Dimethyl Sulfoxide
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 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 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 Phenacetin 62-44-2 10mM (in 1mL DMSO)
Phenacetin (CAS 62-44-2) is a synthetic non-opioid analgesic historically utilized for alleviating pain and reducing fever lacking intrinsic anti-inflammatory effects Its analgesic mechanism primarily involves inhibition of cyclooxygenase (COX) enzyme activity in the central nervous system leading to decreased prostaglandin synthesis Previously studied for its pharmacological action on pain modulation pathways phenacetin serves currently as an experimental reference compound in evaluating nephrotoxic effects in biomedical research following its market withdrawal due to nephropathy concerns
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
Apexbio Technology LLC SB 203580 hydrochloride 869185-85-3 10mM (in 1mL DMSO)
SB 203580 hydrochloride (CAS 869185-85-3) is a selective inhibitor targeting the p38 mitogen-activated protein kinases (MAPKs) specifically isoforms p38-MAPK and p38-MAPK It prevents the downstream phosphorylation and activation of MAP kinase-activated protein kinase 2 (MAPKAPK2) exhibiting an IC50 around 70 nM in neonatal myocytes Additionally SB 203580 hydrochloride inhibits MAPKAPK2 activation and heat shock protein 27 (HSP27) phosphorylation induced by IL-1 osmotic stress or arsenite in KB cells with IC50 values below 1 M It also reduces JNK-mediated activation of c-Jun in neonatal rat cardiac myocytes This compound is widely utilized in research into cellular stress responses inflammation pathways and cardiac signal transduction
Apexbio Technology LLC PF-670462 950912-80-8 10mM (in 1mL DMSO)
PF-670462 (CAS 950912-80-8) is a selective inhibitor of casein kinase 1 (CK1) isoforms CK1 and CK1 serine/threonine kinases involved in circadian rhythm regulation It exhibits inhibitory activity toward CK1 and CK1 with IC50 values of approximately 80 nM and 13 nM respectively In cellular models co-transfected with GFP-tagged PER3 and human CK1 PF-670462 blocks nuclear translocation of PER3 In primary fibroblasts from wild-type mice it dose-dependently prolongs circadian cycle length PF-670462 serves as a useful chemical tool for studying CK1-mediated modulation of circadian rhythms
Apexbio Technology LLC Skepinone-L 1221485-83-1 10mM (in 1mL DMSO)
Skepinone-L (CAS 1221485-83-1) is a selective ATP-competitive inhibitor of p38 mitogen-activated protein kinase (MAPK) This kinase family transduces signals from diverse cellular stressors regulating processes like apoptosis and differentiation Skepinone-L potently inhibits p38 MAPK activity with an IC50 of approximately 5 nM In vitro it dose-dependently reduces phosphorylation of heat shock protein 27 (HSP27) a downstream marker of p38 MAPK in HeLa cells Additionally the compound suppresses key cytokine release (e g TNF- IL-1 IL-10) in human peripheral blood mononuclear cells Oral administration in mice effectively reduced TNF- production illustrating potential applications in inflammation and signaling pathway research
Apexbio Technology LLC Raltegravir (MK-0518) 518048-05-0 10mM (in 1mL DMSO)
Raltegravir (MK-0518) is an inhibitor targeting HIV-1 integrase an enzyme essential for viral genome integration into host cellular DNA This compound disrupts the integrase-catalyzed strand transfer step during viral replication thereby hindering productive HIV infection In vitro studies demonstrate that Raltegravir inhibits replication of multidrug-resistant strains and isolates utilizing either CCR5 or CXCR4 coreceptors Its reported IC50 values typically range within the low nanomolar concentration levels Raltegravir is widely employed as a tool molecule in antiviral mechanism research drug resistance assays and preclinical HIV therapy-focused drug screening studies
Apexbio Technology LLC 17-AAG (KOS953) 75747-14-7 10mM (in 1mL DMSO)
17-AAG (KOS953) is a synthetic derivative of geldanamycin that inhibits heat shock protein 90 (HSP90) It acts by binding to HSP90 causing destabilization of client proteins including HER2 Raf-1 p53 and components of MAPK signaling pathways Reported IC50 for 17-AAG in BT474 cells is approximately 6 nM Its biological activity has been investigated broadly including in multiple myeloma breast cancer thyroid cancer Hodgkin lymphoma and melanoma cellular models Ongoing studies explore 17-AAG both as monotherapy and in combination with agents like bortezomib or trastuzumab for addressing treatment-resistant cancer cell lines Currently 17-AAG is evaluated in Phase II clinical trials
Apexbio Technology LLC SU5416 204005-46-9 10mM (in 1mL DMSO)
SU5416 (CAS 204005-46-9) also known as Semaxanib is a small molecule inhibitor designed to block vascular endothelial growth factor receptor (VEGFR2) particularly targeting Flk-1/KDR receptor tyrosine kinase signaling SU5416 effectively inhibits VEGF-induced phosphorylation of Flk-1 thereby interfering with endothelial cell proliferation angiogenesis and subsequent tumor vascularization Preclinical studies demonstrated suppression of tumor growth accompanied by angiogenesis inhibition Additionally SU5416 acts as an agonist of the aryl hydrocarbon receptor (AHR) modulating immune responses via induction of indoleamine 2 3-dioxygenase (IDO) and regulatory T cell differentiation These properties suggest potential utility not only in cancer research but also in investigating autoimmune conditions and transplant tolerance