Dimethyl Sulfoxide
Apexbio Technology LLC Stattic 19983-44-9 10mM (in 1mL DMSO)
Stattic (CAS 19983-44-9) is a small-molecule inhibitor specifically targeting signal transducer and activator of transcription 3 (STAT3) It suppresses STAT3 activation by blocking its dimerization nuclear translocation and subsequent transcriptional activity In vitro studies demonstrate Stattic inhibits proliferation in multiple head and neck squamous cell carcinoma (HNSCC) cell lines including UM-SCC-17B OSC-19 Cal33 and UM-SCC-22B with reported IC50 values ranging from approximately 2 3 to 3 5 M Additionally Stattic downregulates STAT3-mediated hypoxia-inducible factor-1 (HIF-1) expression resulting in enhanced radiosensitivity in HNSCC cells and shows activity in mouse xenograft tumor models Therefore Stattic serves as a research tool for investigating STAT3-associated signaling pathways and cancer biology
Apexbio Technology LLC AZD2461 1174043-16-3 10mM (in 1mL DMSO)
AZD2461 (CAS 1174043-16-3) is a novel small-molecule inhibitor of poly(ADP-ribose) polymerase (PARP) exhibiting potency with an IC50 of 5 nM PARP enzymes are pivotal regulators of DNA repair and apoptosis-associated processes In breast cancer cell lines such as SKBR-3 and MCF-7 AZD2461 reduces cell viability in a concentration- and time-dependent manner arresting cells predominantly in the G2 phase In BRCA1-deficient mouse KB1P tumors AZD2461 disrupts PARP activity regardless of P-glycoprotein-mediated resistance to other inhibitors like olaparib highlighting its utility in overcoming drug resistance and elucidating DNA repair pathways in cancer research
Apexbio Technology LLC Calcitriol 32222-06-3 10mM (in 1mL DMSO)
Calcitriol the biologically active metabolite of vitamin D3 functions primarily through interaction with the intracellular vitamin D receptor (VDR) regulating transcription of genes involved in mineral homeostasis and immune responses It modulates cellular differentiation proliferation and adaptive immune functions via nuclear receptor-mediated mechanisms In vitro studies demonstrate that calcitriol dose-dependently inhibits lipopolysaccharide (LPS)-stimulated tumor necrosis factor-alpha (TNF- ) and interleukin-1 (IL-1 ) secretion from human peripheral blood mononuclear cells (PBMCs) Additionally animal models indicate that calcitriol administration decreases cytokine release associated with inflammatory stimuli through intracellular calcium-dependent signaling pathways Calcitriol is widely utilized in biomedical research concerning osteometabolic regulation immune modulation and cytokine signaling networks
Apexbio Technology LLC Birinapant (TL32711) 1260251-31-7 10mM (in 1mL DMSO)
Birinapant (TL32711) is a potent antagonist of XIAP and cIAP proteins binding specifically to their BIR domains with Kd values around 45 nM for XIAP and below 1 nM for cIAP1 By promoting rapid degradation of TRAF2-associated cIAP1 and cIAP2 Birinapant suppresses TNF-induced NF- B signaling and facilitates the assembly of RIPK1-dependent caspase-8 complexes thus initiating downstream apoptosis pathways It has been widely employed in biomedical research to investigate apoptosis mechanisms and tumor resistance In melanoma and breast cancer models Birinapant combined with cytokines such as TNF- led to tumor cell growth suppression and sensitized therapy-resistant cells to apoptosis
Apexbio Technology LLC WZ4003 1214265-58-3 10mM (in 1mL DMSO)
WZ4003 (CAS 1214265-58-3) is a selective inhibitor targeting NUAK1 and NUAK2 kinases members of the AMP-activated protein kinase (AMPK) family activated by tumor suppressor kinase LKB1 WZ4003 inhibits NUAK1 and NUAK2 with IC50 values of 20 nM and 100 nM respectively In cellular assays treatment with WZ4003 reduces NUAK1-mediated phosphorylation of MYPT1 at Ser445 It suppresses cell proliferation migration of mouse embryonic fibroblasts and invasion of U2OS cells Thus WZ4003 serves as a valuable tool for investigating NUAK kinase functions in cell proliferation mobility and signaling mechanisms relevant to oncology research
Apexbio Technology LLC Afatinib (BIBW2992) 439081-18-2 10mM (in 1mL DMSO)
Afatinib (BIBW2992 CAS 439081-18-2) is an irreversible inhibitor targeting receptor tyrosine kinases in the ErbB protein family specifically EGFR (ErbB1) and HER2 (ErbB2) By covalently binding to their kinase domains it suppresses downstream ErbB signaling showing demonstrated inhibition with IC50 values of 0 5 nM for EGFR and 14 nM for HER2 Afatinib blocks EGF-induced phosphorylation and cellular proliferation in multiple EGFR- or HER2-expressing lines including A431 NIH-3T3-HER2 NCI-N87 and BT-474 Research applications include tumor xenograft studies and transgenic lung cancer models evaluating EGFR-dependent oncogenic processes and therapeutic responses
Apexbio Technology LLC SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation
Apexbio Technology LLC Clopidogrel 120202-66-6 10mM (in 1mL DMSO)
Clopidogrel (CAS 120202-66-6) is a selective antagonist targeting the platelet P2Y receptor thereby preventing ADP-mediated platelet activation and aggregation Through this mechanism clopidogrel exhibits pronounced antithrombotic properties reducing thrombus formation It is the pharmacologically active enantiomer derived from racemic ( )-clopidogrel hydrochloride Clopidogrel is widely employed in biomedical research examining platelet function thrombosis pathways and therapeutic interventions targeting cardiovascular disease
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
Apexbio Technology LLC Mesna 19767-45-4 10mM (in 1mL DMSO)
Mesna chemically classified as a sulfhydryl-containing compound functions primarily as a protective adjuvant during chemotherapy with oxazaphosphorine agents (such as cyclophosphamide and ifosfamide) Its mode of action involves direct binding and detoxification of urotoxic metabolites notably acrolein thereby facilitating their conversion into stable non-toxic derivatives and mitigating associated bladder toxicity Due to this detoxifying effect Mesna is widely utilized in oncology research and clinical studies investigating chemotherapy-induced urotoxicity prevention Additionally given its structural feature as a thiol donor Mesna finds applications in experimental studies exploring its antioxidant activity and potential cytoprotective effects
Apexbio Technology LLC R406 841290-81-1 10mM (in 1mL DMSO)
R406 (CAS 841290-81-1) is an orally active inhibitor targeting spleen tyrosine kinase (SYK) a non-receptor tyrosine kinase prominently expressed in hematopoietic cells SYK mediates essential signaling upon activation of immune receptors including Fc and B-cell receptors impacting immune responses platelet activation osteoclast differentiation and vascular development By competitively binding to SYK s ATP-binding pocket R406 disrupts SYK-mediated downstream substrate phosphorylation It potently inhibits IgE- and IgG-induced Fc receptor signaling (IC50 56 64 nM) and blocks SYK-dependent B-cell receptor activation (SYK IC50 41 nM) inducing apoptosis in diffuse large B-cell lymphoma cell lines R406 is utilized in research investigating hematologic malignancies and immune-mediated disorders
Apexbio Technology LLC Temsirolimus 162635-04-3 10mM (in 1mL DMSO)
Temsirolimus (CCI-779) is an ester analog of rapamycin functioning as an inhibitor of the mammalian target of rapamycin (mTOR) The compound suppresses mTOR signaling pathways thus inhibiting cellular proliferation and growth In preclinical studies on breast cancer cell lines Temsirolimus displayed inhibitory activities with reported IC50 values of 0 6 nM in BT-474 cells 0 7 nM in MDA-MB-468 and SKBR-3 cells and 50 nM in MCF-7 cells It has been examined in xenograft models of tumors with PTEN mutations and multiple myeloma for investigating pathways related to cell-cycle progression and proliferation regulated by mTOR
Apexbio Technology LLC AZD6244 (Selumetinib) 606143-52-6 10mM (in 1mL DMSO)
AZD6244 (Selumetinib CAS 606143-52-6) is a small-molecule inhibitor selectively targeting MEK1/2 components of the MAP kinase signaling cascade It inhibits MEK1 via a non-ATP-competitive mechanism with an IC50 of 14 1 nM leading to decreased phosphorylation of downstream targets ERK1/2 (IC50 10 3 nM cellular assays) AZD6244 exhibits minimal off-target activity against related kinases including MKK6 EGFR ErbB2 and B-Raf In tumor cell lines harboring activated Ras or B-Raf mutations AZD6244 reduces cell proliferation and inhibits growth in xenograft models Thus AZD6244 is useful for investigating MAP kinase pathway-driven malignancies
Apexbio Technology LLC Dapivirine (TMC120) 244767-67-7 10mM (in 1mL DMSO)
Dapivirine (TMC120) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting HIV-1 viral replication By binding directly to HIV-1 reverse transcriptase dapivirine inhibits viral RNA-dependent DNA polymerase activity thus blocking viral DNA synthesis Dapivirine demonstrates activity against HIV-1 reverse transcriptase with reported IC50 values in the low nanomolar range (approximately 1-10 nM) Due to its molecular specificity and promising in vitro antiviral profile dapivirine is widely utilized in biomedical research exploring topical prevention strategies particularly in the development of vaginal microbicides aimed at reducing HIV transmission
Apexbio Technology LLC Cilengitide 188968-51-6 10mM (in 1mL DMSO)
Cilengitide (CAS 188968-51-6) is a cyclic RGD pentapeptide [Arg-Gly-Asp-DPhe-(NMeVal)] that acts as an inhibitor of integrins v 3 and v 5 These integrins are transmembrane receptors mediating cellular processes such as adhesion migration angiogenesis and invasion Cilengitide binds directly to v 3 integrin receptors inhibiting integrin-mediated activities with an IC50 of 250 nM In in vitro assays cilengitide dose-dependently reduces proliferation and adhesion of endothelial progenitor cells In vivo studies showed that cilengitide administration significantly lowered osteolytic lesion formation and soft tissue involvement in metastatic MDA-MB-231 tumor models