Dimethyl Sulfoxide
Apexbio Technology LLC Verapamil HCl 152-11-4 10mM (in 1mL DMSO)
Verapamil HCl (CAS 152-11-4) is a small molecule belonging to the phenylalkylamine class characterized by selective inhibition of L-type calcium channels By blocking calcium influx through voltage-dependent calcium channels verapamil modulates intracellular calcium signaling affecting smooth muscle contraction cardiac electrophysiology and neurotransmitter release It is frequently utilized in research to investigate calcium channel-related physiological processes cardiovascular function and cellular signaling mechanisms
Apexbio Technology LLC TAK-242 243984-11-4 10mM (in 1mL DMSO)
TAK-242 (CAS 243984-11-4) also known as resatorvid is a cyclohexene derivative that functions as a selective inhibitor of Toll-like receptor 4 (TLR4) signaling Mechanistically TAK-242 binds specifically to the intracellular domain of TLR4 disrupting its interaction with downstream adaptor proteins and thus suppressing activation of inflammatory signal pathways triggered by lipopolysaccharide (LPS) In vitro TAK-242 inhibits LPS-induced production of nitric oxide TNF- and interleukin-6 in macrophages (IC50 1 1 11 nM) Preclinical animal models indicate its potential usefulness in mitigating inflammatory responses associated with neuropsychiatric conditions triggered by stress
Apexbio Technology LLC Roflumilast 162401-32-3 10mM (in 1mL DMSO)
Roflumilast is an orally available selective inhibitor of phosphodiesterase-4 (PDE-4) with an IC50 value of approximately 0 11 nM PDE-4 enzymes catalyze the hydrolysis of cyclic adenosine monophosphate (cAMP) and are predominantly expressed in various inflammatory and immune cells By selectively inhibiting PDE-4 activity Roflumilast elevates intracellular cAMP levels thus regulating cellular inflammatory signaling pathways This mechanism supports its use in the reduction of inflammatory responses associated with chronic obstructive pulmonary disease (COPD) Additionally Roflumilast has been investigated experimentally regarding its potential influence on glucose metabolism in early-stage type 2 diabetes mellitus
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 CYT387 1056634-68-4 10mM (in 1mL DMSO)
CYT387 (CAS 1056634-68-4) is an aminopyrimidine derivative identified through high-throughput screening and optimized with structure-guided medicinal chemistry It functions as an inhibitor targeting Janus kinase family enzymes JAK1 JAK2 JAK3 and TYK2 with reported IC50 values of 11 nM 18 nM 155 nM and 17 nM respectively At concentrations between 500 1500 nM CYT387 selectively suppresses JAK2 signaling inhibits proliferation of JAK2-dependent hematopoietic cell lines and induces apoptosis with minimal effects on non-hematopoietic cells CYT387 is employed in experimental studies of JAK2-mediated signaling pathways and myeloproliferative neoplasms
Apexbio Technology LLC MI-77301 (SAR405838) 1303607-60-4 10mM (in 1mL DMSO)
MI-77301 (SAR405838 CAS 1303607-60-4) is a selective antagonist targeting the murine double minute 2 (MDM2) protein an E3 ubiquitin ligase responsible for negatively regulating tumor-suppressor p53 via ubiquitination and degradation By inhibiting the MDM2-p53 interaction (Ki 0 88 nM) MI-77301 stabilizes p53 elevates protein levels of p53 p21 and MDM2 and induces apoptosis Preclinical studies demonstrate selective growth inhibition in tumor cell lines harboring wild-type p53 (e g SJSA-1 RS4 11 LNCaP HCT-116) and potent tumor regressions in corresponding xenograft mouse models highlighting its utility for mechanistic studies and cancer therapeutic research
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 BI6727 (Volasertib)(Synonyms: Volasertib, BI-6727, BI 6727, Plk inhibitor BI6727, Polo-like kinase inhibitor BI6727), 10mM (in 1mL DMSO), CAS: 755038-65-4.
BI6727 (Volasertib CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk) primarily targeting Plk1 with an IC50 of 0 87 nM and showing lower potency towards Plk2 (IC50 5 nM) and Plk3 (IC50 56 nM) Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types representing a potential therapeutic target BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116 EC50 23 nM) lung (NCI-H460 EC50 21 nM) melanoma (BRO EC50 11 nM) and hematologic cancer (GRANTA EC50 15 nM) In vivo BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models
Apexbio Technology LLC Quizartinib (AC220) 950769-58-1 10mM (in 1mL DMSO)
Quizartinib (AC220) is a second-generation small molecule inhibitor specifically targeting FMS-like tyrosine kinase 3 (FLT3) It exhibits potent inhibitory activity against FLT3 kinases harboring internal tandem duplication (ITD) and wild-type forms with reported IC50 values around 1 1 nM and 4 2 nM respectively Quizartinib demonstrates selectivity for FLT3 with minimal inhibition toward other kinases such as KIT PDGFR / RET and CSF-1R In cell-based assays using MV4-11 AML cell lines that express FLT3-ITD quizartinib reduces FLT3 phosphorylation thus inhibiting downstream signaling pathways involved in tumor cell proliferation and survival Quizartinib is utilized primarily in leukemia research to examine FLT3 signaling dependency and resistance mechanisms providing a useful tool for investigating molecular pathways and therapeutic strategies in acute myeloid leukemia (AML)