Dimethyl Sulfoxide
Apexbio Technology LLC MLN2238(Synonyms: Ixazomib, MLN-2238, Ninlaro, MLN9708, Ixazomib citrate), 10mM (in 1mL DMSO), CAS: 1072833-77-2.
MLN2238 (CAS number 1072833-77-2) is a dipeptidyl boronic acid derivative designed as a reversible inhibitor of the 5 subunit (chymotrypsin-like activity) of the 20S proteasome with reported IC50 and Ki values of 3 4 nM and 0 93 nM respectively At higher concentrations MLN2238 also targets the proteasome s 1 (caspase-like) and 2 (trypsin-like) subunits In preclinical studies using xenograft and genetically-engineered models of hematologic malignancies MLN2238 exhibited potent antitumor activity promoting apoptosis and suppressing pathways such as NF- B MLN2238 has research applications in oncology particularly against multiple myeloma and lymphoma including in bortezomib-resistant cell lines
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 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 GZD824 1421783-64-3 10mM (in 1mL DMSO)
GZD824 (CAS 1421783-64-3) is an orally bioavailable inhibitor of the Bcr-Abl kinase a fusion protein exhibiting tyrosine kinase activity involved in regulating cell cycle progression and genomic stability GZD824 binds competitively to the ATP-binding site of Abl kinase effectively inhibiting the phosphorylation and activation of both wild-type (WT) and resistant mutant forms (e g T315I E255K G250E Q252H H396P M351T and Y253F) GZD824 demonstrates sub-nanomolar IC50 values and substantially reduces proliferation in Bcr-Abl-expressing Ba/F3 cell models Preclinical studies in mouse xenograft leukemia models show GZD824 suppresses tumor growth highlighting its potential applicability in research into resistance mechanisms and targeted leukemia therapies
Apexbio Technology LLC Sirtinol 410536-97-9 10mM (in 1mL DMSO)
Sirtinol (CAS 410536-97-9) is a small-molecule inhibitor targeting class III histone deacetylases (HDAC) specifically the NAD-dependent deacetylases SIRT1 and SIRT2 In MCF-7 human breast cancer cells sirtinol exhibits inhibitory activity against cell proliferation with IC50 values of 48 6 M (24 h) and 43 5 M (48 h) Mechanistically sirtinol reduces SIRT1 expression inducing acetylation of p53 and downregulating cell-cycle proteins such as cyclin B1 cyclin D1 CDK2 and CDK6 leading to G1-phase arrest apoptosis and autophagy This molecule serves as a valuable research tool in epigenetic studies and cancer biology investigations
Apexbio Technology LLC Afatinib (BIBW2992) 439081-18-2 10mM (in 1mL DMSO)
Afatinib (BIBW2992 CAS 439081-18-2) is an irreversible inhibitor targeting receptor tyrosine kinases in the ErbB protein family specifically EGFR (ErbB1) and HER2 (ErbB2) By covalently binding to their kinase domains it suppresses downstream ErbB signaling showing demonstrated inhibition with IC50 values of 0 5 nM for EGFR and 14 nM for HER2 Afatinib blocks EGF-induced phosphorylation and cellular proliferation in multiple EGFR- or HER2-expressing lines including A431 NIH-3T3-HER2 NCI-N87 and BT-474 Research applications include tumor xenograft studies and transgenic lung cancer models evaluating EGFR-dependent oncogenic processes and therapeutic responses
Apexbio Technology LLC EPZ015666 1616391-65-1 10mM (in 1mL DMSO)
EPZ015666 (CAS 1616391-65-1) is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) an enzyme implicated in several cellular pathways including tumorigenesis EPZ015666 inhibits PRMT5 with an IC50 of 22 nM and displays a Ki value of approximately 5 nM It exhibits over 20 000-fold selectivity for PRMT5 relative to other protein methyltransferases tested In mantle cell lymphoma (MCL) cell lines treatment with EPZ015666 reduced methylation levels of the PRMT5 substrate SmD3 and exerted concentration-dependent anti-proliferative effects Additionally EPZ015666 demonstrated dose-dependent tumor growth inhibition in mouse xenograft models of MCL highlighting its potential utility as a molecular tool in cancer biology research
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 4μ8C 14003-96-4 10mM (in 1mL DMSO)
4 8C (CAS 14003-96-4) is a small molecule inhibitor targeting the RNase activity of inositol-requiring enzyme 1 alpha (IRE1 ) an important transmembrane serine/threonine kinase involved in the unfolded protein response (UPR) By selectively blocking IRE1-mediated RNase function 4 8C inhibits downstream UPR gene activation in cell lines exposed to hypoxia or endoplasmic reticulum (ER) stressors including HCT116 colon carcinoma and KP4 pancreatic cancer cells without affecting proliferation or clonogenic survival under these conditions Due to its selective action 4 8C serves as a valuable tool in research investigating ER stress pathways and their roles in cellular adaptation and disease pathology
Apexbio Technology LLC Tadalafil 171596-29-5 10mM (in 1mL DMSO)
Tadalafil (CAS 171596-29-5) also known as IC351 is a selective inhibitor of phosphodiesterase type 5 (PDE5) a primary phosphodiesterase isoenzyme responsible for hydrolyzing cyclic guanosine monophosphate (cGMP) in pulmonary vasculature By competitively and reversibly inhibiting PDE5 tadalafil elevates intracellular cGMP levels thereby inducing vasodilation and attenuating pathological pulmonary arterial constriction Due to high selectivity tadalafil shows minimal inhibition of other PDE isoforms such as PDE1 PDE4 PDE6 PDE7 PDE8 PDE9 and PDE10 It is commonly studied in pulmonary arterial hypertension research and utilized clinically for erectile dysfunction
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 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