Dimethyl Sulfoxide
Apexbio Technology LLC G007-LK 1380672-07-0 10mM (in 1mL DMSO)
G007-LK (CAS 1380672-07-0) is a small molecule inhibitor that selectively targets tankyrase 1 and 2 (TNKS1/2) enzymes within the poly(ADP-ribose) polymerase family that modulate protein complexes through ADP-ribosylation G007-LK inhibits TNKS1 and TNKS2 with IC50 values of 46 nM and 25 nM respectively reducing their auto-poly(ADP-ribosylation) activity Treatment with G007-LK decreases -catenin levels in APC-mutated colorectal cancer cells by promoting formation of -catenin degradation complexes In xenograft mouse models using COLO-320DM cells G007-LK administration suppresses tumor growth dose-dependently indicating its utility in oncology research focusing on the Wnt/ -catenin pathway
Apexbio Technology LLC LB42708 226929-39-1 10mM (in 1mL DMSO)
LB42708 (CAS 226929-39-1) is a selective small-molecule inhibitor of farnesyltransferase (FTase) belonging to a non-peptidic pyrrole-based class It blocks FTase-mediated farnesylation of H-Ras N-Ras and K-Ras4B demonstrated by low nanomolar IC50 values (0 8 nM 1 2 nM and 2 nM respectively) LB42708 shows minimal inhibitory effect on geranylgeranyltransferase I In vitro studies indicate inhibition of Ras-driven signaling pathways decreasing Ras activation and subsequently suppressing VEGF-stimulated endothelial proliferation and migration Researchers use LB42708 in oncology and inflammation studies exemplified by reduced tumor growth in Ras-mutant HCT116 and wild-type Caco-2 xenograft models
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 Cobimetinib 934660-93-2 10mM (in 1mL DMSO)
Cobimetinib (CAS 934660-93-2) is a selective small molecule inhibitor targeting mitogen-activated protein kinase kinase (MEK) MEK functions as a kinase that specifically phosphorylates serine/threonine and tyrosine residues playing a critical role in the MAPK signaling cascade and modulating cell proliferation survival migration differentiation and angiogenesis Cobimetinib effectively inhibits MEK with an IC50 value of 0 9 nM demonstrating potent activity in various experimental cancer models including breast cancer cells harboring KRAS and B-RAF mutations In xenograft mouse models it exhibits dose-dependent tumor growth suppression and sustained inhibition of ERK phosphorylation Cobimetinib is currently evaluated in phase I clinical trials as an anticancer therapeutic candidate
Apexbio Technology LLC SB 225002 182498-32-4 10mM (in 1mL DMSO)
SB 225002 (CAS 182498-32-4) is a selective non-peptide antagonist targeting the chemokine receptor CXCR2 a G protein-coupled receptor involved in interleukin-8 (IL-8)-mediated neutrophil chemotaxis and polarization It inhibits IL-8 binding to CXCR2 with an IC50 of 22 nM and displays over 150-fold selectivity against CXCR1 SB 225002 suppresses neutrophil migration and polarization triggered by IL-8 and GRO in cell-based assays and animal models It also promotes apoptosis and mitotic catastrophe in ovarian cancer cells independently of p53 status highlighting its utility in inflammation and oncology research
Apexbio Technology LLC RepSox 446859-33-2 10mM (in 1mL DMSO)
RepSox (CAS 446859-33-2) is a selective small-molecule inhibitor of TGF receptor-1 (TGF R-1) a serine/threonine kinase receptor involved in regulating tumor transformation cell proliferation and differentiation via TGF signaling pathways RepSox inhibits TGF R-1 activity with an IC50 of 23 nM thereby modulating downstream signaling events In cellular studies RepSox facilitated reprogramming of mouse embryonic fibroblasts (MEFs) into induced pluripotent stem cells (iPSCs) by functionally substituting for Sox2 Due to its capacity to significantly alter expression profiles linked to TGF signaling RepSox serves as a useful tool in stem cell research and cellular reprogramming studies
Apexbio Technology LLC RG2833 1215493-56-3 10mM (in 1mL DMSO)
RG2833 (CAS 1215493-56-3) is a small-molecule inhibitor targeting histone deacetylase (HDAC) In neuronal cell models RG2833 elevates frataxin (FXN) mRNA and protein expression by modifying epigenetic regulation at the FXN locus Studies conducted on peripheral blood mononuclear cells (PBMCs) from patients demonstrated reduced HDAC activity enhanced histone H3 lysine 9 acetylation and elevated FXN mRNA levels upon RG2833 treatment Research utilizing induced pluripotent stem cell (iPSC)-derived neuronal cultures further supports HDAC inhibition as the mechanism underlying RG2833-mediated FXN upregulation This molecule is primarily explored for epigenetic studies in Friedreich s ataxia research
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 Elvitegravir (GS-9137) 697761-98-1 10mM (in 1mL DMSO)
Elvitegravir (GS-9137) is an integrase inhibitor targeting HIV-1 which impedes viral DNA integration during the replication cycle of human immunodeficiency virus type 1 (HIV-1) Its mechanism involves inhibition of the integrase enzyme-mediated DNA strand transfer reaction thereby preventing the insertion of viral genetic material into host genomic DNA and subsequently decreasing viral replication Reported inhibitory concentrations (IC50) against HIV-1 integrase range approximately from 7 to 8 nM Besides its application in HIV-1 research Elvitegravir demonstrates inhibitory effects against other retroviral integrases such as murine leukemia virus (MLV) and simian immunodeficiency virus (SIV) making it suitable for broader antiviral research use
Apexbio Technology LLC Erlotinib 183321-74-6 10mM (in 1mL DMSO)
Erlotinib (CAS 183321-74-6) is an orally bioavailable reversible inhibitor targeting the epidermal growth factor receptor (EGFR) tyrosine kinase It acts by competitively binding the intracellular ATP-binding domain of EGFR thereby preventing receptor autophosphorylation and subsequent signaling cascades involved in proliferation angiogenesis and cell survival In biochemical assays Erlotinib demonstrates potent inhibition of EGFR tyrosine kinase (IC50 2 nmol/L) and cellular autophosphorylation of EGFR (IC50 20 nmol/L) Due to its selective interference with EGFR-mediated signaling Erlotinib is extensively employed in oncology research particularly in studies on EGFR-expressing tumor models
Apexbio Technology LLC GSK343 1346704-33-3 10mM (in 1mL DMSO)
GSK343 (CAS 1346704-33-3) is a selective SAM-competitive inhibitor targeting the histone lysine methyltransferase EZH2 which is the catalytic component of polycomb repressive complex 2 (PRC2) responsible for trimethylation of histone H3 at lysine 27 (H3K27me3) By competitively inhibiting EZH2 s methyltransferase activity GSK343 disrupts H3K27me3-mediated transcriptional silencing It shows potent inhibitory activity against EZH2 (IC50 4 nM) moderate inhibition against EZH1 (240 nM) but minimal impact on other SAM-dependent enzymes In vitro studies with various cancer cell models confirm its ability to reduce H3K27 trimethylation limit proliferation induce apoptosis promote autophagy and enhance chemosensitivity highlighting its utility as a research tool to study EZH2-related mechanisms
Apexbio Technology LLC Fenretinide 65646-68-6 10mM (in 1mL DMSO)
Fenretinide (4-HPR) is a synthetic retinoic acid analog which acts primarily through inhibition of focal adhesion kinase (FAK) and modulation of related signaling cascades Fenretinide induces apoptosis in various tumor cell lines such as prostate ovarian cervical endometrial breast small-cell lung carcinoma and malignant hematopoietic cells Mechanistically Fenretinide promotes apoptotic cell death through reactive oxygen species (ROS)-mediated DNA fragmentation and disrupts tumor cell migration and invasion via interference with the FAK/AKT/GSK3 signaling axis and destabilization of -catenin Fenretinide is frequently utilized as a chemopreventive agent in oncology research particularly for investigating mechanisms of growth inhibition and cell migration suppression
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 Doxercalciferol 54573-75-0 10mM (in 1mL DMSO)
Doxercalciferol chemically known as 1 -Hydroxyvitamin D2 is a synthetic analog of vitamin D2 characterized by selective activation of the vitamin D receptor (VDR) Upon metabolic activation Doxercalciferol undergoes hepatic transformation to its biologically active form inducing gene transcription mediated via the VDR signaling pathway Central to its mechanism activated VDR regulates calcium and phosphate homeostasis influencing cellular differentiation proliferation and parathyroid hormone expression In biomedical research Doxercalciferol serves as a tool compound to investigate the molecular pathways regulated by vitamin D receptor activation particularly in renal insufficiency models bone metabolism studies and parathyroid physiology experiments
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