Dimethyl Sulfoxide
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
Cayman Chemical L-MethIonIn SulfoxIde 10g
A sulfoxide-modified methionine; increases weight gain in weanling mice in the diet at 6.3, 12.6, and 18.9 mmol/g; levels are decreased in patients with vitiligo
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 MRT67307 HCl 2095432-39-4 10mM (in 1mL DMSO)
MRT67307 HCl (CAS 2095432-39-4) is a small-molecule inhibitor targeting several kinases including TBK1 IKK MARK1-4 NUAK1 ULK1/2 and salt-inducible kinases (SIK1-3) It inhibits TBK1 and IKK to block phosphorylation of IRF3 reducing interferon- synthesis without affecting NF- B activation Additionally MRT67307-mediated SIK inhibition promotes regulatory macrophage differentiation leading to elevated anti-inflammatory cytokines (e g IL-10 IL-1ra) and decreased pro-inflammatory cytokines (IL-6 IL-12 TNF) It is utilized to investigate innate immunity macrophage polarization autophagy and inflammation pathways
Apexbio Technology LLC SAG(Synonyms: Smoothened Agonist, SAG dihydrochloride, Hh-Smo agonist, SAG hydrochloride), 10mM (in 1mL DMSO), CAS: 912545-86-9.
SAG (CAS 912545-86-9) is a synthetic small-molecule agonist targeting the Smoothened (SMO) receptor a GPCR-like protein central to the Hedgehog (Hh) signaling pathway It activates SMO with an EC50 of approximately 3 nM thus stimulating downstream Gli transcription factor activity involved in embryonic development and adult tissue homeostasis At concentrations above 1 M SAG exhibits inhibitory effects on pathway signaling It binds directly to SMO forming an interaction with a reported dissociation constant (K D) around 59 nM SAG is employed in biomedical research notably to mitigate glucocorticoid-induced cerebellar injury in primary mouse neuronal cell cultures
Apexbio Technology LLC EPZ-6438 1403254-99-8 10mM (in 1mL DMSO)
EPZ-6438 is a selective inhibitor targeting EZH2 the catalytic subunit of polycomb repressive complex 2 (PRC2) By competitively binding to EZH2 s S-adenosylmethionine (SAM) pocket EPZ-6438 suppresses EZH2-driven trimethylation of histone H3 lysine 27 (H3K27me3) a key epigenetic modification implicated in transcriptional regulation and oncogenesis This selective inhibition of EZH2 exhibits reduced affinity for EZH1 In biological studies EPZ-6438 has demonstrated anti-tumor activity in preclinical malignant rhabdoid tumor models making it useful for examining EZH2-dependent cancer pathways and epigenetic research
Apexbio Technology LLC Fosaprepitant(Synonyms: Fosaprepitant dimeglumine, Emend IV, L-758298, MK-0517, Fosaprepitant meglumine, Ivemend), 10mM (in 1mL DMSO), CAS: 172673-20-0.
Fosaprepitant (CAS 172673-20-0) also known as MK-0517 or L-758 298 is a selective neurokinin-1 (NK-1) receptor antagonist exerting its pharmacological effects primarily through its active metabolite aprepitant This antagonism blocks substance P-mediated biological effects including vomiting responses In established preclinical models such as the cisplatin-triggered emesis in ferrets fosaprepitant demonstrated activity in mitigating chemotherapy-induced vomiting Given aprepitant s favorable penetration into the central nervous system fosaprepitant exhibits high NK-1 receptor affinity and potentiates antiemetic actions of agents such as dexamethasone and granisetron It is used in combination therapies with 5-HT3 antagonists and corticosteroids for chemotherapy-induced nausea and vomiting (CINV)
Apexbio Technology LLC RK-33 1070773-09-9 10mM (in 1mL DMSO)
RK-33 is a small molecule inhibitor targeting DDX3 an RNA helicase frequently overexpressed in various cancer types including lung cancer DDX3 overexpression correlates with poorer survival outcomes in lung cancer patients suggesting therapeutic relevance Mechanistically RK-33 inhibits DDX3 enzymatic activity thereby disrupting downstream signaling pathways particularly the -catenin-dependent Wnt signaling axis In vitro studies indicate RK-33 induces cell cycle arrest at G1 phase promotes apoptosis and enhances cellular radiosensitivity in DDX3-high expressing cell lines (e g A549 H1299 H23 and H460 IC50 4 4 8 4 M) In preclinical in vivo testing using a Twist1/KrasG12D mouse lung cancer model combined treatment of RK-33 with radiation resulted in reduced tumor growth compared with radiation alone RK-33 serves as a research tool to investigate DDX3 biology and potential therapeutic strategies for cancers with elevated DDX3 expression
Apexbio Technology LLC LY2228820 862507-23-1 10mM (in 1mL DMSO)
LY2228820 (CAS 862507-23-1) is a potent selective ATP-competitive small-molecule inhibitor targeting the and isoforms of p38 mitogen-activated protein kinase (MAPK) with reported IC50 values of 5 3 nM and 3 2 nM respectively By suppressing p38 MAPK signaling LY2228820 decreases phosphorylation of heat shock protein 27 (HSP27) induced by Bortezomib thereby elevating cytotoxic effects in multiple myeloma (MM) models Additionally it inhibits secretion of IL-6 by bone marrow mononuclear cells and stromal cells as well as secretion of MIP-1 by patient-derived MM cell subsets and osteoclast precursors In melanoma (B16-F10) and NSCLC (A549) xenograft murine models LY2228820 reduces phosphorylation of MK2 and slows tumor progression respectively highlighting its potential utility in oncology research
Apexbio Technology LLC Micafungin sodium 208538-73-2 10mM (in 1mL DMSO)
Micafungin sodium is an antifungal agent that acts by inhibiting the synthesis of 1 3- -D-glucan an essential polymer for fungal cell wall integrity particularly in Candida albicans In addition to antifungal activities micafungin has been studied for its capacity to suppress biofilm formation by Pseudomonas aeruginosa via downregulation of genes encoding structural biofilm elements such as algC and pelC and the 1 3- -D-glucan-encoding gene ndvB Micafungin has demonstrated synergy with other antifungal compounds in animal models in murine models of systemic Aspergillus fumigatus infection micafungin administration resulted in increased survival rates Micafungin is utilized in biomedical research to investigate antifungal mechanisms combination therapies and inhibition of pathogen biofilms Reported inhibitory activity (IC50) for fungal glucan synthase typically falls within the nanomolar range
Apexbio Technology LLC PD 173074 219580-11-7 10mM (in 1mL DMSO)
PD 173074 (CAS 219580-11-7) is a selective inhibitor targeting fibroblast growth factor receptors (FGFR) exerting its effects by suppressing FGFR tyrosine kinase phosphorylation It has demonstrated dose-dependent inhibitory activity against small cell lung cancer (SCLC) cell lines including H-510 and H-69 by reducing their proliferation colony formation and FGF-2 induced chemotherapy resistance in vitro In murine xenograft models of SCLC PD 173074 reduced tumor progression and significantly prolonged animal survival achieving durable complete responses in some cases PD 173074 represents an important tool compound for investigating the oncogenic role of FGFR signaling in cancer research