Dimethyl Sulfoxide
Apexbio Technology LLC PD318088 391210-00-7 10mM (in 1mL DMSO)
PD318088 (CAS 391210-00-7) is an allosteric non-ATP competitive inhibitor of MEK1/2 kinase activity Structurally related to PD184352 it interacts adjacent to the ATP-binding site of MEK1 in proximity to residues Ile216 Phe209 Arg189 and Asp190 stabilizing a ternary complex involving MEK1/2 and MgATP This binding moderately increases the dissociation constant (Kd) for the MEK dimerization state from 75 nM to 140 nM PD318088 is mainly utilized as a molecular tool in protein kinase signaling research particularly in pathways involving MEK1/2
Apexbio Technology LLC Argatroban 74863-84-6 10mM (in 1mL DMSO)
Argatroban is a synthetic small-molecule inhibitor acting as a direct binder to thrombin s active site thereby blocking the thrombin-mediated conversion of fibrinogen into fibrin It competitively inhibits thrombin-induced platelet activation and blood clot formation exhibiting an inhibitory constant (Ki) of approximately 19 nM Due to its specificity and direct mechanism Argatroban is frequently employed in experimental research scenarios to investigate thrombin-dependent coagulation pathways platelet aggregation studies and antithrombotic effects in various in vitro assays and animal thrombosis models
Apexbio Technology LLC Tubastatin A 1252003-15-8 10mM (in 1mL DMSO)
Tubastatin A (CAS 1252003-15-8) is a selective inhibitor of histone deacetylase 6 (HDAC6) an enzyme mediating acetylation states crucial for regulating both histone and non-histone proteins Tubastatin A inhibits HDAC6 with an IC50 of approximately 15 nM and shows minimal activity against class I HDAC isoforms demonstrating greater than 200-fold selectivity In vitro Tubastatin A induces hyperacetylation of -tubulin reduces neuronal cell death inhibits inflammatory cytokines (IL-6 TNF) production in human THP-1 macrophages and decreases NO secretion from mouse Raw 264 7 cells In animal models it exhibits anti-inflammatory and anti-tumor effects Tubastatin A is utilized in research exploring cancer biology inflammation and neuroprotection
Apexbio Technology LLC Pranlukast 103177-37-3 10mM (in 1mL DMSO)
Pranlukast (CAS 103177-37-3) is a selective antagonist of cysteinyl leukotriene (cysLT) receptors exhibiting its pharmacological action by competitively binding to targeted leukotriene receptor sites It specifically prevents the interaction of endogenous leukotrienes (LTC4 LTD4 LTE4) with corresponding receptors located on pulmonary cell membranes thus reducing leukotriene-driven airway inflammation and bronchoconstriction Binding experiments demonstrate that pranlukast possesses notably greater affinity for LTE4 and LTD4 compared to LTC4 In biomedical research pranlukast is frequently utilized for mechanistic studies and pharmacological modeling of asthma allergic rhinitis and related airway inflammatory conditions
Apexbio Technology LLC SB 203580 152121-47-6 10mM (in 1mL DMSO)
SB 203580 (CAS 152121-47-6) is a pyridinyl imidazole derivative acting as a selective inhibitor of the p38 mitogen-activated protein kinase (MAPK) It competes with ATP binding at or near the kinase ATP-binding region showing a Ki of 21 nM SB 203580 is also reported to inhibit c-Raf in vitro (IC50 2 mM) Experimental studies indicate that SB 203580 reverses multidrug resistance in L1210/VCR cells by reducing tolerance to vincristine Additionally the compound is instrumental in investigating the p38 MAPK pathway in cellular signaling and ischemic neuroprotection models
Apexbio Technology LLC Hesperadin 422513-13-1 10mM (in 1mL DMSO)
Hesperadin is a small-molecule ATP-competitive inhibitor targeting Aurora B kinase a serine/threonine-protein kinase involved in mitotic regulation By occupying the ATP-binding pocket of Aurora B and adjacent hydrophobic regions Hesperadin suppresses kinase activity with an IC50 approximately 250 nM In mitotic cells Aurora B-mediated phosphorylation of histone H3 Ser-10 is inhibited by Hesperadin this phosphorylation event is widely utilized as a mitotic biomarker Furthermore experimental applications of Hesperadin include investigating cell-cycle dynamics chromosome alignment and spindle checkpoint mechanisms as evidenced by its ability to disrupt proper chromosome alignment and segregation at approximately 40 nM IC50
Apexbio Technology LLC KPT-330 1393477-72-9 10mM (in 1mL DMSO)
KPT-330 (CAS 1393477-72-9) is an orally bioavailable small-molecule inhibitor selectively targeting chromosome region maintenance 1 protein (CRM1) a nuclear export receptor involved in the active transport of tumor suppressors transcription factors and cell-cycle regulators Overexpression and deregulation of CRM1 are frequently associated with cancer progression KPT-330 inhibits CRM1 function promoting nuclear retention of regulatory proteins such as p21 and inducing apoptosis through activation of apoptotic signaling pathways (e g PAR-4 activation Bax upregulation PARP cleavage caspase-3 activation) In preclinical studies KPT-330 demonstrated antitumor activity against renal cell carcinoma non-small cell lung cancer and pancreatic cancer models
Apexbio Technology LLC Vidarabine 5536-17-4 10mM (in 1mL DMSO)
Vidarabine is an antiviral nucleoside analog widely studied for inhibiting replication of herpes simplex virus (HSV) and varicella-zoster virus (VZV) Structurally vidarabine is an adenine arabinoside analog that interferes with viral DNA synthesis via competitive inhibition of viral DNA polymerase resulting in chain termination In vitro studies demonstrate antiviral activity against HSV type 1 and type 2 with IC50 values typically ranging approximately from 0 1 to 1 0 M depending on experimental conditions and viral strains Vidarabine is commonly used in biomedical laboratories for investigating viral replication mechanisms screening for antiviral candidates and elucidating nucleoside analog resistance patterns
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 ICG 001 847591-62-2 10mM (in 1mL DMSO)
ICG 001 is a small molecule inhibitor of the canonical Wnt/ -catenin signaling pathway Mechanistically it competes with -catenin for interaction with CREB-binding protein (CBP) thereby selectively disrupting CBP/ -catenin-mediated transcriptional activity driven by the TCF/ -catenin complex (IC50 3 M) Experimental studies demonstrated its use in assessing CBP-dependent biological functions regulated by Wnt signaling Research applications include investigating CBP/ -catenin roles in cancer cell proliferation such as colorectal cancer cells (HCT-116 SW480) glioblastoma stem cell growth and fibrotic responses in pulmonary and dermal experimental models Additionally ICG 001 is under evaluation in clinical studies aiming at treatment of colorectal cancer and leukemia
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 Rimonabant 168273-06-1 10mM (in 1mL DMSO)
Rimonabant (SR141716) is a selective antagonist targeting the cannabinoid type 1 (CB1) receptor It exhibits affinity for CB1 receptors with a Ki of approximately 1 8 nM contrasting with a lower affinity for CB2 receptors (Ki 514 nM) Through blocking CB1 receptor signaling this compound is primarily utilized experimentally to investigate behaviors associated with appetite control energy balance and substance consumption Studies using animal models demonstrate that administration of Rimonabant reduces intake of palatable foods and beverages as well as sucrose and alcohol consumption highlighting its relevance in obesity feeding behavior and addiction-related research contexts
Apexbio Technology LLC CP-673451 343787-29-1 10mM (in 1mL DMSO)
CP-673451 (CAS 343787-29-1) is an ATP-competitive inhibitor with specificity for platelet-derived growth factor receptors (PDGFR- / ) It exhibits inhibitory potency with IC50 values of 10 nM for PDGFR- and 1 nM for PDGFR- while demonstrating significantly less inhibition toward kinases such as VEGFR-1 VEGFR-2 Lck TIE-2 and EGFR In cellular assays CP-673451 effectively inhibits PDGFR- phosphorylation in PAE- cells (IC50 6 4 nM) and reduces c-kit activity in H526 cells at micromolar range Its anticancer efficacy has been established by suppressing tumor growth and vascularization in xenograft models indicating its potential utility in cancer research and angiogenesis studies
Apexbio Technology LLC Regorafenib 755037-03-7 10mM (in 1mL DMSO)
Regorafenib (CAS 755037-03-7) is an orally bioavailable inhibitor targeting multiple receptor tyrosine kinases (RTKs) such as VEGFR1/2/3 PDGFR Kit RET Raf-1 B-RAF and B-RAFV600E By impeding kinase phosphorylation (IC50 values ranging from approximately 1 5 46 nM) regorafenib disrupts signaling pathways associated with angiogenesis tumor cell proliferation and metastasis Preclinically regorafenib inhibited VEGFR2 phosphorylation (IC50 3 nM) and reduced VEGF-induced endothelial cell proliferation in vitro In rodent tumor xenograft models it demonstrated dose-dependent tumor growth suppression and antimetastatic potential supporting its utility for oncology research
Apexbio Technology LLC Cyclopamine 4449-51-8 10mM (in 1mL DMSO)
Cyclopamine (CAS 4449-51-8) is a naturally occurring steroidal alkaloid that selectively inhibits the Hedgehog (Hh) signaling pathway a conserved cascade involved in cellular proliferation and differentiation In human breast cancer cell lines (MCF-7 and MDA-MB-231) cyclopamine treatment (10 20 M) significantly suppresses proliferation induces cell cycle arrest at G1 phase and reduces invasive capabilities In FXR-bla assays cyclopamine exhibits an EC50 of 10 57 M As an Hh-antagonist it is widely utilized in research examining embryogenesis cancer biology tumor invasiveness and developmental defects