Dimethyl Sulfoxide
Apexbio Technology LLC PF-543 1415562-82-1 10mM (in 1mL DMSO)
PF-543 (CAS 1415562-82-1) is a cell-permeable inhibitor targeting sphingosine kinase 1 (SphK1) an enzyme that phosphorylates sphingosine to sphingosine-1-phosphate (S1P) It displays potent inhibitory activity against SphK1 with an IC50 of 3 6 nM through sphingosine-competitive (non-ATP competitive) binding Treatment of SphK1-overexpressing head and neck cancer (1483) cells led to a ten-fold decrease in S1P levels confirming effective target engagement PF-543 is widely utilized as a research tool in studies investigating SphK1-mediated signaling pathways in cancer biology and immune cell trafficking
Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 10mM (in 1mL DMSO)
Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects
Apexbio Technology LLC MK-5172 1350514-68-9 10mM (in 1mL DMSO)
MK-5172 is a selective inhibitor targeting the hepatitis C virus (HCV) NS3/4A protease an enzyme essential for viral replication The HCV virus genome encodes this protease which cleaves polyprotein precursors enabling functional viral proteins formation during replication MK-5172 inhibits protease activity across multiple HCV genotypes demonstrating IC50 values in enzymatic assays at low nanomolar concentrations In cell-based replicon systems MK-5172 exhibits IC50 values of 2 nM (genotype 1a) 0 5 nM (genotype 1b) 8 nM (genotype 2a) and 13 nM (genotype 3) MK-5172 is utilized in antiviral studies examining various genotype infections viral resistant variants and the dynamics of viral load reductions in experimental chronic infections
Apexbio Technology LLC Riociguat 625115-55-1 10mM (in 1mL DMSO)
Riociguat (CAS 625115-55-1) chemically known as BAY 63-2521 is a small-molecule stimulator of soluble guanylate cyclase (sGC) It directly activates sGC independently and also enhances the enzyme s sensitivity to nitric oxide (NO) leading to elevated cyclic guanosine monophosphate (cGMP) levels Elevated cGMP induces smooth muscle relaxation and vasodilation Riociguat has been examined clinically for potential therapeutic roles in chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH)
Apexbio Technology LLC CVT-313 199986-75-9 10mM (in 1mL DMSO)
CVT-313 (CAS 199986-75-9) is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) an enzyme essential for G1/S transition during cell cycle progression By targeting CDK2 CVT-313 effectively reduces hyperphosphorylation of retinoblastoma protein (Rb) leading to cell cycle arrest at the G1/S boundary In vitro studies with MRC-5 fibroblasts demonstrated significant growth inhibition Additionally CVT-313 induces apoptosis in diffuse large B-cell lymphoma by diminishing phosphorylation of Rb at T821 and downregulating anti-apoptotic protein Mcl-1 In animal models of arterial restenosis CVT-313 significantly reduces neointimal proliferation indicating potential utility for proliferative disorders research
Apexbio Technology LLC MLN120B 783348-36-7 10mM (in 1mL DMSO)
MLN120B (CAS 783348-36-7) is a small molecule inhibitor targeting the beta subunit of I B kinase (IKK ) an enzyme integral to the NF- B signaling pathway IKK mediates phosphorylation and subsequent degradation of the NF- B inhibitor I B thereby activating NF- B-dependent transcription involved in inflammatory and immune responses MLN120B inhibits IKK -catalyzed phosphorylation of I B (IC50 20 M) attenuating NF- B activation in multiple myeloma cell lines (RPMI 8226 INA 6 MM 1S) and reducing inflammation-induced joint damage in animal arthritis models Consequently MLN120B serves as a research tool in studying NF- B signaling-mediated disorders
Apexbio Technology LLC SOTRASTAURIN AEB071 1ML DMSO
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 BI6727 VOLASERTIB1ML DMSO
BI6727 (Volasertib CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk) primarily targeting Plk1 with an IC50 of 0 87 nM and showing lower potency towards Plk2 (IC50 5 nM) and Plk3 (IC50 56 nM) Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types representing a potential therapeutic target BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116 EC50 23 nM) lung (NCI-H460 EC50 21 nM) melanoma (BRO EC50 11 nM) and hematologic cancer (GRANTA EC50 15 nM) In vivo BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models
Apexbio Technology LLC BREFELDIN A 10MM IN 1ML DMSO
Brefeldin A (CAS 20350-15-6) commonly abbreviated as BFA is a small-molecule inhibitor targeting ATPase activity with a reported IC50 of approximately 0 2 M Its primary mechanism of action involves disruption of intracellular vesicle transport by blocking protein trafficking from the endoplasmic reticulum (ER) to the Golgi apparatus and inhibiting GTP/GDP exchange Through these activities BFA reduces ATP-mediated vesicular exocytosis thereby diminishing stimulus-dependent hyperalgesia Additionally it induces endoplasmic reticulum stress and promotes p53 expression in tumor cell models like MCF-7 and HeLa ultimately enhancing apoptosis in colorectal cancer cells (HCT116) BFA is widely employed as a pharmacological tool in cellular biology research to study protein secretion vesicular transport dynamics and ER stress pathways
Apexbio Technology LLC DINACICLIB SCH727965 1ML DMSO
Dinaciclib (SCH727965 CAS 779353-01-4) is a small-molecule inhibitor targeting cyclin-dependent kinases (CDKs) specifically CDK1 CDK2 CDK5 and CDK9 It exhibits inhibitory potencies with IC50 values of 3 nM for CDK1 1 nM for CDK2 and CDK5 and 4 nM for CDK9 By suppressing CDK activity dinaciclib interrupts cell cycle progression reduces phosphorylation of retinoblastoma (Rb) protein and triggers apoptosis In addition dinaciclib interacts with the acetyl-lysine binding regions within bromodomains Currently in clinical phases I/II it demonstrates antitumor activity both in vitro and in animal models highlighting its potential applicability in oncology research
Apexbio Technology LLC TIRAPAZAMINE 10MM IN 1ML DMSO
Tirapazamine (CAS 27314-97-2) also known as SR259075 Win59075 or SR4233 is an investigational anticancer agent selectively activated under hypoxic conditions characteristic of solid tumors The compound is bioreduced in hypoxic tumor microenvironments to cytotoxic free radicals leading to cellular damage Tirapazamine downregulates hypoxia-inducible factor-1 (HIF-1 ) thereby influencing pathways associated with tumor adaptive mechanisms to hypoxia Combined treatment with tirapazamine and topoisomerase I inhibitors (such as SN-38 the active metabolite of irinotecan) enhances apoptosis via mitochondria-mediated caspase activation and weakened DNA repair signaling Preclinical investigations including hepatocellular carcinoma xenografts confirm this enhanced tumor suppression Clinical trials evaluating tirapazamine s anticancer efficacy are ongoing
Apexbio Technology LLC -MK 801 10MM IN 1ML DMSO
( )-MK 801 (CAS 70449-94-4) is a potent selective and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor displaying a Ki of approximately 30 5 nM This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes predominantly localized within the hippocampus In vitro assays utilizing rat cortical slice preparations indicate that ( )-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents Due to these pharmacological properties ( )-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events neurotoxicity convulsions and excitatory neurotransmission pathways
Apexbio Technology LLC ASC-J9 10MM IN 1ML DMSO
ASC-J9 (CAS 52328-98-0) is a small-molecule degrader targeting androgen receptor (AR) By promoting degradation of full-length AR and splice variants such as AR3/fAR ASC-J9 inhibits androgen receptor signaling pathways involved in castration-resistant prostate cancer (CRPC) progression and metastatic behavior ASC-J9 interferes with AR-dependent transcriptional modulation and AR-independent signaling pathways notably inhibiting STAT3 phosphorylation and CCL2 chemokine secretion thus reducing macrophage infiltration and prostate cancer invasiveness Research indicates ASC-J9 may represent an alternative therapeutic strategy for CRPC treatment and metastasis prevention
Apexbio Technology LLC S--IBUPROFEN 10MM IN 1ML DMSO
(S)-( )-Ibuprofen (CAS 51146-56-6) is the pharmacologically active enantiomer of the racemic nonsteroidal anti-inflammatory drug (NSAID) ibuprofen Unlike its R(-)-counterpart the S( )-form selectively inhibits cyclooxygenase (COX) enzymes thereby suppressing prostaglandin synthesis at concentrations relevant to clinical settings Due to this stereoselectivity (S)-( )-ibuprofen is widely utilized in biomedical research investigating pain inflammation pathways COX enzyme activity and related drug-target interactions
Apexbio Technology LLC ETONOGESTREL 10MM IN 1ML DMSO
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