Dimethyl Sulfoxide
Apexbio Technology LLC Pioglitazone(Synonyms: Actos, Pioglitazone Hydrochloride, AD-4833, U-72107, Glustin, Zactos, Piozone), 10mM (in 1mL DMSO), CAS: 111025-46-8.
Pioglitazone (CAS 111025-46-8) is a small-molecule agonist selectively targeting peroxisome proliferator-activated receptor gamma (PPAR ) By activating this nuclear receptor pioglitazone influences gene expression pathways involved primarily in glucose and lipid metabolism insulin sensitivity and adipocyte differentiation It is widely employed in biomedical research focusing on metabolic disorders including type 2 diabetes mellitus insulin resistance mechanisms and associated inflammatory processes
Apexbio Technology LLC GMX1778 (CHS828) 200484-11-3 10mM (in 1mL DMSO)
GMX1778 (CHS828 CAS 200484-11-3) is a small-molecule inhibitor targeting nicotinamide phosphoribosyltransferase (NAMPT) an enzyme crucial for NAD biosynthesis with a reported Kd value of 120 nM NAD functions as a cofactor essential for enzymatic oxidation-reduction processes and diverse cellular events including metabolism genomic integrity calcium signaling aging and apoptosis In cultured IM-9 cells exposure to GMX1778 substantially decreases NAD and NM levels in a time-dependent manner GMX1778 displays anti-tumor activity preferentially in NAPRT1-deficient cancer models highlighting its potential utility for investigating metabolic vulnerabilities and targeted cancer therapies
Apexbio Technology LLC AT9283 896466-04-9 10mM (in 1mL DMSO)
AT9283 (CAS 896466-04-9) is a synthetic small-molecule inhibitor developed through fragment-based drug design It inhibits Aurora kinases A and B key components of the serine/threonine kinase family involved in regulating cell division processes as well as targets including Janus kinases (JAKs) BCR-ABL kinase (including the T315I mutant) and Flt-3 With a potent IC50 around 3 nM against Aurora kinases AT9283 exhibits antiproliferative and pro-apoptotic activity in leukemia myeloproliferative diseases solid tumors and B-cell lymphoma models It is utilized primarily in cancer biology research to investigate its therapeutic potential targeting aberrant kinase activity
Apexbio Technology LLC PCI-24781 (CRA-024781) 783355-60-2 10mM (in 1mL DMSO)
PCI-24781 (CRA-024781 CAS 783355-60-2) is a histone deacetylase (HDAC) inhibitor targeting HDAC1 HDAC2 HDAC3 HDAC6 HDAC8 and HDAC10 with reported Ki values of 7 19 8 2 17 280 and 24 nM respectively HDAC enzymes catalyze the removal of acetyl groups from lysine residues on histone proteins thereby regulating chromatin structure and gene expression PCI-24781 induces dose-dependent hyperacetylation of histones and tubulin in human cancer cells (HCT116 DLD-1) leading to apoptosis via p21 upregulation PARP cleavage and H2AX accumulation PCI-24781 demonstrates antitumor activity against multiple tumor cell lines and in xenograft models highlighting its utility for oncology research
Apexbio Technology LLC TG003 300801-52-9 10mM (in 1mL DMSO)
TG003 (CAS 300801-52-9) is a selective inhibitor targeting the Cdc2-like kinase (Clk) family and casein kinase 1 (CK1) Specifically it demonstrates notable potency against mClk1 mClk2 and mClk4 with IC50 values of approximately 20 nM 200 nM and 15 nM respectively TG003 competitively binds with ATP at Clk1 modulating Clk-mediated phosphorylation of serine/arginine-rich (SR) proteins involved in alternative mRNA splicing Studies using HeLa cellular extracts and animal models have shown that TG003 alters splice site selection and pre-mRNA processing suggesting potential utility for investigating RNA splicing regulatory mechanisms
Apexbio Technology LLC Cyclophosphamide monohydrate 6055-19-2 10mM (in 1mL DMSO)
Cyclophosphamide monohydrate is an alkylating cytotoxic agent exhibiting antitumor activity primarily via metabolic activation As a prodrug it undergoes hepatic biotransformation mediated by cytochrome P450 enzymes forming active alkylating metabolites such as 4-hydroxycyclophosphamide which exert cytotoxic effects through interactions with cellular DNA Cyclophosphamide also reversibly inhibits acetylcholinesterase (AChE) displaying an IC50 of approximately 511 M It is widely utilized in experimental cancer studies particularly in pediatric oncology where alterations in drug metabolism or drug-drug interactions impacting cyclophosphamide clearance and therapeutic outcomes have been explored
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC Santacruzamate A (CAY10683) 1477949-42-0 10mM (in 1mL DMSO)
Santacruzamate A (CAY10683 CAS 1477949-42-0) is a selective histone deacetylase (HDAC) inhibitor originally identified in the marine cyanobacterium cf Symploca sp Its mechanism of action involves targeting HDAC enzymes particularly demonstrating high selectivity towards HDAC2 (IC 0 112 nM) when compared with HDAC6 (IC 433 nM) and minimal potency against HDAC4 (IC 1 M) In cellular assays Santacruzamate A reduces growth of tumor cell lines such as HCT-116 colon cancer cells (GI 28 M) and HuT-78 cutaneous T-cell lymphoma cells (GI 1 3 M) It is valuable in epigenetics and oncology research for selectively modulating HDAC2 activity
Apexbio Technology LLC Pexidartinib (PLX3397) 1029044-16-3 10mM (in 1mL DMSO)
Pexidartinib (PLX3397 CAS 1029044-16-3) is a small molecule inhibitor targeting colony-stimulating factor 1 receptor (CSF-1R) a receptor tyrosine kinase involved in macrophage recruitment and activation Through inhibition of CSF-1R activity this compound reduces macrophage infiltration and accumulation demonstrated by diminished macrophage levels in B16F10 melanoma models without affecting Gr-1 myeloid-derived suppressor cells In vivo studies using GL261 glioma models in C57 mice indicate decreased microglial infiltration upon oral dosing with PLX3397 Clinically combined treatment with Pexidartinib and paclitaxel is under evaluation in advanced solid tumors and breast cancer trials
Apexbio Technology LLC Trichostatin A (TSA) 58880-19-6 10mM (in 1mL DMSO)
Trichostatin A (TSA CAS 58880-19-6) is a histone deacetylase (HDAC) inhibitor and antifungal antibiotic isolated from microbial sources TSA acts by reversibly inhibiting HDAC enzymes in a noncompetitive manner leading to increased acetylation of histones particularly histone H4 In mammalian cell cultures TSA treatment results in G1 and G2 phase arrest induction of differentiation and reversion of transformed cellular phenotypes In human breast cancer cell lines TSA inhibits proliferation (IC50 124 4 120 4 nM) and induces hyperacetylation of histone proteins highlighting its utility as a tool compound for investigating epigenetic regulation and oncology-related mechanisms
Apexbio Technology LLC Panobinostat (LBH589) 404950-80-7 10mM (in 1mL DMSO)
Panobinostat (LBH589) is a histone deacetylase (HDAC) inhibitor targeting class I II and IV HDAC enzymes regulating gene expression through histone hyperacetylation In vitro studies indicate panobinostat induces apoptosis and growth arrest in Ph-negative acute lymphoblastic leukemia (ALL) cell lines T-cell (MOLT-4) and pre-B cell (Reh) via caspase activation PARP cleavage and downregulation of c-Myc accompanied by H3K9 and H4K8 hyperacetylation and elevation of cell-cycle regulators (p21 p27) Panobinostat has shown anti-proliferative effects in various cancer models including cutaneous T-cell lymphoma and multiple myeloma (IC50 5-30 nM) and serves as a research tool in studies assessing epigenetic regulation and tumor biology
Apexbio Technology LLC SU11274 658084-23-2 10mM (in 1mL DMSO)
SU11274 (CAS 658084-23-2) is a selective inhibitor targeting Met kinase exhibiting an IC50 of approximately 10 nM The compound specifically suppresses the autophosphorylation of Met at residues Tyr1234/1235 disrupting receptor activity with minimal effects on other receptor tyrosine kinases such as EGFR and PDGFR or serine/threonine kinases including CDK2 In NIH3T3 cells expressing drug-sensitive or resistant MET mutants and in H1993 human lung cancer cells treatment with SU11274 induces a dose-dependent inhibition of Met phosphorylation and impairs receptor ubiquitination leading to receptor accumulation SU11274 serves as a useful tool for investigating Met signaling pathways in oncology research
Apexbio Technology LLC Azacyclonol 115-46-8 10mM (in 1mL DMSO)
Azacyclonol (CAS 115-46-8) chemically referred to as -pipradol is a small molecule utilized primarily in neuropharmacological research due to its antipsychotic properties Although the precise molecular mechanism remains incompletely defined Azacyclonol is understood to modulate central neurotransmitter systems influencing pathways associated with psychosis Studies have demonstrated its capacity to reduce hallucinations and mitigate psychotic symptoms positioning it as a valuable investigational tool in psychiatric research and therapeutic exploration of psychosis-related disorders
Apexbio Technology LLC OTX-015 202590-98-5 10mM (in 1mL DMSO)
OTX-015 (CAS 202590-98-5) is a selective inhibitor of BRD2 BRD3 and BRD4 proteins within the BET (bromodomain and extra-terminal) family involved in transcriptional regulation By disrupting the interaction between these BRD proteins and acetylated histone H4 OTX-015 exhibits inhibitory activity demonstrated by IC50 values between 92 and 112 nM and in vitro EC50 ranging from 10 to 19 nM OTX-015 treatment reduces proliferation (GI50 60 200 nM) induces G1 arrest and promotes apoptosis in various human cancer cell models In xenograft mouse studies of BRD-NUT midline carcinoma orally administered OTX-015 significantly suppresses tumor growth showing potential utility for cancer research