Dimethyl Sulfoxide
TARGETMOL CHEMICALS INC TRAMETINIB DMSO SOLVATE 200MG
Also available in 10 mg 25 mg 50 mg 100 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 2 nM)purity: 99%
Apexbio Technology LLC Salirasib 162520-00-5 10mM (in 1mL DMSO)
Salirasib (CAS 162520-00-5) chemically known as S-trans trans-farnesylthiosalicylic acid (FTS) is a synthetic inhibitor targeting Ras proteins Structurally mimicking the carboxy-terminal farnesylated cysteine found in Ras Salirasib disrupts Ras localization at the cellular membrane thereby reducing activity of H-ras K-ras and N-ras isoforms Research indicates that Salirasib reduces Ras protein levels by approximately 50% at concentrations of 25 50 M in Panc-1 pancreatic cancer cells In xenograft models it exhibits tumor growth inhibition alone and synergistically with gemcitabine Clinical phase I studies support its continued investigation in solid-tumor therapy recommending a dose of 600 mg/day
Apexbio Technology LLC IOX2(Glycine) 931398-72-0 10mM (in 1mL DMSO)
IOX2(Glycine) (CAS 931398-72-0) is a selective inhibitor targeting hypoxia-inducible factor-prolyl hydroxylase-2 (PHD2) a key enzyme regulating oxygen sensing by mediating hydroxylation of HIF-1 IOX2 exhibits high target specificity demonstrating an IC50 of approximately 21 nM against PHD2 in vitro and negligible inhibition (over 100-fold selectivity) toward related enzymes such as JMJD2 isoforms and the 2OG-oxygenase FIH In RCC4 cells IOX2 at 50 M effectively suppresses HIF-1 hydroxylation highlighting its utility as a pharmacological probe in studying hypoxia signaling pathways and oxygen-dependent cellular responses
Apexbio Technology LLC Bromodomain Inhibitor, (+)-JQ1 1268524-70-4 10mM (in 1mL DMSO)
( )-JQ1 is a selective small-molecule inhibitor targeting BET (bromodomain and extraterminal) protein family members particularly BRD4 It competitively binds the acetyl-lysine recognition domain of BRD4 bromodomains 1 and 2 with reported Kd values of approximately 50 nM and 90 nM respectively By selectively inhibiting BET proteins ( )-JQ1 disrupts transcriptional regulatory processes essential in cancer biology rendering it a useful research tool for examining chromatin remodeling and gene expression patterns associated with tumor pathogenesis Additionally ( )-JQ1 specifically targets the testis-specific bromodomain protein BRDT enabling investigations into male reproductive biology by reversibly impairing spermatogenesis
Apexbio Technology LLC SB202190 (FHPI) 152121-30-7 10mM (in 1mL DMSO)
SB202190 (FHPI CAS 152121-30-7) is a selective MAPK inhibitor targeting specifically the p38 isoforms and with reported IC50 values of approximately 50 nM and 100 nM respectively Through inhibition of p38 signaling SB202190 has been observed to stimulate the proliferation of leukemia cell lines including THP-1 and MV4-11 via activation of ERK and C-Raf phosphorylation pathways Additionally SB202190 modulates cellular responses to genotoxic stress such as hydroxyurea-induced premature chromosome condensation and influences histone acetylation status (Lys5 of histone H4) in plant systems Such activities render SB202190 useful for investigating MAP kinase-dependent pathways in cell proliferation and stress responses
Apexbio Technology LLC BPTES 314045-39-1 10mM (in 1mL DMSO)
BPTES (CAS 314045-39-1) is a selective inhibitor of kidney-type glutaminase (GLS) an enzyme responsible for converting glutamine to glutamate and ammonia It exhibits inhibitory activity against GLS with a reported Ki of approximately 3 M GLS-mediated glutamine metabolism is particularly essential in proliferating and malignant cells BPTES reduces glutamine-to-glutamate conversion in tumor cells diminishing the transamination of pyruvate to alanine as observed in decreased alanine-to-pyruvate ratios in animal models In vitro BPTES inhibits growth by approximately 50% of IDH1-mutant AML cells at 20 M concentration but does not significantly affect wild-type AML cells highlighting its relevance for cancer metabolism research
Apexbio Technology LLC LY2886721 1262036-50-9 10mM (in 1mL DMSO)
LY2886721 (CAS 1262036-50-9) is an orally bioavailable inhibitor of -site amyloid precursor protein cleaving enzyme 1 (BACE1) an aspartyl protease integral to amyloid precursor protein (APP) cleavage and amyloid- (A ) generation LY2886721 inhibits BACE1 activity with an IC50 of approximately 20 3 nM effectively reducing soluble APP and elevating soluble APP in human cell models (HEK293Swe) and neuronal cultures (PDAPP) at IC50 values of 18 7 nM and 10 7 nM respectively In animal models such as PDAPP mice oral LY2886721 administration dose-dependently reduces cerebral A C99 and sAPP levels Due to its BACE1 inhibitory action LY2886721 serves as a valuable tool in Alzheimer s disease research and therapeutic development
Apexbio Technology LLC Linezolid(Synonyms: Zyvox, Zyvoxid, U-100766, PNU-100766, U-100766E, PNU100766, Linezolide), 10mM (in 1mL DMSO), CAS: 165800-03-3.
Linezolid (CAS 165800-03-3) is a synthetic oxazolidinone antimicrobial compound with broad-spectrum activity primarily against Gram-positive bacteria including multi-drug resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA) vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae Linezolid inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit thereby preventing formation of the functional 70S initiation complex In cell-free transcription-translation assays using E coli linezolid demonstrates an IC50 of approximately 1 8 mM Due to its pharmacokinetics and high oral bioavailability linezolid is widely utilized in clinical research related to complicated skin infections and bacterial pneumonia
Apexbio Technology LLC Floxuridine 50-91-9 10mM (in 1mL DMSO)
Floxuridine is an antineoplastic antimetabolite compound functioning through inhibition of thymidylate synthase leading to interference with thymidine nucleotide biosynthesis This interruption induces DNA replication stress characterized by formation of double-strand DNA breaks Floxuridine exposure activates cellular DNA damage response pathways specifically ATR and ATM kinase signaling cascades and leads to the phosphorylation of checkpoint kinase 1 (Chk1) This compound has been widely utilized in oncology research to analyze DNA damage mechanisms cellular proliferation inhibition and apoptosis induction in human tumor cell lines Floxuridine demonstrates antiproliferative activity in cell-based assays with reported IC50 values typically ranging between 50 nM and 500 nM depending on cell line and experimental conditions
Apexbio Technology LLC R428 1037624-75-1 10mM (in 1mL DMSO)
R428 (CAS 1037624-75-1) is a potent selective inhibitor of the receptor tyrosine kinase Axl demonstrating an IC50 of 14 nM In comparison to related kinases such as Abl Mer Tyro3 InsR EGFR HER2 and PDGFR R428 displays greater than 50-fold selectivity for Axl By inhibiting Axl catalytic function R428 disrupts downstream intracellular signaling pathways including Akt phosphorylation cellular invasion pro-inflammatory cytokine production angiogenesis and epithelial-mesenchymal transition mediator expression (e g Snail) Preclinical studies utilizing animal xenograft tumor models indicate its capacity to reduce metastatic tumor burden and extend survival both alone and combined with cisplatin R428 is orally bioavailable and represents a valuable tool for cancer research targeting Axl-driven pathogenesis
Apexbio Technology LLC Calpain Inhibitor II, ALLM 136632-32-1 10mM (in 1mL DMSO)
Calpain inhibitor II (also termed ALLM or CPI-2) is a membrane-permeable inhibitor targeting calpain I calpain II as well as cathepsin L and B Calpain inhibition by this compound can activate apoptosis via caspase-mediated pathways Studies conducted in acute lymphoblastic leukemia (ALL) cell lines (such as ALL-1 RS4 11 JURKAT) and non-Hodgkin s lymphoma (NHL) cells (including RAMOS DAUDI) revealed apoptosis induction at concentrations of 50 100 M Additionally apoptosis triggered by calpain inhibitor II appears independent of tyrosine kinases BTK and LYN Unlike calpain inhibitor I calpain inhibitor II does not influence NF- B signaling nor sensitize tumor cells to TRAIL-induced apoptosis This inhibitor is widely employed in apoptosis-related research and studies exploring calpain-associated cellular pathways