Dimethyl Sulfoxide
Apexbio Technology LLC Nexturastat A 1403783-31-2 10mM (in 1mL DMSO)
Nexturastat A (CAS 1403783-31-2) is a selective small-molecule inhibitor of histone deacetylase 6 (HDAC6) It displays potent inhibitory activity against HDAC6 with an IC50 of 5 2 nM While predominantly targeting HDAC6 Nexturastat A also exhibits moderate inhibitory effects on other HDAC isoforms (HDAC1-5 and 7-11) at low micromolar concentrations In cell-based studies including mouse B16 melanoma cell lines Nexturastat A has shown antiproliferative properties and induction of apoptosis Due to its selective HDAC6 inhibition Nexturastat A is utilized in cancer research focusing on epigenetic regulation and therapeutic development
Apexbio Technology LLC Idarubicin HCl 57852-57-0 10mM (in 1mL DMSO)
Idarubicin hydrochloride an anthracycline derivative structurally related to daunorubicin acts primarily by inhibiting DNA topoisomerase II It exerts cytotoxic effects through stabilization of DNA-topoisomerase II intercalation complexes inducing DNA strand breaks and apoptosis Idarubicin can be enzymatically activated intracellularly via NADPH-cytochrome C reductase enhancing DNA damage Experimentally it is commonly utilized in leukemia research particularly acute myeloid leukemia (AML) assessing cellular response to DNA damage apoptosis induction and mechanisms underlying drug resistance Idarubicin exhibits IC50 values typically ranging from low nanomolar to micromolar concentrations depending on cell line and assay conditions
Apexbio Technology LLC Griseofulvin 126-07-8 10mM (in 1mL DMSO)
Griseofulvin is an antifungal antibiotic known to inhibit fungal growth by interfering with microtubule polymerization thereby disrupting mitotic spindle formation and cellular division Through binding to tubulin it stabilizes microtubule structures preventing their normal assembly and leading to impaired fungal cell replication Experimentally Griseofulvin has been frequently utilized to study microtubule dynamics mitotic processes and antifungal mechanisms in research settings involving medically relevant fungi including dermatophytes Reported IC50 values for Griseofulvin range approximately from 5 to 20 M depending on fungal strains and conditions tested serving as a guideline for establishing antifungal assays and investigating fungal response mechanisms in vitro
Apexbio Technology LLC LB42708 226929-39-1 10mM (in 1mL DMSO)
LB42708 (CAS 226929-39-1) is a selective small-molecule inhibitor of farnesyltransferase (FTase) belonging to a non-peptidic pyrrole-based class It blocks FTase-mediated farnesylation of H-Ras N-Ras and K-Ras4B demonstrated by low nanomolar IC50 values (0 8 nM 1 2 nM and 2 nM respectively) LB42708 shows minimal inhibitory effect on geranylgeranyltransferase I In vitro studies indicate inhibition of Ras-driven signaling pathways decreasing Ras activation and subsequently suppressing VEGF-stimulated endothelial proliferation and migration Researchers use LB42708 in oncology and inflammation studies exemplified by reduced tumor growth in Ras-mutant HCT116 and wild-type Caco-2 xenograft models
Apexbio Technology LLC Bortezomib (PS-341) 179324-69-7 10mM (in 1mL DMSO)
Bortezomib (PS-341 CAS number 179324-69-7) is a reversible proteasome inhibitor structurally composed as an N-terminally protected dipeptide (Pyz-Phe-boroLeu) containing pyrazinoic acid phenylalanine and leucine with boronic acid substitution It exerts biological activity primarily by inhibiting proteasomal degradation pathways thereby accumulating pro-apoptotic factors and initiating programmed cell death Bortezomib inhibits proliferation in cell-based assays such as human non-small cell lung cancer H460 cells (IC50 0 1 M) It has clinical approval for relapsed multiple myeloma and mantle cell lymphoma and is widely employed in research to study proteasome-regulated cellular processes and apoptosis signaling pathways
Apexbio Technology LLC Etomidate 10mM (in 1mL DMSO)
A1958 is a small molecule utilized in biomedical research that acts primarily as an inhibitor targeting specific signaling pathways or protein interactions relevant to cellular processes The compound s mechanism typically involves selective modulation or inhibition of targeted biomolecules influencing downstream biological pathways A1958 serves as a research tool for studying cellular mechanisms underlying disease states aiding in cell-based assays to elucidate molecular function and clarify therapeutic targets in biomedical studies
Apexbio Technology LLC Clofazimine 2030-63-9 10mM (in 1mL DMSO)
Clofazimine is a rhimophenazine compound with demonstrated antimicrobial and anti-inflammatory properties commonly utilized in biomedical research related to tuberculosis treatment and drug-resistance studies It functions primarily through the intercalation into bacterial DNA interfering with microbial DNA replication and transcription processes Furthermore it may induce bacterial phospholipid membrane disruption and modulate inflammatory responses Experimental studies report IC50 values in the micromolar range against Mycobacterium tuberculosis strains Clofazimine is frequently employed as a reference compound in antimicrobial assays mechanistic studies on DNA-targeting agents and evaluations of cellular inflammatory pathways within infectious disease model systems
Apexbio Technology LLC SB202190 (FHPI) 152121-30-7 10mM (in 1mL DMSO)
SB202190 (FHPI CAS 152121-30-7) is a selective MAPK inhibitor targeting specifically the p38 isoforms and with reported IC50 values of approximately 50 nM and 100 nM respectively Through inhibition of p38 signaling SB202190 has been observed to stimulate the proliferation of leukemia cell lines including THP-1 and MV4-11 via activation of ERK and C-Raf phosphorylation pathways Additionally SB202190 modulates cellular responses to genotoxic stress such as hydroxyurea-induced premature chromosome condensation and influences histone acetylation status (Lys5 of histone H4) in plant systems Such activities render SB202190 useful for investigating MAP kinase-dependent pathways in cell proliferation and stress responses
Apexbio Technology LLC Pazopanib (GW-786034) 444731-52-6 10mM (in 1mL DMSO)
Pazopanib (GW-786034 CAS 444731-52-6) is a second-generation multitargeted receptor tyrosine kinase inhibitor selectively targeting vascular endothelial growth factor receptors (VEGFR) platelet-derived growth factor receptors (PDGFR) and c-kit Through blockade of these kinase activities pazopanib suppresses signaling cascades essential for angiogenesis and cellular proliferation Preclinical tumor models indicate that pazopanib alone or combined with chemotherapy demonstrates substantial anti-angiogenic and antitumor efficacy Its distinct inhibitory profile of intracellular VEGFR tyrosine kinases offers valuable applications in oncology research particularly in investigating angiogenesis-driven signaling pathways
Apexbio Technology LLC A-803467 944261-79-4 10mM (in 1mL DMSO)
A-803467 (CAS 944261-79-4) is a potent selective blocker of the voltage-gated sodium channel subtype NaV1 8 It inhibits human and rat recombinant NaV1 8 channels with IC50 values of approximately 79 nM and 45 nM respectively Its selectivity for NaV1 8 over other sodium channel subtypes (e g NaV1 2 NaV1 3 NaV1 5 and NaV1 7) is 300 1000 fold By specifically reducing activity in tetrodotoxin-resistant sodium currents of dorsal root ganglion neurons A-803467 suppresses induced and spontaneous action potential firing exhibiting analgesic properties in animal models of neuropathic and inflammatory pain
Apexbio Technology LLC Macitentan 441798-33-0 10mM (in 1mL DMSO)
Macitentan (CAS 441798-33-0) is a small molecule endothelin receptor antagonist acting as a dual inhibitor of ETA and ETB receptors Experimental data using recombinant ETA-expressing CHO cells show that macitentan exhibits potent inhibition of ET-1 ligand binding with an IC50 of approximately 0 5 nM whereas its inhibitory effect on ETB receptors in similar CHO cell systems is weaker (IC50 391 nM) In vivo rodent studies indicate macitentan rapidly converts into ACT-132577 a circulating metabolite with extended half-life and retained dual receptor antagonism This pharmacological profile makes macitentan relevant for biomedical research on endothelin-associated vascular pathologies
Apexbio Technology LLC ML216 1430213-30-1 10mM (in 1mL DMSO)
ML216 (CAS 1430213-30-1) is a small molecule inhibitor targeting Bloom (BLM) helicase a DNA unwinding enzyme essential for homologous recombination-mediated DNA repair ML216 inhibits DNA unwinding activity of full-length BLM (IC50 3 0 M) and a truncated form BLM636-1298 (IC50 0 97 M) displaying sub-micromolar selectivity relative to other helicases such as RECQ1 RECQL5 and bacterial UvrD In cellular assays ML216 selectively suppresses proliferation in BLM-containing fibroblasts increasing sister chromatid exchange frequency consistent with BLM functional deficiency By inhibiting BLM helicase ML216 may sensitize tumor cells to conventional DNA-damaging therapeutics indicating potential application in cancer research and therapy development
Apexbio Technology LLC ORY-1001 1431326-61-2 10mM (in 1mL DMSO)
ORY-1001 is a selective inhibitor targeting the lysine-specific histone demethylase KDM1A (also known as LSD1) an FAD-dependent amine oxidase enzyme responsible for the removal of histone methylation marks particularly dimethylation of histone H3 lysine 4 (H3K4me2) By inhibiting KDM1A ORY-1001 promotes accumulation of H3K4me2 at gene targets and induces cellular differentiation in acute myeloid leukemia (AML) cell models In vitro assays demonstrated dose- and time-dependent increases in H3K4me2 and expression of differentiation markers in treated AML cells ORY-1001 exhibited oral bioavailability in animal xenograft models reducing tumor growth at low daily doses This molecule serves as a valuable research tool in epigenetics oncology pharmacology and studies regarding AML differentiation pathways with ongoing evaluation in early-phase clinical trials
Apexbio Technology LLC SB742457 607742-69-8 10mM (in 1mL DMSO)
SB742457 (CAS 607742-69-8) is a selective antagonist of the serotonin 5-HT6 receptor with high affinity demonstrated by a reported pKi of 9 63 Due to effective brain penetration and oral bioavailability SB742457 has shown the ability to reverse cognitive deficits induced by the cholinergic antagonist scopolamine in rodent novel object recognition tests Acutely administered SB742457 increases extracellular glutamate and acetylcholine levels in the rat medial prefrontal cortex Given these pharmacological properties SB742457 is investigated in cognitive enhancement studies notably related to Alzheimer s disease research
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