Dimethyl Sulfoxide
Apexbio Technology LLC Flucytosine 2022-85-7 10mM (in 1mL DMSO)
Flucytosine also known as 5-Fluorocytosine (5-FC) is a fluorinated pyrimidine analogue with antifungal properties It exerts its biological activity by penetrating fungal cells and undergoing intracellular conversion into 5-fluorouracil (5-FU) via cytosine deaminase Subsequently 5-FU metabolites inhibit nucleic acid synthesis interfering with fungal RNA and DNA synthesis pathways thus blocking cellular proliferation In laboratory experiments Flucytosine is commonly utilized for antifungal susceptibility assays fungal growth inhibition studies as well as research into antifungal resistance mechanisms The typical reported in vitro antifungal activity displays IC50 values ranging from approximately 0 12 to 8 g/mL depending on fungal species and experimental conditions
Apexbio Technology LLC Simvastatin (Zocor) 79902-63-9 10mM (in 1mL DMSO)
Simvastatin (CAS 79902-63-9) marketed as Zocor is a synthetic lactone derived from fermented Aspergillus terreus metabolites Following oral administration the inactive lactone is hydrolyzed into an active -hydroxy acid metabolite which specifically inhibits HMG-CoA reductase the rate-limiting enzyme in cholesterol biosynthesis Simvastatin demonstrates antiproliferative effects in hepatocellular carcinoma cells (HepG2 Huh7) inducing apoptosis cell cycle arrest at G0/G1 reducing expression of cyclins (D1 E) and cyclin-dependent kinases (CDK1 2 4) while elevating CDK inhibitors p19 and p27 It is therefore utilized extensively for research in cancer biology cardiovascular pathology and lipid metabolism disorders
Apexbio Technology LLC Nilotinib(AMN-107) 641571-10-0 10mM (in 1mL DMSO)
Nilotinib (AMN-107 CAS 641571-10-0) is an orally bioavailable selective inhibitor targeting the BCR-ABL tyrosine kinase Derived structurally from imatinib nilotinib inhibits both wild-type (WT p210) and mutant forms (E281K E292K F317L M351T F486S) of BCR-ABL reducing their autophosphorylation activity with IC50 values ranging from 20 to 42 nM It also exhibits substantial inhibitory activity against activated KIT mutants (e g V560del K642E) and various KIT double mutations and effectively suppresses PDGFR and PDGFR kinases Nilotinib is utilized extensively in research related to chronic myeloid leukemia and gastrointestinal stromal tumors involving kinase-driven pathologies
Apexbio Technology LLC LY2109761 700874-71-1 10mM (in 1mL DMSO)
LY2109761 (CAS 700874-71-1) is a selective small-molecule inhibitor targeting type I and type II transforming growth factor-beta (TGF- ) receptors (T RI/II) with Ki values of 38 nM and 300 nM respectively Acting through ATP-binding site competition in the TGF- receptor I kinase domain (IC50 69 nM) LY2109761 inhibits downstream signaling pathways implicated in tumor development and metastasis In preclinical studies LY2109761 reduced proliferation migration invasion and promoted apoptosis across various cancer cell types including pancreatic carcinoma glioblastoma and myelomonocytic leukemia It also lowered radiotherapy-induced pulmonary fibrosis in animal models illustrating its broad research utility
Apexbio Technology LLC A66 1166227-08-2 10mM (in 1mL DMSO)
A66 (CAS 1166227-08-2) is a selective inhibitor of the p110 catalytic subunit of class I phosphatidylinositol-4 5-bisphosphate 3-kinase (PI3K) with an IC50 of 32 nM This compound specifically decreases phosphorylation of Akt/PKB and downstream S6K at Thr389 in various cell models including PIK3CA-mutant H1047R cell lines C2C12 myoblasts and 3T3-L1 adipocytes In animal studies A66 reduces tumor growth in xenograft models and improves insulin sensitivity under chronic metabolic stress highlighting its utility in research on PI3K signaling in cancer and metabolic disease
Apexbio Technology LLC Verteporfin 129497-78-5 10mM (in 1mL DMSO)
Verteporfin (CAS 129497-78-5) is a porphyrin-derived small molecule used as a photosensitizer in photodynamic therapy (PDT) Upon photoactivation verteporfin induces targeted vascular endothelial cytotoxicity through intravascular damage and thrombosis formation leading to selective vessel closure Experimental studies indicate verteporfin treatment triggers DNA fragmentation and enhances apoptotic events in vitro displaying potent cytotoxicity against HL-60 cells at concentrations around 100 ng/mL Independently of photoactivation verteporfin also directly modifies and inhibits the autophagy adaptor protein p62 impacting its binding to polyubiquitinated substrates Verteporfin is relevant to biomedical research involving PDT mechanisms autophagy pathways and angiogenesis
Apexbio Technology LLC Axitinib (AG 013736) 319460-85-0 10mM (in 1mL DMSO)
Axitinib (CAS 319460-85-0) also known as AG 013736 is an orally bioavailable selective inhibitor targeting vascular endothelial growth factor receptor (VEGFR) tyrosine kinases 1 2 and 3 It inhibits VEGFR phosphorylation with IC50 values of approximately 0 1 nM (VEGFR-1) 0 2 nM (VEGFR-2) and 0 1 0 3 nM (VEGFR-3) and demonstrates significantly higher selectivity relative to FGFR-1 Axitinib reduces phosphorylation of VEGF-mediated intracellular signaling proteins Akt eNOS and ERK1/2 and exhibits in vivo suppression of VEGFR-2 activation (EC50 0 49 nM) Its antiangiogenic action results in tumor growth delay in human xenograft models (e g HCT-116 SN12C) highlighting its utility in cancer research
Apexbio Technology LLC Kaempferol(Synonyms: Kempferol, Kaempherol, Kaempferide, Robigenin, Rhamnolutein, Populnetin), 10mM (in 1mL DMSO), CAS: 520-18-3.
Kaempferol (CAS 520-18-3) is a naturally derived flavonoid isolated from sources including Gingko biloba and red wine It functions biologically by activating the mitochondrial calcium uniporter (EC50 7 M) Additionally kaempferol promotes apoptosis through the caspase-9 pathway by suppressing polo-like kinase 1 (PLK1) expression thereby inhibiting cancer cell proliferation in diverse cell lines It also demonstrates antioxidant properties and reduces osteoclast-mediated bone resorption in vitro These characteristics make kaempferol valuable for researching mitochondrial physiology cancer biology and bone metabolism
Apexbio Technology LLC LCL161 1005342-46-0 10mM (in 1mL DMSO)
LCL161 (CAS 1005342-46-0) is a small-molecule antagonist targeting inhibitor of apoptosis (IAP) proteins specifically designed as a mimetic of the endogenous second mitochondria-derived activator of caspase (SMAC) LCL161 binds to and inhibits XIAP and cIAP1/2 proteins frequently overexpressed in malignant cells It demonstrates antiproliferative activity in vitro against selected hepatocellular carcinoma cell lines (Hep3B PLC5) and hematologic cancer models (ALL) with IC50 values in the micromolar range In in vivo tumor xenograft studies oral administration of LCL161 has led to significant growth delays across various malignancies including osteosarcoma and glioblastoma Its combination with AAVP-delivered TNF- results in synergistic antitumor effects indicating its utility in oncology research
Apexbio Technology LLC PD123319 130663-39-7 10mM (in 1mL DMSO)
PD123319 (CAS 130663-39-7) is a non-peptide antagonist targeting angiotensin II (Ang II) receptors particularly the AT2 receptor subtype It binds selectively exhibiting an IC50 of 34 nM in rat adrenal assays and 210 nM in rat brain binding assays Additionally PD123319 inhibits Ang II binding to bovine adrenal glomerulosa microsomal preparations with an IC50 of 6 9 nM Its antagonistic activity leads to reduced cyclic GMP synthesis and elevated prostaglandin E2 production without altering protein tyrosine phosphorylation or thymidine incorporation mediated by Ang II PD123319 serves as a useful pharmacological tool in investigating Ang II receptor signaling pathways
Apexbio Technology LLC Prilocaine 721-50-6 10mM (in 1mL DMSO)
Prilocaine (CAS 721-50-6) is a local anesthetic molecule categorized within the amino amide class Its primary pharmacological mechanism involves reversible blockade of voltage-gated sodium channels in neuronal membranes thereby inhibiting action potential propagation and sensory nerve impulse conduction Due to its sodium channel-blocking profile prilocaine is commonly investigated in biomedical research examining reversible neural inhibition pain modulation pathways and sensory signal transmission mechanisms
Apexbio Technology LLC Carvedilol 72956-09-3 10mM (in 1mL DMSO)
Carvedilol is an antagonist targeting 1- and -adrenergic receptors employed in research on cardiovascular diseases especially congestive heart failure and hypertension Mechanistically carvedilol blocks adrenergic receptor-mediated signaling influencing sympathetic nervous system activity Additionally carvedilol exhibits antioxidative properties in vitro studies demonstrate suppression of Fe2 -induced lipid peroxidation (IC50 8 1 M) protection of -tocopherol depletion due to Fe2 exposure (IC50 17 6 M) and reduction of hydroxyl radical-derived DMPO-OH signals (IC50 25 M) It also inhibits proliferation (IC50 0 3-2 0 M) and migration (IC50 3 M) in vascular smooth muscle cells induced by platelet-derived growth factor supporting investigation of vascular remodeling processes
Apexbio Technology LLC CX-4945 (Silmitasertib) 1009820-21-6 10mM (in 1mL DMSO)
CX-4945 (Silmitasertib CAS 1009820-21-6) is an orally bioavailable inhibitor targeting casein kinase 2 (CK2) via ATP-competitive binding with an IC50 of approximately 1 nM It suppresses CK2-mediated signaling pathways notably by reducing phosphorylation of Akt at Ser129 independently of PTEN activation thus impacting PI3K/Akt pathway regulation In vitro studies report that CX-4945 treatment leads to increased total expression and decreased phosphorylation of cell cycle regulators p21 and p27 causing cell cycle arrest (G2/M in BT-474 breast carcinoma G1 in BxPC-3 pancreatic carcinoma) In vivo it displays antitumor activity in BxPC-3 mouse xenograft models highlighting its utility for oncology research
Apexbio Technology LLC SB 431542 301836-41-9 10mM (in 1mL DMSO)
SB 431542 (CAS number 301836-41-9) is a selective ATP-competitive inhibitor targeting activin receptor-like kinase 5 (ALK5) a type I receptor within the transforming growth factor- (TGF- ) signaling pathway It inhibits ALK5 activity with an IC50 value of 94 nM thereby preventing phosphorylation of Smad2 proteins and their subsequent nuclear accumulation Additionally SB 431542 inhibits closely related receptors ALK4 and ALK7 while showing minimal or no significant activity against ALK1 ALK2 ALK3 and ALK6 at relevant concentrations Commonly utilized in cellular assays to investigate TGF- signaling this compound is valuable for studying associated cellular processes and diseases
Apexbio Technology LLC SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation