Dimethyl Sulfoxide
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 Celastrol 34157-83-0 10mM (in 1mL DMSO)
Celastrol (CAS 34157-83-0) is a triterpene compound isolated from the Chinese medicinal herb Thunder of God Vine It functions as a proteasome inhibitor targeting the proteolytic activities within the 20S and 26S proteasome complexes leading to intracellular accumulation of ubiquitinated substrates including I B- Bax and p27 thereby inducing apoptosis in cancer cell lines such as human prostate cancer (PC-3 and LNCaP) Celastrol also inhibits NF- B signaling decreasing LPS-induced production of inflammatory cytokines (TNF- and IL-1 ) in human PBMCs and augmenting TNF-mediated apoptosis in KBM-5 cells Its anti-inflammatory and pro-apoptotic properties make celastrol relevant in cancer and inflammation research
Apexbio Technology LLC HTH-01-015(Synonyms: HTH01015, WZ4003, NUAK1 inhibitor WZ4003, NUAK1-IN-1, NUAK1 inhibitor, WZ-4003), 10mM (in 1mL DMSO), CAS: 1613724-42-7.
HTH-01-015 (CAS 1613724-42-7) is a highly selective inhibitor targeting the NUAK1 kinase exhibiting potent inhibitory activity with an IC50 of approximately 100 nM It specifically blocks NUAK1-mediated phosphorylation of MYPT1 at Ser445 with negligible off-target effects among a comprehensive panel of 139 other kinases Cellular studies demonstrate that treatment with HTH-01-015 reduces migration of mouse embryonic fibroblasts (MEFs) suppresses proliferation in U2OS and MEF cell lines at concentrations around 10 M and significantly inhibits invasion of U2OS cells within 3D Matrigel transwell assays This compound serves as a useful research tool for investigating NUAK1-related signaling pathways in cancer biology and cellular dynamics
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 EMD638683 1181770-72-8 10mM (in 1mL DMSO)
EMD638683 (CAS 1181770-72-8) is a selective inhibitor of serum- and glucocorticoid-inducible kinases (SGKs) including isoforms SGK1 SGK2 and SGK3 SGK1 regulates key cellular processes such as ion transport survival proliferation and responses to steroid hormones EMD638683 shows inhibitory activity against SGK1 SGK2 and SGK3 (IC50 3 M) significantly reducing SGK-dependent phosphorylation of NDRG1 in vitro It demonstrates limited off-target interactions inhibiting only MSK1 and PRK2 at 1 M while sparing numerous other kinases In cell models EMD638683 influences mitochondrial polarization and caspase activity exhibiting antitumor effects in colorectal tumor cells and antihypertensive activity in vivo
Apexbio Technology LLC LDN193189 Hydrochloride 1062368-62-0 10mM (in 1mL DMSO)
LDN193189 Hydrochloride is a selective pharmacological inhibitor targeting BMP type I receptor kinases specifically activin receptor-like kinase 2 (ALK2) and ALK3 The compound acts by blocking receptor-mediated activation of Smad-dependent signaling pathways (Smad1/5/8 phosphorylation) as well as mitigating associated non-Smad signaling including phosphorylation of Akt and p38 Commonly utilized in biomedical research involving cellular differentiation epithelial barrier integrity and heterotopic ossification LDN193189 has shown the capacity to modulate BMP-induced phenotypic changes in various cell lines such as C2C12 myoblasts and bronchial epithelial cells and to influence related in vivo processes
Apexbio Technology LLC Polydatin 27208-80-6 10mM (in 1mL DMSO)
Polydatin (CAS 27208-80-6) is a naturally occurring stilbenoid isolated primarily from the roots of Polygonum cuspidatum Structurally it represents the glucoside derivative of resveratrol exerting antioxidant and anti-inflammatory effects through modulation of oxidative stress-related pathways Research indicates that polydatin influences signaling cascades such as NF- B MAPK and Nrf2 contributing to its protective roles in cellular injury models including cardiovascular dysfunction neurodegeneration and inflammatory conditions Polydatin is soluble in methanol ethanol and acetone and stability is maintained by storage under sealed cool dry conditions
Apexbio Technology LLC Vemurafenib (PLX4032, RG7204) 918504-65-1 10mM (in 1mL DMSO)
Vemurafenib (PLX4032 RG7204 CAS 918504-65-1) is a small-molecule inhibitor targeting BRAF kinase primarily inhibiting the activity of the oncogenic BRAF V600E mutant by competitively binding its ATP-binding site It also inhibits related kinases such as CRAF ARAF and wild-type BRAF In cells lacking BRAF mutations vemurafenib may paradoxically stimulate downstream MEK signalling due to transactivation mechanisms within RAF dimers Vemurafenib serves as an important research tool for investigating RAF-mediated signaling pathways in oncology particularly in melanoma studies
Apexbio Technology LLC GSK2126458(Synonyms: Omipalisib, GSK-2126458, GSK 2126458, Omipalisib (GSK2126458)), 10mM (in 1mL DMSO), CAS: 1086062-66-9.
GSK2126458 (CAS 1086062-66-9) is a small molecule inhibitor targeting PI3K and mTOR pivotal regulators in cell growth proliferation and tumor progression GSK2126458 demonstrates potent inhibitory activity against PI3K (Ki 19 pM) In colon cancer cells combined use with DDR1-IN-1 enhances its antiproliferative effects Additionally the compound induces G1 phase arrest in BT474 breast cancer cells and sensitizes nasopharyngeal carcinoma (NPC) cell lines to radiation therapy In vivo studies show that combining GSK2126458 with radiation or with MEK and BRAF inhibitors suppresses tumor growth GSK2126458 also influences cellular autophagy pathways highlighting its utility in oncology-focused biomedical research
Apexbio Technology LLC Batimastat (BB-94)(Synonyms: BB-94, Batimastat, MMP inhibitor BB-94), 10mM (in 1mL DMSO), CAS: 130370-60-4.
Batimastat (BB-94 CAS 130370-60-4) is a synthetic small-molecule inhibitor targeting matrix metalloproteinases (MMPs) Structurally a polypeptide-like analogue of collagen substrates batimastat contains a peptidic backbone and a hydroxamate moiety that binds the catalytic zinc atom of MMPs It inhibits several MMP subtypes markedly including MMP-1 MMP-2 MMP-3 MMP-7 and MMP-9 with reported IC50 values of 3 4 20 6 and 4 nM respectively In preclinical studies batimastat demonstrates inhibitory effects on tumor growth and angiogenesis across various tumor models including ovarian and colon carcinoma xenografts making it relevant for cancer research and therapeutic development
Apexbio Technology LLC Melatonin(Synonyms: N-acetyl-5-methoxytryptamine, MEL, Circadin, Melovine, Melatol), 10mM (in 1mL DMSO), CAS: 73-31-4.
Melatonin (CAS 73-31-4) is a naturally occurring hormone functioning primarily as an agonist at the G protein-coupled melatonin receptors MT and MT Through receptor activation melatonin regulates circadian rhythmicity and contributes significantly to sleep-wake cycle maintenance Additionally melatonin demonstrates immunomodulatory capabilities and possesses robust antioxidant properties in vivo combating oxidative stress Due to these characteristics it is frequently investigated in research related to sleep disorders circadian biology immune function and oxidative stress signaling pathways
Apexbio Technology LLC GM 6001 142880-36-2 10mM (in 1mL DMSO)
GM 6001 (Ilomastat Galardin CAS 142880-36-2) is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) including MMP-1 -2 -3 -8 and -9 with reported Ki values of 0 4 nM 0 5 nM 27 nM 0 1 nM and 0 2 nM respectively MMPs participate in extracellular matrix remodeling and mediate signaling events induced by GPCR agonists through EGFR transactivation GM 6001 suppresses EGFR phosphorylation ERK activation and subsequent DNA synthesis induced by stimuli such as bombesin and lysophosphatidic acid (LPA) Additionally this compound has potential applications in cartilage research facilitating meniscal repair under inflammatory conditions by dampening IL-1-mediated MMP activity