Dimethyl Sulfoxide
Apexbio Technology LLC 3-Deazaneplanocin A (DZNep) hydrochloride 120964-45-6 10mM (in 1mL DMSO)
3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor targeting histone methyltransferase EZH2 exhibiting inhibitory activity with an IC50 range of 0 08-0 24 M Additionally DZNep inhibits S-adenosylhomocysteine hydrolase (SAHH) at a Ki of 50 pM EZH2 acts as a catalytic subunit of polycomb repressive complex 2 (PRC2) participating in modulation of gene expression via histone methylation Research demonstrates that DZNep suppresses EZH2-dependent gene regulation pathways in cancer cells leading to altered expression of cell-cycle and apoptosis-associated genes DZNep is commonly utilized in epigenetic studies of various tumors and metabolic dysfunction models including AML liver fibrosis and lipid accumulation studies
Apexbio Technology LLC AZD6244 (Selumetinib) 606143-52-6 10mM (in 1mL DMSO)
AZD6244 (Selumetinib CAS 606143-52-6) is a small-molecule inhibitor selectively targeting MEK1/2 components of the MAP kinase signaling cascade It inhibits MEK1 via a non-ATP-competitive mechanism with an IC50 of 14 1 nM leading to decreased phosphorylation of downstream targets ERK1/2 (IC50 10 3 nM cellular assays) AZD6244 exhibits minimal off-target activity against related kinases including MKK6 EGFR ErbB2 and B-Raf In tumor cell lines harboring activated Ras or B-Raf mutations AZD6244 reduces cell proliferation and inhibits growth in xenograft models Thus AZD6244 is useful for investigating MAP kinase pathway-driven malignancies
Selleck Chemical LLC GSK2256098 10mM 1mL in DMSOPurity 99.82
GSK2256098 10mM 1mL in DMSOPurity 99.82
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 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 Radezolid 869884-78-6 10mM (in 1mL DMSO)
Radezolid is an oxazolidinone-class antibiotic under investigation targeting Gram-positive bacterial pathogens including methicillin-resistant Staphylococcus aureus (MRSA) By accumulating intracellularly within various host cells such as macrophages epithelial cells and endothelial cells Radezolid disrupts bacterial protein synthesis through inhibition of bacterial ribosomal translation In vitro assessments show antibacterial potency approximately tenfold greater than Linezolid at identical concentrations in infected cell models MIC90 values for MRSA strains indicate enhanced potency relative to Linezolid with MIC90 at approximately 0 5 mg/l compared to 2 0 mg/l for Linezolid Experimental animal models display increased Radezolid accumulation in infected tissues (2 4-fold higher tissue AUC compared to non-infected counterparts) Radezolid is explored in research settings examining complicated skin infections and community-acquired pneumonia (CAP)
Apexbio Technology LLC PCI-34051(Synonyms: PCI 34051, PCI34051, HDAC8 inhibitor PCI-34051, PCI-34051 HDAC inhibitor), 10mM (in 1mL DMSO), CAS: 950762-95-5.
PCI-34051 (CAS 950762-95-5) is a selective inhibitor of histone deacetylase 8 (HDAC8) with over 200-fold specificity compared to other HDAC isoforms including HDAC1 HDAC2 HDAC3 HDAC6 and HDAC10 Through selective HDAC8 inhibition PCI-34051 preferentially triggers caspase-dependent apoptosis in T-cell lymphoma and leukemia-derived cell lines while sparing normal hematopoietic (e g PBMCs) and fibroblast cells Cell death induction by PCI-34051 occurs without detectable histone or tubulin hyperacetylation This compound serves as a valuable research tool for dissecting HDAC8-related pathways and evaluating therapeutic potential for hematologic malignancies
Apexbio Technology LLC Losmapimod 585543-15-3 10mM (in 1mL DMSO)
Losmapimod (CAS 585543-15-3) also known as GW856553 is a selective orally bioavailable inhibitor of p38 mitogen-activated protein kinase (MAPK) It exhibits potent inhibitory activity against p38 and p38 isoforms with reported pKi values of 8 1 and 7 6 respectively By inhibiting p38 MAPK a kinase essential in inflammatory signaling pathways and cytokine production Losmapimod has demonstrated beneficial effects in preclinical and clinical models It improves nitric oxide-mediated vasodilation and reduces markers of systemic inflammation such as C-reactive protein and fibrinogen This molecule is utilized in research studies addressing inflammation-driven cardiovascular disorders hypercholesterolemia and chronic obstructive pulmonary disease (COPD)
Apexbio Technology LLC PF-04449913 1095173-27-5 10mM (in 1mL DMSO)
PF-04449913 (CAS 1095173-27-5) is an orally bioavailable small molecule inhibitor targeting smoothened (SMO) a critical component of the Hedgehog (Hh) signaling pathway Activation of SMO by Hh ligands typically initiates signaling cascades involving Gli transcription factors influencing cellular proliferation and oncogenesis PF-04449913 inhibits SMO activity with an IC50 of 5 nM thereby suppressing downstream Gli-mediated signaling Preclinical pharmacokinetic studies demonstrated favorable properties including a half-life of approximately 30 hours 55% oral bioavailability low plasma clearance (1 03 mL/min/kg) and moderate distribution (2 7 L/kg) PF-04449913 is actively explored in cancer research contexts
Apexbio Technology LLC Pirfenidone 53179-13-8 10mM (in 1mL DMSO)
Pirfenidone (CAS 53179-13-8) is a small molecule antifibrotic agent exhibiting anti-inflammatory properties Mechanistically pirfenidone reduces levels of pro-inflammatory mediators notably TNF- via translational regulation independent of MAPK pathway activation It suppresses TGF- -mediated signaling and extracellular matrix protein production contributing to decreased fibrotic responses in cellular and animal models In vivo pirfenidone administration mitigates fibrosis and inflammatory cytokine expression in tissues such as lung liver and kidney Clinically pirfenidone is investigated primarily for idiopathic pulmonary fibrosis demonstrating reductions in fibrosis progression and improved functional parameters
Apexbio Technology LLC Bilobalide 33570-04-6 10mM (in 1mL DMSO)
Bilobalide (CAS 33570-04-6) is a terpenic trilactone derived from Ginkgo biloba noted for neuroprotective activities It modulates neuronal function partly via interactions with ion channel receptors as evidenced by altered potencies upon receptor-site mutations Bilobalide promotes -secretase-mediated cleavage of amyloid precursor protein (APP) resulting in increased sAPP secretion and reduced amyloid-beta (A ) levels through a PI3K-dependent signaling pathway Animal studies indicate analgesic activity reducing hyperalgesia and inflammation-induced edema comparable to diclofenac Additionally bilobalide improves cognitive performance in animal models associated with enhanced antioxidant markers (SOD/GSH) and reduced oxidative stress (NOS/MDA)