Dimethyl Sulfoxide
Apexbio Technology LLC AM1241(Synonyms: AM-1241, CB2 receptor agonist AM1241, Cannabinoid receptor CB2 agonist AM1241, AM 1241), 10mM (in 1mL DMSO), CAS: 444912-48-5.
AM1241 (CAS number 444912-48-5) is a selective agonist of the cannabinoid receptor type 2 (CB2) a G protein-coupled receptor encoded by the CNR2 gene CB2 receptors modulate inflammation and neuropathic pain pathways outside the central nervous system In vitro studies suggest stereoisomer-dependent activities specifically the S-enantiomer demonstrates higher functional potency toward human and rodent CB2 receptors compared to the R-enantiomer In animal models AM1241 administration reduces neuropathic pain phenotypes including hyperalgesia and allodynia and shows potential for delaying disease progression in an ALS (amyotrophic lateral sclerosis) mouse model Currently AM1241 remains a valuable investigational tool in preclinical pain and neurodegeneration research
Apexbio Technology LLC Dacomitinib (PF299804, PF299) 1110813-31-4 10mM (in 1mL DMSO)
Dacomitinib (PF299804 CAS 1110813-31-4) is an irreversible pan-HER small-molecule inhibitor that targets the epidermal growth factor receptor (EGFR/ErbB-1) ERBB2 (HER2) and ERBB4 (HER4) It acts by covalently binding EGFR family tyrosine kinases inhibiting downstream signaling through phospho-HER family proteins AKT and ERK Dacomitinib shows activity in vitro inducing G0/G1 cell cycle arrest and apoptosis and suppresses proliferation in trastuzumab- or lapatinib-resistant HER2-amplified breast cancer cell lines In vivo studies demonstrate antitumor effects in EGFR-mutant (e g T790M) gefitinib-resistant lung cancer xenografts making it relevant for non-small cell lung cancer research
Apexbio Technology LLC Etonogestrel(Synonyms: 3-Ketodesogestrel, Implanon, Nexplanon, ORG-3236, 11-Methylenelevonorgestrel), 10mM (in 1mL DMSO), CAS: 54048-10-1.
Etonogestrel (CAS 54048-10-1) is a synthetic steroidal molecule derived as the biologically active metabolite of the progestin desogestrel Structurally it belongs to the 19-nortestosterone class and acts primarily through potent binding and agonist activity at progesterone receptors Through this receptor binding it modulates various physiological processes including ovulation suppression cervical mucus viscosity enhancement and endometrial alteration Etonogestrel serves as a widely researched hormonal contraceptive with applications in reproductive biology studies endocrinological research and pharmaceutical development
Apexbio Technology LLC MK-8245 1030612-90-8 10mM (in 1mL DMSO)
MK-8245 (CAS 1030612-90-8) is a potent liver-selective small molecule inhibitor of stearoyl-CoA desaturase (SCD) SCD1 catalyzes fatty acid desaturation and represents a target for treating type II diabetes obesity dyslipidemia and other metabolic disorders MK-8245 demonstrates strong inhibitory activity against rat mouse and human SCD1 with an IC50 of approximately 1 nM and displays liver-specific tissue distribution mediated by organic anion transporting polypeptides (OATPs) Animal studies revealed MK-8245 reduces blood glucose levels and hepatic triglycerides dose-dependently supporting its application in metabolic disease research
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 PF-477736 952021-60-2 10mM (in 1mL DMSO)
PF-477736 is an ATP-competitive small-molecule inhibitor of checkpoint kinase 1 (Chk1) It selectively inhibits Chk1 kinase activity demonstrating nanomolar inhibitory potency in kinase assays and exhibits lower affinity toward related kinases such as CDK1 and Chk2 In vitro studies utilizing human cancer cell lines show PF-477736 disrupts Chk1-dependent G2-phase cell-cycle arrest induced by DNA-damaging agents preferentially targeting tumor cells with compromised p53 function while minimizing cytotoxicity to normal cells PF-477736 is widely utilized experimentally to study DNA damage response mechanisms potential chemosensitizing effects and therapeutic implications for cancers harboring p53 mutations
Apexbio Technology LLC BV6 1001600-56-1 10mM (in 1mL DMSO)
BV6 (CAS 1001600-56-1) is a selective inhibitor targeting the inhibitor of apoptosis protein (IAP) family The IAP family includes proteins such as XIAP c-IAP1 and c-IAP2 that regulate programmed cell death pathways BV6 induces apoptosis and sensitizes cancer cells to chemotherapeutic agents and radiation by decreasing expression levels of IAPs including XIAP and c-IAP1 In vitro treatment with BV6 exhibited an IC50 of 7 2 M in H460 non-small cell lung carcinoma cells and enhanced their response to radiation BV6 is employed in research exploring cancer cell apoptosis modulation and therapeutic resistance
Apexbio Technology LLC STF-62247 315702-99-9 10mM (in 1mL DMSO)
STF-62247 (CAS 315702-99-9) is a small molecule that selectively targets renal cell carcinoma (RCC) cells carrying von Hippel-Lindau (VHL) gene deletions It exhibits cytotoxicity in both wild-type and VHL-deficient RCC cells via a mechanism independent of hypoxia-inducible factor (HIF) with reported IC50 values of 16 M and 0 625 M respectively In VHL-deficient RCC cells STF-62247 induces acidification autophagy and subsequent apoptotic cell death In mouse xenograft models bearing VHL-deficient SN12C tumors STF-62247 significantly reduced tumor growth This compound is useful for studying therapeutic strategies targeting VHL-deficient tumors
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 SBI-0206965 1884220-36-3 10mM (in 1mL DMSO)
SBI-0206965 (CAS 1884220-36-3) is a small-molecule inhibitor targeting ULK1 (UNC-51-like kinase 1) a serine/threonine kinase pivotal in regulating autophagy initiation ULK1 functions downstream of mTORC1 and is modulated by AMPK influencing cellular responses to nutrient deprivation In cellular assays using A549 cells SBI-0206965 at 5 mM effectively suppresses AZD8055-induced autophagy and increases apoptotic response upon nutrient starvation in MEFs U87MG glioblastoma and mouse lung cancer cell lines SBI-0206965 serves as a useful research tool for investigating autophagy pathways tumor cell survival and apoptosis mechanisms
Apexbio Technology LLC Dihydromyricetin 27200-12-0 10mM (in 1mL DMSO)
Dihydromyricetin also termed Ampelopsin is a natural flavanonol compound frequently investigated for its antioxidant and anticancer properties It exerts biological effects primarily through modulation of molecular pathways involving oxidative stress responses apoptosis regulation and GABA-A receptor enhancement at benzodiazepine binding sites Studies indicate dihydromyricetin acts as a positive allosteric modulator on GABA-A receptors suggesting potential for research related to alcohol intoxication and associated neural mechanisms In cellular assays dihydromyricetin demonstrates antiproliferative activity against various cancer cell lines typically exhibiting IC50 concentrations in the micromolar range Thus this compound is widely utilized in biomedical research including cell signaling pathway analysis antioxidant mechanism exploration and studies examining potential therapeutic roles in oncology and neuropharmacology
Apexbio Technology LLC YM201636 371942-69-7 10mM (in 1mL DMSO)
YM201636 is a cell-permeable selective inhibitor of the mammalian class III phosphatidylinositol phosphate kinase PIKfyve It functions by targeting and inhibiting PIKfyve enzymatic activity at an IC50 of approximately 33 nM thus reducing the biosynthesis of phosphatidylinositol (3 5)-bisphosphate (PtdIns(3 5)P2) Treatment of various mammalian cell lines (including NIH3T3 MDCK MCF10A COS7 and MEFs) with YM201636 induces the formation of enlarged intracellular vacuoles pointing toward changes in endosomal transport and membrane trafficking Furthermore YM201636 has shown utility in studying insulin-mediated signaling by inhibiting insulin-dependent class I PI3K activation lowering Akt phosphorylation and preventing surface translocation of GLUT4 in adipocytes Researchers frequently utilize this compound to analyze intracellular vesicular transport pathways and phosphoinositide-dependent signaling events
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