Dimethyl Sulfoxide
Apexbio Technology LLC MHY1485 326914-06-1 10mM (in 1mL DMSO)
MHY1485 (CAS 326914-06-1) is a potent activator of mammalian target of rapamycin (mTOR) a serine/threonine kinase critical for cellular growth metabolism and survival pathways By activating mTOR signaling MHY1485 inhibits autophagy initiation and disrupts the fusion step between autophagosomes and lysosomes resulting in accumulation of autophagic marker LC3-II and enlarged autophagic structures In cultured rat Ac2F hepatic cells MHY1485 suppresses basal and starvation-induced autophagic flux Additionally MHY1485 treatment promotes ovarian follicular development and increases explant growth in mouse ovarian culture models providing a useful tool in biomedical research of mTOR signaling and reproductive biology
Apexbio Technology LLC Bromodomain Inhibitor, (+)-JQ1 1268524-70-4 10mM (in 1mL DMSO)
( )-JQ1 is a selective small-molecule inhibitor targeting BET (bromodomain and extraterminal) protein family members particularly BRD4 It competitively binds the acetyl-lysine recognition domain of BRD4 bromodomains 1 and 2 with reported Kd values of approximately 50 nM and 90 nM respectively By selectively inhibiting BET proteins ( )-JQ1 disrupts transcriptional regulatory processes essential in cancer biology rendering it a useful research tool for examining chromatin remodeling and gene expression patterns associated with tumor pathogenesis Additionally ( )-JQ1 specifically targets the testis-specific bromodomain protein BRDT enabling investigations into male reproductive biology by reversibly impairing spermatogenesis
Apexbio Technology LLC Baicalein 491-67-8 10mM (in 1mL DMSO)
Baicalein is a natural flavonoid compound extracted from the medicinal herb Scutellaria baicalensis known to function as an inhibitor of lipoxygenase enzymes It selectively inhibits the 12-lipoxygenase (12-LOX) mediated metabolic pathway involved in arachidonic acid metabolism subsequently modulating inflammatory responses and cell proliferation signaling Baicalein demonstrates bioactivity as reflected by reported IC50 values typically ranging from 0 6 M to 2 5 M against purified human platelet 12-LOX enzyme It is utilized in biomedical research primarily to study inflammation pathways tumor cell proliferation processes and mechanisms underlying apoptosis induction
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 Telaprevir (VX-950) 402957-28-2 10mM (in 1mL DMSO)
Telaprevir (VX-950) is an inhibitor that targets the hepatitis C virus (HCV) NS3-4A protease an essential enzyme for HCV replication Structurally derived from the viral NS5A/5B substrate Telaprevir binds to the NS3-4A protease in a covalent reversible manner through a slow-binding and dissociation mechanism thereby interrupting viral polyprotein processing Experimental studies have demonstrated that Telaprevir inhibits genotype 1 (H strain) NS3 protease with a reported inhibition constant (Ki) of approximately 7 nM In HCV replicon cell assays Telaprevir exhibits antiviral activity effectively suppresses viral replication and delays the development of viral resistance showing synergy when combined with interferon-alpha (IFN- ) Telaprevir serves as a research tool for studying antiviral mechanisms and therapeutic combinations in preclinical HCV models
Apexbio Technology LLC MC1568 852475-26-4 10mM (in 1mL DMSO)
MC1568 (CAS 852475-26-4) is a histone deacetylase (HDAC) inhibitor derived from the (aryloxopropenyl)pyrrolyl hydroxyamide chemical class It selectively targets class II HDAC enzymes particularly class IIa subtypes (HDAC4 HDAC5 HDAC7 HDAC9) inhibiting maize class II HDAC activity with an IC50 of 22 M MC1568 modulates muscle differentiation pathways by reducing MEF2D expression stabilizing HDAC-HDAC3-MEF2D complexes and preventing MEF2D acetylation in cultured myocytes It also interferes with differentiation signals mediated via RAR and PPAR nuclear receptors serving as a valuable tool in epigenetic and cellular differentiation studies
Apexbio Technology LLC JNJ-26481585 875320-29-9 10mM (in 1mL DMSO)
JNJ-26481585 (CAS 875320-29-9) is a small-molecule inhibitor targeting class I histone deacetylases (HDACs) specifically HDAC1 HDAC2 and HDAC3 with reported IC50 values of 0 11 0 33 and 4 8 nM respectively It exhibits potent anti-proliferative activity across various human cancer cell lines including lung breast colon prostate ovarian and brain cancers (IC50 range 3 1 246 nM) Mechanistically JNJ-26481585 induces histone H3 acetylation alleviates HDAC-mediated repression of the p21waf1 cip1 promoter and promotes apoptosis in colorectal cancer cell models Consequently this compound serves as a research tool for cancer epigenetics and therapeutic assessment
Apexbio Technology LLC SLx-2119 911417-87-3 10mM (in 1mL DMSO)
SLx-2119 (CAS 911417-87-3) also known as KD-025 is a selective inhibitor targeting Rho-associated protein kinase 2 (ROCK2) exhibiting an IC50 of approximately 105 nM ROCK2 is a serine/threonine kinase central to cytoskeletal modulation and cellular signaling particularly expressed within neuronal and vascular cells SLx-2119 reduces connective tissue growth factor (CTGF) mRNA expression selectively in human intestinal smooth muscle cells isolated from radiation-induced fibrosis tissue (RE-SMC) whereas normal smooth muscle cells remain unaffected Additionally in a murine model of focal cerebral ischemia SLx-2119 treatment yields a dose-dependent decrease in infarct size across aged and diabetic models highlighting its research applicability in ischemic stroke and fibrotic disorders
Apexbio Technology LLC PF-3758309 898044-15-0 10mM (in 1mL DMSO)
PF-3758309 (CAS 898044-15-0) is a selective ATP-competitive inhibitor of p21-activated kinase 4 (PAK4) a serine/threonine kinase involved in cytoskeletal reorganization and cellular signaling mediated by Cdc42-GTP and JNK-GTP interactions PF-3758309 inhibits phosphorylation of PAK4 substrates (e g GEF-H1 IC50 1 3 nM) and suppresses PAK4-mediated anchorage-independent growth In xenograft tumor models (HCT116 A549) oral administration of PF-3758309 significantly reduced tumor growth demonstrating its utility in research investigating PAK-dependent oncogenic pathways
Apexbio Technology LLC Vardenafil 224785-90-4 10mM (in 1mL DMSO)
Vardenafil (CAS 224785-90-4) is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) It inhibits PDE5 enzyme activity with an IC50 of approximately 0 7 nM in vitro Compared with other PDE isoforms (PDE1-4 and PDE6) vardenafil demonstrates superior selectivity toward PDE5 though moderate inhibition of PDE6 (IC50 11 nM) is observed Vardenafil enhances cGMP accumulation in human corpus cavernosum and significantly potentiates nitric oxide (SNP)- acetylcholine- and electrical field stimulation-induced relaxation in human trabecular smooth muscle Its vasodilatory effects render it suitable for research in erectile function and related vascular physiology
Apexbio Technology LLC Salirasib 162520-00-5 10mM (in 1mL DMSO)
Salirasib (CAS 162520-00-5) chemically known as S-trans trans-farnesylthiosalicylic acid (FTS) is a synthetic inhibitor targeting Ras proteins Structurally mimicking the carboxy-terminal farnesylated cysteine found in Ras Salirasib disrupts Ras localization at the cellular membrane thereby reducing activity of H-ras K-ras and N-ras isoforms Research indicates that Salirasib reduces Ras protein levels by approximately 50% at concentrations of 25 50 M in Panc-1 pancreatic cancer cells In xenograft models it exhibits tumor growth inhibition alone and synergistically with gemcitabine Clinical phase I studies support its continued investigation in solid-tumor therapy recommending a dose of 600 mg/day
Apexbio Technology LLC Pracinostat (SB939) 929016-96-6 10mM (in 1mL DMSO)
Pracinostat (SB939 CAS 929016-96-6) is an orally bioavailable inhibitor of histone deacetylases (HDAC) preferentially targeting class I II and IV HDACs with substantially lower affinity for class III enzymes By inhibiting these enzymes pracinostat promotes accumulation of acetylated histone H3 and acetylated -tubulin subsequently upregulating cell cycle regulator p21 In preclinical investigations SB939 demonstrated antiproliferative activity in various tumor cell lines including colon ovarian prostate cancers acute myeloid leukemia (AML) and B-cell lymphoma highlighting its potential utility in oncology research
Apexbio Technology LLC CASPOFUNGIN 10MM IN 1ML DMSO
Caspofungin (CAS 162808-62-0) is a small-molecule inhibitor of -1 3-glucan synthase an enzyme essential for the biosynthesis of -(1 3)-D-glucan a fundamental cell wall component in pathogenic fungi such as Candida albicans Caspofungin selectively inhibits -1 3-glucan synthase activity with a reported IC50 of approximately 0 6 nmol/L in membrane preparations of C albicans Caspofungin demonstrates potent antifungal activity against various Candida isolates including azole-resistant strains (MIC90 0 5 g/mL) and shows prolonged post-antifungal effects lasting 6 8 hours It is widely utilized in biomedical research involving fungal infections and antifungal therapeutics
Apexbio Technology LLC CHIDAMIDE 10MM IN 1ML DMSO
Chidamide (CAS 743420-02-2) is a benzamide-based histone deacetylase (HDAC) inhibitor that targets enzymes responsible for the reversible acetylation of lysine residues on histone tails By modulating HDAC activity Chidamide promotes chromatin remodeling influencing transcription factor access and subsequent gene transcription In vitro studies on human leukemia cell lines and primary myeloid leukemia cells indicate that Chidamide induces cell cycle arrest at the G1 phase differentiation and apoptosis via ROS-dependent mechanisms Therefore Chidamide shows considerable potential in research focused on hematologic malignancies and cancer therapy
Apexbio Technology LLC N6022 10MM IN 1ML DMSO
N6022 (CAS 1208315-24-5) is a selective reversible inhibitor of S-nitrosoglutathione reductase (GSNOR) an enzyme involved in regulating the levels of S-nitrosoglutathione (GSNO) Inhibition of GSNOR leads to elevated GSNO concentrations promoting vasodilatory and anti-inflammatory effects In biochemical assays N6022 exhibits IC50 values of 8 nM (GSNO reduction assay) and 32 nM (HMGSH oxidation assay) with corresponding Ki values of 2 5 nM and 3 1 nM respectively Due to its selectivity profile and potency N6022 has entered clinical evaluation for inflammatory pulmonary conditions