Dimethyl Sulfoxide
Apexbio Technology LLC AZD2461 1174043-16-3 10mM (in 1mL DMSO)
AZD2461 (CAS 1174043-16-3) is a novel small-molecule inhibitor of poly(ADP-ribose) polymerase (PARP) exhibiting potency with an IC50 of 5 nM PARP enzymes are pivotal regulators of DNA repair and apoptosis-associated processes In breast cancer cell lines such as SKBR-3 and MCF-7 AZD2461 reduces cell viability in a concentration- and time-dependent manner arresting cells predominantly in the G2 phase In BRCA1-deficient mouse KB1P tumors AZD2461 disrupts PARP activity regardless of P-glycoprotein-mediated resistance to other inhibitors like olaparib highlighting its utility in overcoming drug resistance and elucidating DNA repair pathways in cancer research
Sigma Aldrich Fine Chemicals Biosciences Dimethyl sulfoxide ACS reagent, >=99.9% | 67-68-5 | MFCD00002089 | 500ML
Dimethyl sulfoxide ACS reagent, >=99.9% | Purity: >=99.9% | Mol Wt: 78.13 | 67-68-5 | MFCD00002089 | 500ML
Apexbio Technology LLC Z-YVAD-FMK 210344-97-1 10mM (in 1mL DMSO)
Z-YVAD-FMK (CAS 210344-97-1) is a cell-permeable irreversible inhibitor of caspase-1 By inhibiting caspase-1 activity it interferes with caspase-mediated signaling cascades involved in cell apoptosis and cytokine maturation In Caco-2 cells Z-YVAD-FMK reduces butyrate-induced growth inhibition and fully abrogates butyrate s effects at 100 mol/L Additionally in MyD88-deficient murine bone marrow dendritic cells Z-YVAD-FMK effectively blocks alum-induced caspase-1 activation and subsequent IL-1 release It serves as a valuable research tool for investigating caspase-dependent apoptotic pathways and inflammatory responses
Apexbio Technology LLC PF-562271 HCl 939791-41-0 10mM (in 1mL DMSO)
PF-562271 HCl (CAS 939791-41-0) is a potent ATP-competitive reversible inhibitor targeting focal adhesion kinase (FAK) and its homolog proline-rich tyrosine kinase 2 (Pyk2) It inhibits FAK and Pyk2 enzymatic activity with reported IC50 values of 1 5 nmol/L and 14 nmol/L respectively FAK is a non-receptor tyrosine kinase regulating cell adhesion migration and growth while Pyk2 shares structural similarity to FAK In animal models of cancer PF-562271 reduces tumor progression and metastatic spread with dose-dependent suppression of FAK phosphorylation (EC50 93 ng/mL) Thus PF-562271 serves as an important tool for investigating FAK/Pyk2-mediated pathways in oncology research
Apexbio Technology LLC Nanaomycin A 52934-83-5 10mM (in 1mL DMSO)
Nanaomycin A is a selective inhibitor targeting DNA methyltransferase 3B (DNMT3B) with an IC50 of approximately 500 nM It acts by specifically inhibiting DNMT3B-mediated DNA methylation without notably affecting DNMT1 activity In cell-based studies employing cancer cell lines such as HCT116 A549 and HL60 treatment with Nanaomycin A reduced global DNA methylation levels and reactivated transcription of tumor suppressor genes previously silenced via promoter hypermethylation Its use in epigenetics-related research includes quantitative assessment of DNMT3B function investigation of DNA methylation regulation mechanisms and evaluation of gene reactivation consequent to DNMT3B inhibition
Cayman Chemical DMSO asy Reagent 1mL
A DPP-9 inhibitor (IC50 0.0034 UM) selective for DDP-9 over DPP-8 DPP-4 DPP-2 FAP and prolyl endopeptidase (IC50s 0.6 >10 >5 10 and >10 UM respectively) induces LDH release from THP-1 and HL-60 leukemia cells at 10 UM
Apexbio Technology LLC Dapivirine (TMC120) 244767-67-7 10mM (in 1mL DMSO)
Dapivirine (TMC120) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting HIV-1 viral replication By binding directly to HIV-1 reverse transcriptase dapivirine inhibits viral RNA-dependent DNA polymerase activity thus blocking viral DNA synthesis Dapivirine demonstrates activity against HIV-1 reverse transcriptase with reported IC50 values in the low nanomolar range (approximately 1-10 nM) Due to its molecular specificity and promising in vitro antiviral profile dapivirine is widely utilized in biomedical research exploring topical prevention strategies particularly in the development of vaginal microbicides aimed at reducing HIV transmission
Apexbio Technology LLC Etodolac 41340-25-4 10mM (in 1mL DMSO)
Etodolac (CAS 41340-25-4) is a selective cyclooxygenase-2 (COX-2) inhibitor belonging to the class of non-steroidal anti-inflammatory drugs (NSAIDs) It exhibits inhibitory activity against COX-2 with an IC50 of 53 5 nM Etodolac is commonly utilized for research involving inflammatory conditions such as osteoarthritis and rheumatoid arthritis In isolated rabbit articular chondrocytes stimulated with TNF Etodolac prevented apoptotic cell shrinkage and suppressed caspase-3/7 activation Conversely in human malignant rhabdoid tumor cells (FRTK-1) Etodolac induced apoptosis in a dose-dependent manner increasing activities of caspase-3 -8 and -9
Apexbio Technology LLC Sephin1 13098-73-2 10mM (in 1mL DMSO)
Sephin1 (CAS 13098-73-2) is a selective inhibitor of PPP1R15A a regulatory subunit of protein phosphatase 1 involved in the regulation of stress-induced eIF2 dephosphorylation Under endoplasmic reticulum (ER) stress phosphorylated eIF2 attenuates protein synthesis preventing accumulation of misfolded proteins By inhibiting PPP1R15A Sephin1 sustains eIF2 phosphorylation extending translational attenuation during ER stress In cell assays Sephin1 selectively disrupts PPP1R15A-PP1c complexes without affecting PPP1R15B-mediated complexes In mouse models harboring misfolded protein mutations (e g MPZ or SOD1) Sephin1 administration mitigates molecular cellular and functional deficits thus relevant for proteostasis-related disease studies
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 Sotrastaurin (AEB071)(Synonyms: AEB071, Sotrastaurin, PKC inhibitor AEB071, PKC inhibitor Sotrastaurin, Sotrastaurin base, AEB-071), 10mM (in 1mL DMSO), CAS: 425637-18-9.
Sotrastaurin (AEB071 CAS 425637-18-9) is a small-molecule inhibitor targeting protein kinase C (PKC) with inhibitory activity against classical and novel PKC isoforms PKC plays an integral role in immune cell signaling influencing T-cell activation proliferation and cytokine synthesis Sotrastaurin blocks PKC-mediated pathways thereby suppressing T-cell activation proliferation IL-2 mRNA expression and NK-cell function as demonstrated in ex vivo lymphocyte assays Due to its immunoregulatory properties Sotrastaurin has potential therapeutic applications in autoimmune conditions including psoriasis
Apexbio Technology LLC Brassinolide 72962-43-7 10mM (in 1mL DMSO)
Brassinolide (CAS 72962-43-7) is a naturally occurring steroidal plant growth regulator It influences various physiological processes in plants including stem elongation leaf differentiation flower formation and fruit development In vitro studies indicated that brassinolide induces apoptosis in human prostate cancer PC-3 cells characterized by increased caspase-3 activity and decreased Bcl-2 protein expression In animal models brassinolide reduced blood glucose levels in diabetic rats demonstrating non-dose-dependent hypoglycemic effects without observed toxicity Brassinolide is valuable in research related to cancer cell apoptosis and glucose metabolism regulation
Apexbio Technology LLC CO-1686 (AVL-301) 1374640-70-6 10mM (in 1mL DMSO)
CO-1686 (AVL-301 CAS 1374640-70-6) is an orally delivered irreversible small molecule inhibitor targeting mutated epidermal growth factor receptor (EGFR) It functions by forming a covalent bond at cysteine 797 in the ATP-binding domain of EGFR selectively inhibiting mutant variants such as L858R/T790M with reported IC50 values below 0 51 nM CO-1686 preferentially targets mutant EGFR over wild-type demonstrating approximately 22-fold selectivity Preclinical studies using non-small cell lung cancer (NSCLC) cell lines and xenograft models carrying EGFR mutations showed potent anti-proliferative and tumor regression effects Thus CO-1686 represents a valuable research tool in studying mutant EGFR-mediated oncogenesis
Apexbio Technology LLC Tolcapone 134308-13-7 10mM (in 1mL DMSO)
Tolcapone (CAS 134308-13-7) is an orally bioavailable reversible small-molecule inhibitor targeting catechol-O-methyltransferase (COMT) Acting through competitive inhibition tolcapone structurally incorporates a catechol moiety with electron-withdrawing substituents facilitating anionic formation that binds potently to COMT s catalytic site (reported IC50 of approximately 36 nM in rat liver assays) By competitively occupying this active site tolcapone prevents the enzymatic methylation of endogenous catechols such as levodopa thus prolonging levodopa s bioavailability Tolcapone is primarily investigated as adjunctive therapeutic agent in Parkinson s disease research enabling reduced levodopa dosage while enhancing symptomatic control