiting an IC50 of approximately 15 M It prevents phosphatase complexes from removing phosphate groups from eIF2 thus maintaining its phosphorylated state and modulating protein synthesis during cellular stress responses Salubrinal is utilized experimentally in vitro to investigate apoptotic mechanisms related to endoplasmic reticulum (ER) stress For instance it provides cytoprotection against ER stress-induced apoptosis triggered by protein glycosylation inhibitors or ER-Golgi trafficking inhibitors In vivo murine models employ salubrinal to explore cellular processes underlying oxidative stress and nephrotoxicity induced by chemotherapeutic treatments through modulation of ER stress-associated apoptosis signaling pathways Currently no clinical trials involving salubrinal have been reported