Dimethyl Sulfoxide
Apexbio Technology LLC GSK343 1346704-33-3 10mM (in 1mL DMSO)
GSK343 (CAS 1346704-33-3) is a selective SAM-competitive inhibitor targeting the histone lysine methyltransferase EZH2 which is the catalytic component of polycomb repressive complex 2 (PRC2) responsible for trimethylation of histone H3 at lysine 27 (H3K27me3) By competitively inhibiting EZH2 s methyltransferase activity GSK343 disrupts H3K27me3-mediated transcriptional silencing It shows potent inhibitory activity against EZH2 (IC50 4 nM) moderate inhibition against EZH1 (240 nM) but minimal impact on other SAM-dependent enzymes In vitro studies with various cancer cell models confirm its ability to reduce H3K27 trimethylation limit proliferation induce apoptosis promote autophagy and enhance chemosensitivity highlighting its utility as a research tool to study EZH2-related mechanisms
Sigma Aldrich Fine Chemicals Biosciences CryoSOfreeTM DMSO free Cry
We are committed to bringing you Greener Alternative Products which adhere to one or more of The 12 Principles of Greener Chemistry. This product has Inherently Safer Chemistry compared to the standard use of DMSO for cryopreservation of cell cultures. for more information see here.
Apexbio Technology LLC CH5138303 959763-06-5 10mM (in 1mL DMSO)
CH5138303 (CAS 959763-06-5) is a potent inhibitor targeting Heat Shock Protein 90 (HSP90) exhibiting strong binding affinity with a Kd of 0 48 nM HSP90 a molecular chaperone regulates protein folding stability and degradation and maintains oncogenic proteins crucial to tumor cell proliferation CH5138303 effectively reduces protein levels and phosphorylation of HSP90 client proteins including Raf1 AKT EGFR and HER2 in NCI-N87 cancer cells In animal studies using human gastric cancer NCI-N87 xenografts oral administration of CH5138303 demonstrates significant antitumor activity achieving a tumor growth inhibition (TGI) rate of 136% at an ED of 3 9 mg/kg
Medchemexpress LLC S63845 Solution, 10 mM * 1 mL in DMSO
S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
Apexbio Technology LLC Pranlukast 103177-37-3 10mM (in 1mL DMSO)
Pranlukast (CAS 103177-37-3) is a selective antagonist of cysteinyl leukotriene (cysLT) receptors exhibiting its pharmacological action by competitively binding to targeted leukotriene receptor sites It specifically prevents the interaction of endogenous leukotrienes (LTC4 LTD4 LTE4) with corresponding receptors located on pulmonary cell membranes thus reducing leukotriene-driven airway inflammation and bronchoconstriction Binding experiments demonstrate that pranlukast possesses notably greater affinity for LTE4 and LTD4 compared to LTC4 In biomedical research pranlukast is frequently utilized for mechanistic studies and pharmacological modeling of asthma allergic rhinitis and related airway inflammatory conditions
Apexbio Technology LLC 3-Deazaneplanocin A (DZNep) hydrochloride 120964-45-6 10mM (in 1mL DMSO)
3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor targeting histone methyltransferase EZH2 exhibiting inhibitory activity with an IC50 range of 0 08-0 24 M Additionally DZNep inhibits S-adenosylhomocysteine hydrolase (SAHH) at a Ki of 50 pM EZH2 acts as a catalytic subunit of polycomb repressive complex 2 (PRC2) participating in modulation of gene expression via histone methylation Research demonstrates that DZNep suppresses EZH2-dependent gene regulation pathways in cancer cells leading to altered expression of cell-cycle and apoptosis-associated genes DZNep is commonly utilized in epigenetic studies of various tumors and metabolic dysfunction models including AML liver fibrosis and lipid accumulation studies
Apexbio Technology LLC Danusertib (PHA-739358) 827318-97-8 10mM (in 1mL DMSO)
Danusertib (PHA-739358 CAS 827318-97-8) is a pyrrolopyrazole-based aminopyrazole derivative that functions as a pan-inhibitor of aurora kinases prominently targeting aurora B kinase (ABK) It also exhibits inhibitory activity against several other tyrosine kinases including the T315I mutant form RET TRK-A and fibroblast growth factor receptor-1 (FGFR-1) Due to its broad kinase inhibition profile danusertib has demonstrated significant antitumor activity in various xenograft spontaneous and genetically engineered animal models and is thus useful in oncology research involving leukemia and solid tumors
Apexbio Technology LLC SAR245409 (XL765) 1349796-36-6 10mM (in 1mL DMSO)
SAR245409 (XL765 CAS 1349796-36-6) is a selective dual inhibitor of phosphatidylinositol-3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with high potency against PI3K (IC50 9 nM) It suppresses the PI3K/Akt/mTOR signaling cascade by preventing formation of phosphatidylinositol-3 4 5-triphosphate (PIP3) at the cell membrane and downstream phosphorylation of AKT p70S6 kinase and S6 SAR245409 demonstrates antitumor activity in cancer models exhibiting genetic alterations in PI3K pathways enhancing growth suppression and apoptosis It is commonly employed in preclinical studies evaluating PI3K/mTOR-targeted approaches in cancer therapy
Apexbio Technology LLC SAG(Synonyms: Smoothened Agonist, SAG dihydrochloride, Hh-Smo agonist, SAG hydrochloride), 10mM (in 1mL DMSO), CAS: 912545-86-9.
SAG (CAS 912545-86-9) is a synthetic small-molecule agonist targeting the Smoothened (SMO) receptor a GPCR-like protein central to the Hedgehog (Hh) signaling pathway It activates SMO with an EC50 of approximately 3 nM thus stimulating downstream Gli transcription factor activity involved in embryonic development and adult tissue homeostasis At concentrations above 1 M SAG exhibits inhibitory effects on pathway signaling It binds directly to SMO forming an interaction with a reported dissociation constant (K D) around 59 nM SAG is employed in biomedical research notably to mitigate glucocorticoid-induced cerebellar injury in primary mouse neuronal cell cultures
Apexbio Technology LLC Matrine(Synonyms: Sophocarpidine, Matridin, (-)-Matrine, α-Matrine, (−)-α-Matrine, L-Matrine, Kushenin), 10mM (in 1mL DMSO), CAS: 519-02-8.
Matrine (CAS 519-02-8) is an alkaloid derived from plants in the Sophora genus with demonstrated anticancer and anti-inflammatory activities It functions in part through agonism of kappa-opioid and possibly other receptors Matrine inhibits the MNK45 gastric cancer cell line proliferation (IC50 540 g/ml MTT assay) by modifying protein expression profiles (e g NF- B XIAP CIAP p-ERK) In vitro matrine induces apoptosis in NSCLC cells through ROS generation caspase activation and p38 pathway modulation Animal studies suggest therapeutic roles in cardiac injury and sepsis-related lung inflammation
Apexbio Technology LLC EPZ-6438 1403254-99-8 10mM (in 1mL DMSO)
EPZ-6438 is a selective inhibitor targeting EZH2 the catalytic subunit of polycomb repressive complex 2 (PRC2) By competitively binding to EZH2 s S-adenosylmethionine (SAM) pocket EPZ-6438 suppresses EZH2-driven trimethylation of histone H3 lysine 27 (H3K27me3) a key epigenetic modification implicated in transcriptional regulation and oncogenesis This selective inhibition of EZH2 exhibits reduced affinity for EZH1 In biological studies EPZ-6438 has demonstrated anti-tumor activity in preclinical malignant rhabdoid tumor models making it useful for examining EZH2-dependent cancer pathways and epigenetic research
Apexbio Technology LLC Fosaprepitant(Synonyms: Fosaprepitant dimeglumine, Emend IV, L-758298, MK-0517, Fosaprepitant meglumine, Ivemend), 10mM (in 1mL DMSO), CAS: 172673-20-0.
Fosaprepitant (CAS 172673-20-0) also known as MK-0517 or L-758 298 is a selective neurokinin-1 (NK-1) receptor antagonist exerting its pharmacological effects primarily through its active metabolite aprepitant This antagonism blocks substance P-mediated biological effects including vomiting responses In established preclinical models such as the cisplatin-triggered emesis in ferrets fosaprepitant demonstrated activity in mitigating chemotherapy-induced vomiting Given aprepitant s favorable penetration into the central nervous system fosaprepitant exhibits high NK-1 receptor affinity and potentiates antiemetic actions of agents such as dexamethasone and granisetron It is used in combination therapies with 5-HT3 antagonists and corticosteroids for chemotherapy-induced nausea and vomiting (CINV)
Apexbio Technology LLC RK-33 1070773-09-9 10mM (in 1mL DMSO)
RK-33 is a small molecule inhibitor targeting DDX3 an RNA helicase frequently overexpressed in various cancer types including lung cancer DDX3 overexpression correlates with poorer survival outcomes in lung cancer patients suggesting therapeutic relevance Mechanistically RK-33 inhibits DDX3 enzymatic activity thereby disrupting downstream signaling pathways particularly the -catenin-dependent Wnt signaling axis In vitro studies indicate RK-33 induces cell cycle arrest at G1 phase promotes apoptosis and enhances cellular radiosensitivity in DDX3-high expressing cell lines (e g A549 H1299 H23 and H460 IC50 4 4 8 4 M) In preclinical in vivo testing using a Twist1/KrasG12D mouse lung cancer model combined treatment of RK-33 with radiation resulted in reduced tumor growth compared with radiation alone RK-33 serves as a research tool to investigate DDX3 biology and potential therapeutic strategies for cancers with elevated DDX3 expression
Apexbio Technology LLC Fluoxetine HCl(Synonyms: Prozac, Sarafem, Fluoxetine Hydrochloride, Lilly 110140, Fluoxeren, Fluctin), 10mM (in 1mL DMSO), CAS: 56296-78-7.
Fluoxetine HCl (CAS 56296-78-7) is a selective serotonin reuptake inhibitor (SSRI) that specifically blocks presynaptic serotonin (5-HT) transporters resulting in elevated extracellular serotonin levels It modulates serotonergic signaling through inhibition of serotonin-induced membrane currents in cloned 5HT2C receptors exhibiting an IC50 around 20 M and binds 5HT2C receptors expressed in HeLa cells (Ki approximately 65-97 nM) Fluoxetine treatment has been shown in vivo to stimulate neurogenesis and enhance neuronal maturation and synaptic plasticity within rat hippocampus and prefrontal cortex Widely employed in neuroscience research fluoxetine aids in studies of depression stress resilience and neuro-regulatory mechanisms involving serotonergic signaling