Dimethyl Sulfoxide
Apexbio Technology LLC Thioridazine HCl 130-61-0 10mM (in 1mL DMSO)
Thioridazine HCl is a pharmacological inhibitor targeting dopamine receptor subtypes D2 and D4 as well as a calcium channel blocker It modulates dopaminergic neurotransmission by interfering with receptor-mediated signaling and reduces intracellular calcium influx via calcium channel inhibition (IC50 approximately 1 0 M) Thioridazine is frequently utilized in research contexts involving dopaminergic signaling pathways calcium-related cellular processes and investigations of pharmacological sensitivity shifts following prolonged receptor modulation Specifically it is employed experimentally to examine receptor-mediated cardiovascular responses such as hypotension and to assess alterations in dopamine receptor responsiveness induced by chronic exposure regimens
Apexbio Technology LLC CPI-169 1450655-76-1 10mM (in 1mL DMSO)
CPI-169 is a selective small-molecule inhibitor targeting enhancer of zeste homolog 2 (EZH2) a catalytic component of polycomb repressive complex 2 (PRC2) By inhibiting EZH2 enzymatic activity CPI-169 suppresses methylation at histone H3 lysine 27 (H3K27me3) thereby altering chromatin structure and gene expression profiles Pharmacological experiments demonstrate inhibition of EZH2 with subnanomolar IC50 values and cellular studies indicate reductions of H3K27 trimethylation at nanomolar concentrations CPI-169 has been utilized experimentally to investigate EZH2-dependent epigenetic processes cell proliferation apoptosis pathways and therapeutic potential particularly in lymphoma and cancer biology studies employing in vitro and in vivo models
Apexbio Technology LLC LDC1267 1361030-48-9 10mM (in 1mL DMSO)
LDC1267 (CAS 1361030-48-9) is a selective inhibitor of the TAM receptor tyrosine kinases Mer Tyro3 and Axl demonstrating IC50 values of less than 5 nM 8 nM and 29 nM respectively By inhibiting TAM signaling LDC1267 abolishes Gas6-mediated suppression in NKG2D-activated natural killer (NK) cells thus enhancing NK-mediated cytotoxicity Preclinical studies show reduced metastasis of melanoma and 4T1 breast tumor cells upon LDC1267 administration in mouse models an effect reliant on NK cell function LDC1267 provides a research tool for investigating TAM-regulated immune modulation in cancer models
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 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 GW3965 HCl 405911-17-3 10mM (in 1mL DMSO)
GW3965 HCl is a selective non-steroidal agonist targeting liver X receptors (LXR and LXR ) nuclear transcription factors involved in cholesterol and lipid metabolism Activation of LXRs modulates cholesterol homeostasis by enhancing cholesterol efflux from macrophages stimulating hepatic bile acid synthesis and reducing intestinal cholesterol absorption GW3965 recruits steroid receptor coactivator-1 (SRC-1) to human LXRR in vitro and functions as a full agonist on cellular assays for both LXR and LXR receptors In animal studies oral administration elevated plasma HDL cholesterol levels and increased expression of the cholesterol transporter ABCA1 in macrophages GW3965 is useful in research investigating cholesterol metabolism atherosclerosis and vascular responses mediated by Angiotensin II signaling
Apexbio Technology LLC SGI-1776 free base 1025065-69-3 10mM (in 1mL DMSO)
SGI-1776 free base (CAS 1025065-69-3) is an ATP-competitive inhibitor targeting Pim kinases a serine/threonine protein kinase family implicated in regulating cellular survival pathways It selectively inhibits all three isoforms Pim-1 Pim-2 and Pim-3 leading to decreased phosphorylation of downstream substrates involved in cell cycle regulation and apoptosis such as p21Cip1/WAF1 and Bad Cellular studies indicate that SGI-1776 induces G1 cell cycle arrest promotes apoptosis and overcomes chemoresistance mediated by multidrug resistance protein 1 (MDR1) in taxane-resistant prostate cancer cells
Apexbio Technology LLC Flutamide 13311-84-7 10mM (in 1mL DMSO)
Flutamide is a synthetic nonsteroidal antiandrogen agent commonly employed in biomedical research and clinical oncology Its pharmacological activity is mediated through competitive antagonism at the androgen receptor (AR) whereby its active metabolite interacts specifically with AR exhibiting a receptor binding affinity at a K sub i /sub value around 55 nM By interfering with androgen signaling pathways flutamide inhibits AR-mediated transcriptional activity resulting in reduced cellular proliferation particularly in androgen-dependent tissues In research contexts this compound is frequently utilized to investigate AR-mediated cell biology androgen-dependent tumor development and as a pharmacological tool in model systems studying prostate cancer biology and therapeutic resistance mechanisms
Apexbio Technology LLC CUDC-907 1339928-25-4 10mM (in 1mL DMSO)
CUDC-907 (CAS 1339928-25-4) is a dual inhibitor targeting histone deacetylases (HDACs 1 2 3 10) and class I phosphatidylinositol 3-kinases (PI3K) It exhibits nanomolar inhibitory activity against these enzymes blocking PI3K-mediated Akt signaling and increasing acetylation of histones and non-histone substrates (e g tubulin p53) In cancer cell models CUDC-907 induces G2-M phase arrest and reduces phosphorylation of downstream proteins such as p70S6 4EBP-1 MEK STAT3 and SRC Preclinical studies demonstrate its anti-tumor activity in lymphoma and NSCLC xenografts making it relevant for oncology research
Apexbio Technology LLC WZ4003 1214265-58-3 10mM (in 1mL DMSO)
WZ4003 (CAS 1214265-58-3) is a selective inhibitor targeting NUAK1 and NUAK2 kinases members of the AMP-activated protein kinase (AMPK) family activated by tumor suppressor kinase LKB1 WZ4003 inhibits NUAK1 and NUAK2 with IC50 values of 20 nM and 100 nM respectively In cellular assays treatment with WZ4003 reduces NUAK1-mediated phosphorylation of MYPT1 at Ser445 It suppresses cell proliferation migration of mouse embryonic fibroblasts and invasion of U2OS cells Thus WZ4003 serves as a valuable tool for investigating NUAK kinase functions in cell proliferation mobility and signaling mechanisms relevant to oncology research
Apexbio Technology LLC JNK-IN-8 1410880-22-6 10mM (in 1mL DMSO)
JNK-IN-8 (CAS 1410880-22-6) is a potent and specific inhibitor of c-Jun N-terminal kinase (JNK) isoforms JNK1 JNK2 and JNK3 It functions by forming a covalent bond with a conserved cysteine residue in JNKs inducing conformational alteration in the kinase activation loop consequently impairing substrate binding Its IC50 values for JNK1 JNK2 and JNK3 are 4 67 nM 18 7 nM and 0 98 nM respectively In cellular assays JNK-IN-8 prevention of c-Jun phosphorylation demonstrates robust selectivity towards the JNK signaling pathway thus making it valuable as a research tool in studying stress-related cellular responses and apoptosis
Sigma Aldrich Fine Chemicals Biosciences Dimethyl sulfoxide Reagent
Dimethyl sulfoxide is an amphipathic molecule soluble in both aqueous and organic solvents. It is commonly used as an aprotic solvent and also as a reagent in organic synthesis.
Apexbio Technology LLC RO4929097(Synonyms: RO-4929097, RO 4929097, Gamma-Secretase Inhibitor RO4929097, RO4929097 γ-secretase inhibitor), 10mM (in 1mL DMSO), CAS: 847925-91-1.
RO4929097 (CAS 847925-91-1) is a potent selective small-molecule inhibitor of -secretase an essential protease in the Notch signaling pathway It inhibits -secretase with high specificity (IC50 4 nM EC50 5 nM) showing minimal inhibitory activity against closely related proteases and over 100-fold selectivity versus a broad spectrum of other proteases By preventing Notch receptor cleavage and subsequent signaling activation RO4929097 suppresses proliferation and tumorigenesis across various tumor models including melanoma breast colorectal pancreatic and lung cancers Clinical studies have assessed RO4929097 alone or combined with other anticancer agents for advanced solid tumors
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 Irinotecan(Synonyms: CPT-11, Campto, Camptosar, irinotecan hydrochloride, Irinotecan HCl, irinotecan hydrochloride trihydrate), 10mM (in 1mL DMSO), CAS: 97682-44-5.
Irinotecan (CAS 97682-44-5) also known as CPT-11 is an anticancer prodrug that acts as an inhibitor of topoisomerase I Upon enzymatic activation by carboxylesterase (CCE) to its potent metabolite SN-38 it stabilizes the DNA-topoisomerase I cleavable complex causing DNA damage and apoptosis In vitro studies show Irinotecan inhibits various colorectal cancer cell lines including LoVo (IC50 15 8 M) and HT-29 (IC50 5 17 M) Additionally xenograft models such as COLO 320 demonstrate pronounced tumor growth suppression Irinotecan is widely utilized in research to investigate DNA damage mechanisms and therapeutic efficacy in colorectal cancer