Dimethyl Sulfoxide
Apexbio Technology LLC PP 2 (AG 1879) 172889-27-9 10mM (in 1mL DMSO)
PP 2 (AG 1879 CAS 172889-27-9) is a selective inhibitor targeting Src family tyrosine kinases such as Lck and Fyn with reported IC50 values of approximately 4 nM and 5 nM respectively Src family kinases are composed of nine closely related tyrosine kinases including Src Yes Fyn Fgr Yrk Lyn Blk Hck and Lck PP 2 suppresses early T-cell signaling by blocking Lck- and Fyn-mediated tyrosine phosphorylation following anti-CD3 stimulation Research in glioma cell models (U251) has demonstrated PP 2-mediated inhibition of Src-dependent cellular invasion and proliferation at micromolar concentrations PP 2 exhibits moderate inhibitory activity toward EGF-R (IC50 480 nM) and minimal effect on ZAP-70 and JAK2 Thus PP 2 serves as a research tool for studying Src kinase-dependent signaling pathways implicated in cancer and immunological responses
Apexbio Technology LLC BML-210(CAY10433) 537034-17-6 10mM (in 1mL DMSO)
BML-210 (CAY10433 CAS 537034-17-6) is a small molecule inhibitor targeting histone deacetylases (HDACs) enzymes responsible for removing acetyl groups from lysine residues on histone proteins leading to chromatin compaction and transcriptional repression BML-210 demonstrates HDAC inhibitory activity with an IC50 of 87 M In cellular assays this compound increases FXN mRNA expression and histone H4 acetylation induces G1 cell cycle arrest and apoptosis and enhances erythroid and granulocytic differentiation in human leukemia cell lines (K562 HL-60) BML-210 is utilized in research investigating epigenetic modulation leukemia biology and gene regulation mechanisms
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 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 CB-5083 1542705-92-9 10mM (in 1mL DMSO)
CB-5083 (CAS 1542705-92-9) is an orally bioavailable small-molecule inhibitor targeting the AAA ATPase p97 (also termed valosin-containing protein VCP) P97 functions in diverse cellular processes related to protein homeostasis including membrane fusion intracellular trafficking and degradation pathways CB-5083 selectively inhibits the second ATPase domain of p97 (IC50 15 4 nM) promoting cytoplasmic protein degradation and triggering apoptosis in cultured cancer cell lines such as A549 and HCT116 In vivo orally administered CB-5083 demonstrates significant reduction of tumor growth in xenograft models The compound is being investigated clinically for treatment of solid tumors and multiple myeloma
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 CCT128930 HCl 885499-61-6 (free base) 10mM (in 1mL DMSO)
CCT128930 HCl is a potent selective ATP-competitive inhibitor targeting AKT2 kinase with an IC50 of approximately 6 nM It exhibits higher selectivity for AKT2 compared to related kinases such as PKA and p70S6K Akt protein kinase involved in diverse cellular pathways including metabolism proliferation apoptosis transcription control and cell mobility is frequently deregulated in various tumor types In cancer cell models CCT128930 HCl impairs cellular proliferation and reduces phosphorylation of specific Akt downstream substrates Preclinical studies employing PTEN-deficient glioma cells and breast cancer xenograft models show inhibition of signaling activity and tumor growth Consequently CCT128930 HCl serves as a promising research tool for studying Akt-mediated signaling mechanisms pathway regulation and potential therapeutic responses in cancer biology
Apexbio Technology LLC (+)-MK 801(Synonyms: Dizocilpine, Dizocilpine maleate, MK-801, (+)-MK-801, (+)-Dizocilpine), 10mM (in 1mL DMSO), CAS: 70449-94-4.
( )-MK 801 (CAS 70449-94-4) is a potent selective and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor displaying a Ki of approximately 30 5 nM This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes predominantly localized within the hippocampus In vitro assays utilizing rat cortical slice preparations indicate that ( )-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents Due to these pharmacological properties ( )-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events neurotoxicity convulsions and excitatory neurotransmission pathways
Apexbio Technology LLC Ticagrelor 274693-27-5 10mM (in 1mL DMSO)
Ticagrelor (CAS 274693-27-5) is an orally active reversible antagonist targeting the platelet P2Y12 receptor By competitively binding to P2Y12 ticagrelor inhibits ADP-mediated platelet aggregation resulting in dose-dependent suppression of platelet activation and thrombosis in vitro Unlike other P2Y12 inhibitors requiring metabolic activation ticagrelor acts without metabolic transformation though it is primarily metabolized by CYP3A4 and CYP2C19 enzymes This compound is frequently employed in biomedical research exploring platelet function thrombosis mechanisms and drug-drug interactions involving cytochrome P450 enzymes
Apexbio Technology LLC GDC-0068 (RG7440) 1001264-89-6 10mM (in 1mL DMSO)
GDC-0068 (RG7440 CAS number 1001264-89-6) is a selective small-molecule inhibitor targeting Akt isoforms Akt1 Akt2 and Akt3 It inhibits Akt activity with IC50 values of 5 nM 18 nM and 8 nM for Akt1 Akt2 and Akt3 respectively Akt signaling within the PI3K-Akt pathway regulates cellular proliferation survival and tumorigenesis and is frequently dysregulated in cancers harboring mutations in PTEN or PI3K GDC-0068 binds to and inhibits Akt activation resulting in reduced tumor cell proliferation cell-cycle arrest and induction of apoptosis supporting its utility in oncology research
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 JIB-04 199596-05-9 10mM (in 1mL DMSO)
JIB-04 (CAS 199596-05-9) is a selective small-molecule inhibitor targeting Jumonji histone demethylases specifically suppressing enzymes including JARID1A JMJD2 family members (JMJD2A-E) and JMJD3 Structurally categorized as a pyridine hydrazone derivative JIB-04 inhibits demethylase activity independently of competitive binding with -ketoglutarate In vitro assays revealed IC50 values ranging from 230 nM to 1100 nM across various Jumonji enzymes Additionally JIB-04 demonstrates preferential inhibition of cancer cell proliferation versus normal cells notably in lung and prostate cancer cell lines and effectively reduces tumor growth in mouse xenograft models highlighting its relevance for cancer research