Dimethyl Sulfoxide
Apexbio Technology LLC SKI II 312636-16-1 10mM (in 1mL DMSO)
SKI II (CAS 312636-16-1) is a small-molecule inhibitor of sphingosine kinase (SK) an enzyme involved in converting sphingosine into sphingosine-1-phosphate (S1P) SKI II inhibits SK activity with an IC50 of 0 5 M through a mechanism independent of competition at the ATP-binding site Selectivity assessments showed no inhibitory effect against human kinases ERK2 PKC-I or PI3K Cellular assays demonstrate that SKI II effectively inhibits endogenous SK reducing S1P synthesis and subsequently suppressing proliferation and inducing apoptosis in various cancer cell lines including MDA-MB-231 T-24 MCF-7 and MCF-7/VP cells
Apexbio Technology LLC TIC10 41276-02-2 10mM (in 1mL DMSO)
TIC10 (TRAIL-inducing compound 10) is a small molecule inhibitor with oral bioavailability capable of penetrating the blood-brain barrier It functions primarily by simultaneously inhibiting Akt and ERK pathways resulting in Foxo3a nuclear translocation and transcriptional activation of TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) TRAIL is involved in apoptosis induction in cancer cells often compromised during tumor progression TIC10 triggers the expression of TRAIL independently of p53 status enabling apoptosis in diverse cancer cell types In preclinical xenograft models and orthotopic glioblastoma studies TIC10 has demonstrated TRAIL-mediated antitumor activity supporting its use in cancer biology research and therapeutic investigations
Apexbio Technology LLC MK-5108 (VX-689) 1010085-13-8 10mM (in 1mL DMSO)
MK-5108 (VX-689 CAS 1010085-13-8) is a selective inhibitor targeting Aurora A kinase (AAK) functioning through competitive interaction with its ATP-binding pocket It exhibits sub-nanomolar inhibition of Aurora A kinase (IC50 0 064 nM) and displays additional inhibitory activity against Aurora B and Aurora C kinases (IC50 14 nM and IC50 12 nM respectively) MK-5108 has been extensively studied in cancer research contexts demonstrating antiproliferative activity across various tumor types including breast cervical colorectal ovarian and pancreatic cancers
Apexbio Technology LLC Everolimus (RAD001) 159351-69-6 10mM (in 1mL DMSO)
Everolimus (RAD001) is an orally bioavailable small-molecule inhibitor targeting mammalian target of rapamycin (mTOR) an integral serine/threonine kinase regulating cell proliferation metabolism and survival within the PI3K/Akt pathway Everolimus binds intracellularly to the immunophilin FKBP12 the resulting complex subsequently interacts directly with mTOR inhibiting its kinase activity thereby reducing downstream phosphorylation of S6 kinase 1 (S6K1) and the eukaryotic initiation factor 4E-binding protein (4EBP) Functionally Everolimus exerts immunosuppressive properties used clinically to prevent organ transplant rejection and demonstrates antitumor activity against several malignancies including renal cell carcinoma and basal cell carcinoma Commonly utilized in cancer research Everolimus inhibits mTOR with IC50 values reported in the low nanomolar range ( 1 3 nM)
Apexbio Technology LLC Q-VD(OMe)-OPh 10mM (in 1mL DMSO)
Q-VD(OMe)-OPh is a pan-caspase inhibitor structurally identified as quinolyl-valyl-O-methylaspartyl-[2 6-difluorophenoxy]-methyl ketone As a broad-spectrum inhibitor Q-VD(OMe)-OPh reversibly targets multiple caspases involved in apoptotic signaling including initiator caspases (such as caspases 8 9 10 and 12) and executioner caspases (such as caspase 3) thereby blocking intrinsic extrinsic and endoplasmic reticulum-mediated apoptotic pathways In recombinant enzyme assays this inhibitor displays nanomolar-range IC values against caspases 1 3 8 and 9 Due to minimal cytotoxicity at tested concentrations Q-VD(OMe)-OPh serves as a tool compound in apoptosis-related biomedical research applied broadly for dissecting caspase-dependent apoptotic mechanisms and evaluating cytoprotective strategies
Apexbio Technology LLC Temsirolimus 162635-04-3 10mM (in 1mL DMSO)
Temsirolimus (CCI-779) is an ester analog of rapamycin functioning as an inhibitor of the mammalian target of rapamycin (mTOR) The compound suppresses mTOR signaling pathways thus inhibiting cellular proliferation and growth In preclinical studies on breast cancer cell lines Temsirolimus displayed inhibitory activities with reported IC50 values of 0 6 nM in BT-474 cells 0 7 nM in MDA-MB-468 and SKBR-3 cells and 50 nM in MCF-7 cells It has been examined in xenograft models of tumors with PTEN mutations and multiple myeloma for investigating pathways related to cell-cycle progression and proliferation regulated by mTOR
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 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 GDC-0941 957054-30-7 10mM (in 1mL DMSO)
GDC-0941 (CAS 957054-30-7) is a selective small-molecule inhibitor of class I phosphoinositide 3-kinase (PI3K) a critical component involved in the PI3K/Akt signaling pathway frequently dysregulated in cancer By competitively binding to the ATP-binding site of PI3K GDC-0941 inhibits generation of the downstream signaling molecule phosphatidylinositol-3 4 5-trisphosphate (PIP3) Exhibiting high selectivity against p110 / (IC50 approx 3 nM) and moderate selectivity for p110 (33 nM) and p110 (75 nM) GDC-0941 has demonstrated antiproliferative activity across diverse tumor cell lines in vitro (e g A2780 PC3 U87MG) and tumor growth inhibition in xenograft cancer models supporting its utility in cancer research
Apexbio Technology LLC Dorsomorphin 2HCl 1219168-18-9 10mM (in 1mL DMSO)
Dorsomorphin 2HCl (CAS 1219168-18-9) is a small-molecule inhibitor targeting BMP signaling through selective blockade of BMP type I receptors ALK2 ALK3 and ALK6 It prevents phosphorylation of downstream effectors SMAD1/5/8 with an IC50 of approximately 0 47 mM Originally identified by zebrafish phenotypic screening as a disruptor of embryonic dorsoventral patterning Dorsomorphin has been employed to dissect BMP-regulated pathways in iron homeostasis significantly affecting hepcidin expression and iron metabolism in vitro and in vivo It is widely utilized in mechanistic studies of BMP function and signaling regulation
Apexbio Technology LLC SRT1720 HCl 1001645-58-4 10mM (in 1mL DMSO)
SRT1720 HCl is a small molecule activator of SIRT1 exerting more potent activation than resveratrol It functions through a SIRT1- and PGC-1 -dependent mechanism modulating mitochondrial oxidative metabolism and insulin sensitivity The compound has demonstrated activity in regulating cell growth and apoptosis in multiple myeloma (MM) cells without notably affecting normal cell viability Its antitumor properties relate to activation of caspase-8 caspase-9 caspase-3 and PARP enhancement of reactive oxygen species generation induction of ATM/CHK2 signaling suppression of NF- B signaling and reduction of VEGF-induced migration SRT1720 is utilized in biomedical research to investigate metabolic pathways tumor biology and potential sensitization effects to chemotherapy agents
Apexbio Technology LLC Pepstatin A 26305-03-3 10mM (in 1mL DMSO)
Pepstatin A is a pentapeptide functioning as an inhibitor targeting aspartic proteases including pepsin renin HIV protease and cathepsin D It inhibits human renin and HIV protease with IC50 values of approximately 15 M and 2 M respectively and shows inhibitory activity toward pepsin and cathepsin D at IC50 values below 5 M and 40 M Mechanistically Pepstatin A acts through binding to the catalytic site of aspartic proteases restricting proteolytic activity In biomedical research it is utilized to study viral protein processing osteoclast differentiation mediated by cathepsins and as a standard tool in enzyme inhibition assays examining aspartic protease function
Apexbio Technology LLC Pracinostat (SB939) 929016-96-6 10mM (in 1mL DMSO)
Pracinostat (SB939 CAS 929016-96-6) is an orally bioavailable inhibitor of histone deacetylases (HDAC) preferentially targeting class I II and IV HDACs with substantially lower affinity for class III enzymes By inhibiting these enzymes pracinostat promotes accumulation of acetylated histone H3 and acetylated -tubulin subsequently upregulating cell cycle regulator p21 In preclinical investigations SB939 demonstrated antiproliferative activity in various tumor cell lines including colon ovarian prostate cancers acute myeloid leukemia (AML) and B-cell lymphoma highlighting its potential utility in oncology research
Apexbio Technology LLC Meptazinol HCl 59263-76-2 10mM (in 1mL DMSO)
Meptazinol HCl also chemically known as WY-22811 hydrochloride is a centrally acting analgesic agent characterized as a partial agonist at the 1 opioid receptor Structurally it belongs to the synthetic opioid family and interacts selectively with opioid receptors in the central nervous system to modulate pain transmission Its partial agonist properties allow for analgesic activity with generally reduced risk of respiratory depression compared to full opioid agonists making it a useful compound in pharmacological studies examining opioid receptor activation modulation and analgesic effects In biomedical research settings Meptazinol HCl is commonly employed to investigate pain management mechanisms opioid receptor signaling pathways receptor selectivity profiles and analgesia-related side effect mitigation
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