Dimethyl Sulfoxide
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 Betaxolol HCl 63659-19-8 10mM (in 1mL DMSO)
Betaxolol HCl (CAS 63659-19-8) is a selective inhibitor targeting the adrenergic receptor It demonstrates antagonist activity by competitively binding and inhibiting this receptor subtype which plays a significant role in cardiovascular regulation Betaxolol exhibits an IC value of approximately 6 M indicative of moderate inhibitory potency In biomedical research betaxolol serves as a pharmacological tool to investigate receptor signaling pathways and their involvement in conditions such as hypertension arrhythmias and cardiovascular disorders
Apexbio Technology LLC Bexarotene 153559-49-0 10mM (in 1mL DMSO)
Bexarotene is a synthetic selective agonist for retinoid X receptors (RXRs) a subclass of nuclear hormone receptors involved in the regulation of gene transcription Upon binding to RXRs Bexarotene modulates the expression of target genes associated with cell differentiation proliferation and apoptosis Due to this mechanism Bexarotene is commonly employed in research investigating tumor growth inhibition cellular differentiation pathways and apoptosis induction Researchers also frequently utilize this retinoid derivative to elucidate RXR-mediated signaling pathways in oncology and to explore potential therapeutic applications for various malignancies
Apexbio Technology LLC XL-888 1149705-71-4 10mM (in 1mL DMSO)
XL-888 (CAS 1149705-71-4) is an orally bioavailable small molecule inhibitor targeting heat shock protein 90 (HSP90) It selectively inhibits HSP90 and HSP90 with IC50 values of 22 nM and 44 nM respectively while exhibiting markedly weaker inhibition against a panel of other kinases Structural analyses indicated XL-888 binds HSP90 via hydrogen bonding interactions involving the Asp93 residue In tumor cell assays XL-888 potently suppresses proliferation with IC50 values in the range of 0 1-45 5 nM XL-888 is used in oncology research particularly for studying resistance mechanisms to targeted therapies
Apexbio Technology LLC Flucytosine 2022-85-7 10mM (in 1mL DMSO)
Flucytosine also known as 5-Fluorocytosine (5-FC) is a fluorinated pyrimidine analogue with antifungal properties It exerts its biological activity by penetrating fungal cells and undergoing intracellular conversion into 5-fluorouracil (5-FU) via cytosine deaminase Subsequently 5-FU metabolites inhibit nucleic acid synthesis interfering with fungal RNA and DNA synthesis pathways thus blocking cellular proliferation In laboratory experiments Flucytosine is commonly utilized for antifungal susceptibility assays fungal growth inhibition studies as well as research into antifungal resistance mechanisms The typical reported in vitro antifungal activity displays IC50 values ranging from approximately 0 12 to 8 g/mL depending on fungal species and experimental conditions
Apexbio Technology LLC A66 1166227-08-2 10mM (in 1mL DMSO)
A66 (CAS 1166227-08-2) is a selective inhibitor of the p110 catalytic subunit of class I phosphatidylinositol-4 5-bisphosphate 3-kinase (PI3K) with an IC50 of 32 nM This compound specifically decreases phosphorylation of Akt/PKB and downstream S6K at Thr389 in various cell models including PIK3CA-mutant H1047R cell lines C2C12 myoblasts and 3T3-L1 adipocytes In animal studies A66 reduces tumor growth in xenograft models and improves insulin sensitivity under chronic metabolic stress highlighting its utility in research on PI3K signaling in cancer and metabolic disease
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 Nilotinib(AMN-107) 641571-10-0 10mM (in 1mL DMSO)
Nilotinib (AMN-107 CAS 641571-10-0) is an orally bioavailable selective inhibitor targeting the BCR-ABL tyrosine kinase Derived structurally from imatinib nilotinib inhibits both wild-type (WT p210) and mutant forms (E281K E292K F317L M351T F486S) of BCR-ABL reducing their autophosphorylation activity with IC50 values ranging from 20 to 42 nM It also exhibits substantial inhibitory activity against activated KIT mutants (e g V560del K642E) and various KIT double mutations and effectively suppresses PDGFR and PDGFR kinases Nilotinib is utilized extensively in research related to chronic myeloid leukemia and gastrointestinal stromal tumors involving kinase-driven pathologies
Apexbio Technology LLC THZ1 1604810-83-4 10mM (in 1mL DMSO)
THZ1 (CAS 1604810-83-4) is a covalent inhibitor of cyclin-dependent kinase 7 (CDK7) targeting specifically the cysteine residue C312 outside its kinase domain It exhibits potent inhibition with an IC50 of 3 2 nM against CDK7 in kinase binding assays In cellular studies THZ1 suppresses proliferation of Jurkat and Loucy T-cell acute lymphoblastic leukemia (T-ALL) cell lines (IC50 50 nM and 0 55 nM respectively) by disrupting CDK7-mediated signaling transcriptional regulation mediated by RUNX1 and RNA polymerase II CTD phosphorylation Thus THZ1 is utilized in cancer research to investigate transcriptional dysregulation in malignancies
Apexbio Technology LLC Proparacaine HCl 5875-06-9 10mM (in 1mL DMSO)
Proparacaine HCl (CAS 5875-06-9) is a small-molecule antagonist of voltage-gated sodium channels By inhibiting sodium ion entry through these channels Proparacaine HCl effectively suppresses action potential generation and neuronal signaling Assays demonstrate an ED50 value of approximately 3 4 mM Due to its sodium channel inhibition Proparacaine HCl is utilized in scientific research to study neuronal excitability ion channel function and related electrophysiological processes