Dimethyl Sulfoxide
Apexbio Technology LLC Olmesartan 144689-24-7 10mM (in 1mL DMSO)
Olmesartan (CAS 144689-24-7) is a small molecule angiotensin II receptor antagonist primarily acting by selectively blocking the binding of angiotensin II to AT1 receptors This mechanism interrupts angiotensin II-mediated vasoconstriction and aldosterone secretion resulting in antihypertensive effects In biomedical research Olmesartan serves as a valuable tool for examining hypertensive disease models elucidating angiotensin II signaling pathways and exploring therapeutic strategies targeting cardiovascular regulation
Apexbio Technology LLC E-64 66701-25-5 10mM (in 1mL DMSO)
E-64 is a selective inhibitor targeting cysteine proteases isolated originally from Aspergillus cultures Structurally classified as an L-trans-epoxysuccinyl peptide it irreversibly inhibits proteases such as papain ficin and bromelain by covalent binding to the active-site cysteine residue Its inhibitory activity additionally extends to mammalian cysteine proteases including cathepsins B H and L as well as calcium-dependent protease calpain with reported IC50 values ranging approximately between 10-100 nM depending on specific enzyme assays and conditions In research laboratories E-64 is primarily utilized for mechanistic studies active-site titration assays and quantitative evaluation of cysteine protease concentrations and enzyme kinetics
Apexbio Technology LLC PF-543 1415562-82-1 10mM (in 1mL DMSO)
PF-543 (CAS 1415562-82-1) is a cell-permeable inhibitor targeting sphingosine kinase 1 (SphK1) an enzyme that phosphorylates sphingosine to sphingosine-1-phosphate (S1P) It displays potent inhibitory activity against SphK1 with an IC50 of 3 6 nM through sphingosine-competitive (non-ATP competitive) binding Treatment of SphK1-overexpressing head and neck cancer (1483) cells led to a ten-fold decrease in S1P levels confirming effective target engagement PF-543 is widely utilized as a research tool in studies investigating SphK1-mediated signaling pathways in cancer biology and immune cell trafficking
Apexbio Technology LLC MK-5172 1350514-68-9 10mM (in 1mL DMSO)
MK-5172 is a selective inhibitor targeting the hepatitis C virus (HCV) NS3/4A protease an enzyme essential for viral replication The HCV virus genome encodes this protease which cleaves polyprotein precursors enabling functional viral proteins formation during replication MK-5172 inhibits protease activity across multiple HCV genotypes demonstrating IC50 values in enzymatic assays at low nanomolar concentrations In cell-based replicon systems MK-5172 exhibits IC50 values of 2 nM (genotype 1a) 0 5 nM (genotype 1b) 8 nM (genotype 2a) and 13 nM (genotype 3) MK-5172 is utilized in antiviral studies examining various genotype infections viral resistant variants and the dynamics of viral load reductions in experimental chronic infections
Apexbio Technology LLC CFI-400945 1338806-73-7 10mM (in 1mL DMSO)
CFI-400945 (CAS 1338806-73-7) is an orally bioavailable inhibitor specifically targeting polo-like kinase 4 (PLK4) a member of the polo-like kinase family involved in centriole duplication and cell cycle control By competitively inhibiting ATP binding to PLK4 CFI-400945 potently suppresses PLK4 catalytic activity (IC50 2 8 nM) and blocks PLK4 autophosphorylation in cellular assays (EC50 12 3 nM) The compound exhibits high selectivity against other polo-like kinases and demonstrates antiproliferative activity in various cancer cell lines Thus CFI-400945 is applied in cancer biology research particularly for studying centrosome regulation and tumor growth inhibition
Apexbio Technology LLC Reparixin 266359-83-5 10mM (in 1mL DMSO)
Reparixin (CAS 266359-83-5) is a noncompetitive allosteric inhibitor of chemokine receptors CXCR1 and CXCR2 which are seven-transmembrane G-protein coupled receptors involved notably in acute inflammatory responses Reparixin specifically disrupts CXCR1/2-mediated neutrophil recruitment and migration without affecting other receptor pathways In murine ischemia-reperfusion injury models Reparixin administration significantly inhibits neutrophil influx and associated inflammation-related tissue damage Thus Reparixin serves as a valuable research tool for investigating CXCR-dependent inflammatory mechanisms and evaluating therapeutic potentials in conditions such as acute lung injury and spinal cord damage
Apexbio Technology LLC Reversine 656820-32-5 10mM (in 1mL DMSO)
Reversine (CAS 656820-32-5) is a small molecule inhibitor targeting Aurora kinases a family of serine/threonine kinases involved in mitotic progression Reversine inhibits Aurora kinase A B and C with IC50 values of 150 nM 500 nM and 400 nM respectively In vitro studies show reversine can induce dedifferentiation of murine myoblast cells and possesses regenerative potential Additionally reversine displays anti-tumor effects by suppressing the expression of Aurora kinases thus disrupting cell-cycle progression In cervical carcinoma mouse models (U14 cells) reversine combined with aspirin synergistically decreases tumor growth highlighting reversine s value for cancer biology research
Apexbio Technology LLC AGN 194310 229961-45-9 10mM (in 1mL DMSO)
AGN 194310 is a pan-retinoic acid receptor (RAR) antagonist with affinity for RAR RAR and RAR It binds these receptors with Kd values of 3 nM 2 nM and 5 nM respectively By competing with RAR agonists AGN 194310 blocks receptor-mediated cellular responses In cell-based assays AGN 194310 inhibits the proliferation and colony formation of prostate carcinoma cell lines (LNCaP PC3 DU-145) induces G1 cell cycle arrest and promotes apoptosis In addition it suppresses agonist-induced differentiation in HL60 cells AGN 194310 serves as a research tool to investigate RAR-driven signaling pathways and tumor cell growth mechanisms particularly in oncology studies examining retinoid receptor functions
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 MLN120B 783348-36-7 10mM (in 1mL DMSO)
MLN120B (CAS 783348-36-7) is a small molecule inhibitor targeting the beta subunit of I B kinase (IKK ) an enzyme integral to the NF- B signaling pathway IKK mediates phosphorylation and subsequent degradation of the NF- B inhibitor I B thereby activating NF- B-dependent transcription involved in inflammatory and immune responses MLN120B inhibits IKK -catalyzed phosphorylation of I B (IC50 20 M) attenuating NF- B activation in multiple myeloma cell lines (RPMI 8226 INA 6 MM 1S) and reducing inflammation-induced joint damage in animal arthritis models Consequently MLN120B serves as a research tool in studying NF- B signaling-mediated disorders
Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 10mM (in 1mL DMSO)
Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects
Apexbio Technology LLC Riociguat 625115-55-1 10mM (in 1mL DMSO)
Riociguat (CAS 625115-55-1) chemically known as BAY 63-2521 is a small-molecule stimulator of soluble guanylate cyclase (sGC) It directly activates sGC independently and also enhances the enzyme s sensitivity to nitric oxide (NO) leading to elevated cyclic guanosine monophosphate (cGMP) levels Elevated cGMP induces smooth muscle relaxation and vasodilation Riociguat has been examined clinically for potential therapeutic roles in chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH)
Apexbio Technology LLC CVT-313 199986-75-9 10mM (in 1mL DMSO)
CVT-313 (CAS 199986-75-9) is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) an enzyme essential for G1/S transition during cell cycle progression By targeting CDK2 CVT-313 effectively reduces hyperphosphorylation of retinoblastoma protein (Rb) leading to cell cycle arrest at the G1/S boundary In vitro studies with MRC-5 fibroblasts demonstrated significant growth inhibition Additionally CVT-313 induces apoptosis in diffuse large B-cell lymphoma by diminishing phosphorylation of Rb at T821 and downregulating anti-apoptotic protein Mcl-1 In animal models of arterial restenosis CVT-313 significantly reduces neointimal proliferation indicating potential utility for proliferative disorders research
Apexbio Technology LLC BI6727 VOLASERTIB1ML DMSO
BI6727 (Volasertib CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk) primarily targeting Plk1 with an IC50 of 0 87 nM and showing lower potency towards Plk2 (IC50 5 nM) and Plk3 (IC50 56 nM) Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types representing a potential therapeutic target BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116 EC50 23 nM) lung (NCI-H460 EC50 21 nM) melanoma (BRO EC50 11 nM) and hematologic cancer (GRANTA EC50 15 nM) In vivo BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models
Apexbio Technology LLC Pirarubicin 72496-41-4 10mM (in 1mL DMSO)
Pirarubicin is a DNA intercalating anthracycline antibiotic structurally related to doxorubicin that targets the DNA topoisomerase II enzyme By stabilizing the cleavable DNA-enzyme complex pirarubicin induces DNA strand breaks and inhibits DNA replication and cellular proliferation Its primary mode of action involves disruptive interactions with topoisomerase II-mediated DNA cleavage and repair mechanisms Pirarubicin is utilized as an antineoplastic agent in oncology research particularly in evaluating its activity against diverse cancer cell lines In vitro studies reported IC50 values typically ranging from approximately 0 1 to several micromolar concentrations varying according to cell type and experimental conditions Therefore pirarubicin serves as a tool compound in pharmacological studies investigating DNA-topoisomerase inhibitors and therapeutic resistance mechanisms