Dimethyl Sulfoxide
Apexbio Technology LLC ML347 1062368-49-3 10mM (in 1mL DMSO)
ML347 (CAS 1062368-49-3) is a potent and selective inhibitor of bone morphogenetic protein (BMP) type I receptors specifically targeting ALK2 Mechanistically ML347 selectively inhibits ALK2 kinase activity with an IC50 of 32 nM while also inhibiting ALK1 with a comparable IC50 of 46 nM Notably ML347 displays approximately 300-fold selectivity for ALK2 over ALK3 and lacks inhibitory activity against closely related kinases such as ALK6 and KDR In the BMP4-induced C2C12BRA cell-based assay ML347 exhibits inhibitory activity with an IC50 of 152 nM As a selective ALK2 inhibitor ML347 serves as a valuable probe in BMP pathway research
Apexbio Technology LLC Influenza Hemagglutinin (HA) Peptide 92000-76-5 10mM (in 1mL DMSO)
Influenza hemagglutinin (HA) peptide (sequence YPYDVPDYA) is commonly utilized in biomedical studies as an epitope tag for protein detection and isolation Derived from the influenza virus hemagglutinin protein HA mediates viral entry into host cells through initial receptor binding (via HA1 subunit) and subsequent membrane fusion (via HA2 subunit) Under acidic intracellular conditions HA undergoes conformational changes enabling membrane destabilization and viral fusion Synthetic HA-derived peptides can mimic this fusogenic mechanism enhancing gene transfer efficiency in vitro through promoting cellular uptake of transfection complexes in various cultured cell lines including K562 HeLa and BNL CL 2 hepatocyte cells Typically employed within transferrin-polylysine-DNA based delivery systems these HA peptides facilitate membrane disruption increasing complex internalization reported IC50 values vary depending on specific cellular systems and experimental conditions
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 CEP-18770 847499-27-8 10mM (in 1mL DMSO)
CEP-18770 (CAS 847499-27-8) is a reversible boronic acid-based inhibitor of proteasome chymotrypsin-like activity It specifically targets the proteasome s P2 threonine protease subunit reducing NF- B signaling and the expression of downstream effectors With a reported IC50 of 3 8 nM CEP-18770 induces apoptosis in multiple myeloma cell lines and inhibits osteoclastogenesis and angiogenesis via suppression of RANKL signaling Research supports its potential use in oncology particularly for multiple myeloma showing selective cytotoxicity sparing normal epithelial and bone marrow-derived cells
Apexbio Technology LLC ML-323(Synonyms: ML323, ML 323, USP1 inhibitor ML323, ML-323 USP1-UAF1 inhibitor, USP1/UAF1 inhibitor ML323), 10mM (in 1mL DMSO), CAS: 1572414-83-5.
ML-323 (CAS 1572414-83-5) is a small molecule inhibitor selectively targeting the USP1-UAF1 deubiquitinase complex with a reported IC50 of 76 nM USP1-UAF1 participates in DNA damage response pathways by regulating ubiquitination status of proteins such as PCNA and FANCD2 In cellular assays ML-323 inhibits USP1 UAF1-mediated deubiquitination enhancing cisplatin-induced cytotoxicity in human NSCLC (H596) and osteosarcoma (U2OS) cells The molecule shows minimal cytotoxicity alone and exhibits high selectivity over other human DUBs and protease families providing a valuable research tool for DNA repair and cancer biology studies
Apexbio Technology LLC Bay 11-7085(Synonyms: BAY-11-7085, BAY 117085, BAY117085, Bay11-7085, BAY 11 7085, BAY-117085, Bay 11 7085), 10mM (in 1mL DMSO), CAS: 196309-76-9.
Bay 11-7085 (CAS 196309-76-9) is a soluble inhibitor of nuclear factor-kappa B (NF- B) activation It inhibits cell proliferation and promotes apoptosis in various cell types through interference with NF- B signaling pathways Studies have demonstrated that Bay 11-7085 decreases DNA synthesis in endometriotic stromal cells (ECSCs) leading to cell cycle arrest at G0/G1 phase Furthermore treatment with Bay 11-7085 induces apoptosis by downregulating anti-apoptotic proteins such as Bcl-2 and Bcl-XL while enhancing activation of caspase-3 caspase-8 and caspase-9 Bay 11-7085 is commonly employed as a chemical probe in biomedical research on inflammation and apoptosis pathways
Apexbio Technology LLC Linsitinib(Synonyms: OSI-906, ASP7487, IGF-1R inhibitor OSI-906, IGF-1R/IR inhibitor OSI-906, OSI906), 10mM (in 1mL DMSO), CAS: 867160-71-2.
Linsitinib (CAS 867160-71-2) also known as OSI-906 is a small-molecule inhibitor targeting both insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) kinases It exhibits potent inhibitory effects with IC50 values of 75 nM against IR and 35 nM against IGF-1R In vitro studies using the 3T3/hulGF-1R (LISN) cell line demonstrate that Linsitinib inhibits IGF-1R ligand-dependent autophosphorylation and downstream signaling via pERK1/2 pAKT and p-p70S6K It shows antiproliferative activity across multiple cancer cell lines and exhibits dose-dependent tumor growth inhibition in LISN xenograft animal models supporting its utility in oncology research
Apexbio Technology LLC Go 6983(Synonyms: GO-6983, GO6983, PKC Inhibitor GO 6983, Pan-PKC Inhibitor GO-6983, PKC inhibitor GO6983, 133053-19-7), 10mM (in 1mL DMSO), CAS: 133053-19-7.
Go 6983 (CAS 133053-19-7) is a selective inhibitor of protein kinase C isoforms PKC PKC PKC PKC and PKC with reported IC50 values of approximately 7 nM 7 nM 6 nM 10 nM and 20 mM respectively Protein kinase C (PKC) isoforms act as receptors for tumor-promoting phorbol ester mediating various downstream cellular functions In cancer cell models Go 6983 suppresses PKC and PKC activation induced by phorbol esters and reduces PKC expression inhibiting cell survival pathways It is frequently employed in biomedical studies examining PKC-dependent signaling in cancer progression and epithelial-to-mesenchymal transition (EMT)
Apexbio Technology LLC ARN-509 956104-40-8 10mM (in 1mL DMSO)
ARN-509 is a synthetic biaryl thiohydantoin derivative acting as a competitive inhibitor of the androgen receptor (AR) It binds AR with an IC50 of approximately 16 nmol/L blocking receptor-mediated signaling pathways implicated in prostate cell proliferation Androgen receptor is a nuclear hormone receptor crucial for male sexual differentiation and prostate cancer cell growth Overexpression or hyperactivation of AR frequently occurs in castration-resistant prostate cancer Experimental data indicate that ARN-509 treatment reduces AR-driven transcription and inhibits cell proliferation in prostate cancer cell lines such as LNCaP and VCaP In murine xenograft models oral dosing of ARN-509 diminishes androgen-dependent reporter gene activity reduces tumor cell proliferation and induces apoptosis ARN-509 is utilized in biomedical research to investigate AR signaling and prostate cancer therapeutics
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 Ferrostatin-1 (Fer-1) 347174-05-4 10mM (in 1mL DMSO)
Ferrostatin-1 (Fer-1) is a selective inhibitor of ferroptosis a regulated form of iron-dependent oxidative cell death characterized by lipid peroxidation It functions primarily by reducing lipid reactive oxygen species (ROS) thus inhibiting membrane lipid peroxidation and preventing ferroptosis induction triggered by compounds such as erastin In experimental contexts Fer-1 is employed to investigate ferroptotic pathways in different disease models including cancer biology neurodegeneration and ischemic injury Ferrostatin-1 demonstrates an IC50 value of approximately 60 nM in inhibiting ferroptosis induced by erastin in cellular assays rendering it suitable for mechanistic studies and therapeutic research involving modulation of iron-dependent oxidative damage pathways
Apexbio Technology LLC CUDC-101 1012054-59-9 10mM (in 1mL DMSO)
CUDC-101 (CAS 1012054-59-9) is a multitargeted small molecule inhibitor that concurrently targets epidermal growth factor receptor (EGFR) HER2 and class I and II histone deacetylases (HDACs) By inhibiting EGFR and HER2 kinases directly and simultaneously blocking HDAC activity CUDC-101 downregulates multiple oncogenic signaling pathways including those mediated by Akt HER3 and MET Preclinical assessments demonstrate that CUDC-101 inhibits growth of diverse tumor cell lines and xenograft models notably including those resistant to EGFR-targeted agents such as lapatinib and erlotinib These characteristics render CUDC-101 valuable for oncology research and drug resistance studies
Apexbio Technology LLC TAK-242 243984-11-4 10mM (in 1mL DMSO)
TAK-242 (CAS 243984-11-4) also known as resatorvid is a cyclohexene derivative that functions as a selective inhibitor of Toll-like receptor 4 (TLR4) signaling Mechanistically TAK-242 binds specifically to the intracellular domain of TLR4 disrupting its interaction with downstream adaptor proteins and thus suppressing activation of inflammatory signal pathways triggered by lipopolysaccharide (LPS) In vitro TAK-242 inhibits LPS-induced production of nitric oxide TNF- and interleukin-6 in macrophages (IC50 1 1 11 nM) Preclinical animal models indicate its potential usefulness in mitigating inflammatory responses associated with neuropsychiatric conditions triggered by stress
Apexbio Technology LLC Bromodomain Inhibitor, (+)-JQ1 1268524-70-4 10mM (in 1mL DMSO)
( )-JQ1 is a selective small-molecule inhibitor targeting BET (bromodomain and extraterminal) protein family members particularly BRD4 It competitively binds the acetyl-lysine recognition domain of BRD4 bromodomains 1 and 2 with reported Kd values of approximately 50 nM and 90 nM respectively By selectively inhibiting BET proteins ( )-JQ1 disrupts transcriptional regulatory processes essential in cancer biology rendering it a useful research tool for examining chromatin remodeling and gene expression patterns associated with tumor pathogenesis Additionally ( )-JQ1 specifically targets the testis-specific bromodomain protein BRDT enabling investigations into male reproductive biology by reversibly impairing spermatogenesis
Apexbio Technology LLC INCB28060 1029712-80-8 10mM (in 1mL DMSO)
INCB28060 (CAS 1029712-80-8) also known as Capmatinib or INC280 is an ATP-competitive inhibitor of the receptor tyrosine kinase c-Met (HGFR) This receptor plays essential roles in cellular processes including embryogenesis healing proliferation invasion and angiogenesis and is frequently overexpressed or mutated in cancers INCB28060 blocks c-Met phosphorylation and downstream signaling exhibiting an IC50 of 0 13 nM In preclinical studies it suppresses proliferation in cancer cell lines (e g SNU-5 S114) and inhibits migration in U-87MG and H441 cells In mouse tumor models oral administration reduces c-Met activation and tumor progression INCB28060 serves as a tool compound for investigating c-Met function in cancer research