Quinolines and derivatives
Apexbio Technology LLC Rocilinostat (ACY-1215) 1316214-52-4 200mg
Rocilinostat (ACY-1215 CAS 1316214-52-4) is a selective inhibitor of histone deacetylase 6 (HDAC6) HDAC6 enzymatically regulates various cellular processes including protein trafficking cell-cycle progression and cytoskeletal organization and its dysregulated activity is implicated in tumor progression and cancer metastasis Rocilinostat potently inhibits HDAC6 (IC50 5 nM) while showing minimal activity against other HDAC isoforms and sirtuins (IC50 1 M) Preclinical studies using multiple myeloma (MM) cell lines and xenograft mouse models demonstrated rocilinostat can enhance acetylation of -tubulin disrupt protein stability pathways and sensitize cancer cells to proteasome inhibitors such as bortezomib and carfilzomib resulting in increased apoptosis and reduction in tumor growth
Apexbio Technology LLC JNJ-26481585 875320-29-9 200mg
JNJ-26481585 (CAS 875320-29-9) is a small-molecule inhibitor targeting class I histone deacetylases (HDACs) specifically HDAC1 HDAC2 and HDAC3 with reported IC50 values of 0 11 0 33 and 4 8 nM respectively It exhibits potent anti-proliferative activity across various human cancer cell lines including lung breast colon prostate ovarian and brain cancers (IC50 range 3 1 246 nM) Mechanistically JNJ-26481585 induces histone H3 acetylation alleviates HDAC-mediated repression of the p21waf1 cip1 promoter and promotes apoptosis in colorectal cancer cell models Consequently this compound serves as a research tool for cancer epigenetics and therapeutic assessment
Apexbio Technology LLC CUDC-101 1012054-59-9 200mg
CUDC-101 (CAS 1012054-59-9) is a multitargeted small molecule inhibitor that concurrently targets epidermal growth factor receptor (EGFR) HER2 and class I and II histone deacetylases (HDACs) By inhibiting EGFR and HER2 kinases directly and simultaneously blocking HDAC activity CUDC-101 downregulates multiple oncogenic signaling pathways including those mediated by Akt HER3 and MET Preclinical assessments demonstrate that CUDC-101 inhibits growth of diverse tumor cell lines and xenograft models notably including those resistant to EGFR-targeted agents such as lapatinib and erlotinib These characteristics render CUDC-101 valuable for oncology research and drug resistance studies
Apexbio Technology LLC Solanesol 13190-97-1 200mg
Solanesol is a lipophilic terpene alcohol derived from plants in the Solanaceae family characterized by anti-inflammatory neuroprotective and antimicrobial activity In vitro studies indicate solanesol regulates specific signaling pathways implicated in inflammatory responses and neurodegenerative processes possibly through modulation of enzyme activity and intracellular targets Experimental evidence demonstrates solanesol inhibits inflammation-associated enzymes with reported IC50 values typically ranging from low to mid micromolar concentrations depending on cell types and assay conditions This compound is utilized in biochemical research focused on elucidating molecular pathways involved in inflammation-mediated diseases and evaluating therapeutic potential as a neuroprotective agent
Apexbio Technology LLC AS 602801 848344-36-5 200mg
AS 602801 (CAS 848344-36-5) is a selective small-molecule inhibitor targeting c-Jun N-terminal kinase (JNK) a kinase implicated in immune and apoptotic signaling pathways Preclinical studies indicate that AS 602801 suppresses T-cell proliferation and promotes apoptosis altering gene expression in RRMS-derived CD4 and CD8 T-cells and innate receptor expression in RRMS-associated CD11b cells Animal models show beneficial effects in autoimmune disorders and neuronal apoptosis scenarios Thus AS 602801 is investigated primarily for therapeutic potential in multiple sclerosis and fibrotic conditions
Apexbio Technology LLC SM-164 957135-43-2 200mg
SM-164 (CAS 957135-43-2) is a bivalent small molecule mimetic of the endogenous inhibitor Smac designed to antagonize cellular inhibitor of apoptosis proteins (cIAP-1 cIAP-2) and X-linked inhibitor of apoptosis protein (XIAP) By binding specifically to the BIR2 and BIR3 domains of cIAP-1 and XIAP as well as the BIR3 domain of cIAP-2 (Ki of 0 31 nM 0 56 nM and 1 1 nM respectively) SM-164 promotes degradation of cIAP-1 and inhibition of XIAP In tumor cells this leads to caspase activation and TNF -dependent apoptosis SM-164 is utilized in cancer research to investigate apoptosis regulation and anticancer therapy strategies
Apexbio Technology LLC Rucaparib (free base) 283173-50-2 200mg
Rucaparib (free base) (CAS 283173-50-2) also known as AG014699 or PF-01367338 is a pharmacological inhibitor targeting poly(ADP-ribose) polymerase (PARP) a nuclear enzyme centrally involved in DNA damage signaling and base excision repair pathways By impeding PARP activity Rucaparib compromises DNA repair capacity leading to persistent DNA strand breaks as evidenced by increased gamma-H2AX and p53BP1 foci It has demonstrated radiosensitizing properties in prostate cancer cells notably those harboring PTEN deficiency or expressing ETS gene fusion proteins due partly to inhibition of non-homologous end-joining (NHEJ) DNA repair Rucaparib serves as a tool compound in oncology research to study chemosensitization and radiosensitization strategies
Apexbio Technology LLC PF-543 1415562-82-1 200mg
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 MK-8245 1030612-90-8 200mg
MK-8245 (CAS 1030612-90-8) is a potent liver-selective small molecule inhibitor of stearoyl-CoA desaturase (SCD) SCD1 catalyzes fatty acid desaturation and represents a target for treating type II diabetes obesity dyslipidemia and other metabolic disorders MK-8245 demonstrates strong inhibitory activity against rat mouse and human SCD1 with an IC50 of approximately 1 nM and displays liver-specific tissue distribution mediated by organic anion transporting polypeptides (OATPs) Animal studies revealed MK-8245 reduces blood glucose levels and hepatic triglycerides dose-dependently supporting its application in metabolic disease research
Apexbio Technology LLC Tideglusib 865854-05-3 200mg
Tideglusib is a potent selective inhibitor of glycogen synthase kinase-3 (GSK-3 ) functioning through irreversible and ATP-noncompetitive inhibition with reported IC50 of 60 nM Mechanistically Tideglusib binds in a manner independent of ATP leading to sustained enzyme inactivation Preclinical studies utilizing animal models demonstrate Tideglusib s ability to attenuate hyperphosphorylation of Tau protein reduce amyloid plaque accumulation prevent neuronal loss and enhance cognitive performance Currently undergoing clinical investigation Tideglusib has advanced through Phase II studies for Alzheimer s disease (AD) and progressive supranuclear palsy (PSP) exploring therapeutic applicability related to its GSK-3 inhibition activity
Apexbio Technology LLC Cobicistat (GS-9350) 1004316-88-4 200mg
Cobicistat (GS-9350) is a selective inhibitor of cytochrome P450 3A enzyme (CYP3A) showing inhibitory activity with an IC50 ranging from 0 03 to 0 285 M in vitro It lacks intrinsic anti-HIV activity but serves primarily as a pharmacokinetic enhancer used in combination therapy to increase the systemic exposure of HIV-1 protease inhibitors such as atazanavir and darunavir Clinically cobicistat is administered orally to HIV-1-infected adults facilitating optimized dosing regimens Due to its selective CYP3A inhibitory mechanism cobicistat is employed in pharmacokinetic studies and drug-drug interaction investigations related to HIV treatments
Apexbio Technology LLC GSK1838705A 1116235-97-2 200mg
GSK1838705A (CAS 1116235-97-2) is a small molecule inhibitor targeting the kinase activity of insulin-like growth factor-1 receptor (IGF-1R) insulin receptor and anaplastic lymphoma kinase (ALK) It exhibits potent inhibition with IC50 values of 2 0 nM for IGF-1R 1 6 nM for insulin receptor and 0 5 nM for ALK In preclinical research GSK1838705A suppresses proliferation of hematologic malignancy-derived tumor cells including multiple myeloma and Ewing sarcoma lines and inhibits tumor xenograft growth in vivo Additionally despite targeting the insulin receptor it minimally affects glucose homeostasis at effective doses Due to its multi-target kinase inhibitory profile GSK1838705A serves as a promising tool for cancer biology research
Apexbio Technology LLC Ki16198 355025-13-7 200mg
Ki16198 (CAS 355025-13-7) is the methyl ester derivative of Ki16425 and functions as an antagonist of lysophosphatidic acid (LPA) receptors preferentially inhibiting LPA1 and LPA3 receptor subtypes Ki16198 reduces receptor-mediated inositol phosphate production with Ki values of 0 34 M (LPA1) and 0 93 M (LPA3) showing minimal inhibition of LPA2 and no significant activity against LPA4 6 In vitro Ki16198 attenuates LPA-induced proliferation migration invasion and proMMP-9 expression in cancer cells In vivo studies report suppression of pancreatic tumor growth metastasis and ascites formation highlighting its utility in investigating LPA-related cancer progression pathways
Apexbio Technology LLC AMG-900 945595-80-2 200mg
AMG-900 (CAS 945595-80-2) is a small-molecule inhibitor targeting Aurora kinases a group of serine/threonine kinases crucial for mitosis regulation It exhibits potent ATP-competitive inhibitory activity against all three Aurora kinase isoforms resulting in suppression of Aurora-A and Aurora-B autophosphorylation events AMG-900 induces disruption of cellular mitotic processes leading to cell cycle arrest and subsequent apoptotic cell death Preclinically AMG-900 demonstrates activity across multiple tumor cell lines including multidrug-resistant and taxane-resistant variants and inhibits tumor growth in mouse xenograft models suggesting utility for cancer research
Apexbio Technology LLC GSK1070916 942918-07-2 200mg
GSK1070916 (CAS 942918-07-2) is a selective ATP-competitive inhibitor targeting Aurora kinase B and C displaying Ki values of 0 38 nM and 1 5 nM respectively The compound demonstrates marked selectivity over Aurora kinase A with IC50 values of approximately 5 nM (Aurora B) versus 1259 nM (Aurora A) In vitro studies show that GSK1070916 inhibits proliferation of human lung cancer cells (A549) with an EC50 of roughly 7 nM Additionally the compound effectively reduces phosphorylation of histone H3 an Aurora B substrate and exhibits tumor growth inhibition in HL-60 xenograft mouse models GSK1070916 is utilized in tumor biology research investigating Aurora kinase signaling pathways