Dimethyl Sulfoxide
Apexbio Technology LLC Radezolid 869884-78-6 10mM (in 1mL DMSO)
Radezolid is an oxazolidinone-class antibiotic under investigation targeting Gram-positive bacterial pathogens including methicillin-resistant Staphylococcus aureus (MRSA) By accumulating intracellularly within various host cells such as macrophages epithelial cells and endothelial cells Radezolid disrupts bacterial protein synthesis through inhibition of bacterial ribosomal translation In vitro assessments show antibacterial potency approximately tenfold greater than Linezolid at identical concentrations in infected cell models MIC90 values for MRSA strains indicate enhanced potency relative to Linezolid with MIC90 at approximately 0 5 mg/l compared to 2 0 mg/l for Linezolid Experimental animal models display increased Radezolid accumulation in infected tissues (2 4-fold higher tissue AUC compared to non-infected counterparts) Radezolid is explored in research settings examining complicated skin infections and community-acquired pneumonia (CAP)
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 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 Mocetinostat (MGCD0103, MG0103) 726169-73-9 10mM (in 1mL DMSO)
Mocetinostat (MGCD0103 MG0103 CAS 726169-73-9) is an isotype-selective inhibitor of human histone deacetylases (HDACs) It selectively targets class I HDAC enzymes (HDAC1 HDAC2 HDAC3) and class IV HDAC11 without affecting class II HDACs Mocetinostat inhibits these isoforms with IC50 values of 0 15 mol/L (HDAC1) 0 29 mol/L (HDAC2) 1 66 mol/L (HDAC3) and 0 59 mol/L (HDAC11) resulting in histone hyperacetylation cell cycle arrest and apoptosis in various cancer cell lines It serves as a research tool for studying epigenetic regulation and as a candidate compound for anticancer drug development
Apexbio Technology LLC RG7388 1229705-06-9 10mM (in 1mL DMSO)
RG7388 (CAS 1229705-06-9) is a second-generation selective inhibitor of the MDM2-p53 interaction It functions by blocking the binding between MDM2 and wild-type p53 thereby stabilizing and activating the p53 tumor-suppressor pathway In human cancer cell lines RG7388 shows high potency with reported IC50 values of 6 nM (MDM2 binding assay) and 0 03 M (MTT assay) Preclinical studies demonstrate cell-cycle arrest and apoptosis selectively in wild-type p53-expressing cells and tumor regression in xenograft mouse models including sarcoma and neuroblastoma RG7388 is currently under clinical evaluation for multiple solid and hematologic malignancies
Apexbio Technology LLC YO-01027 (Dibenzazepine, DBZ) 209984-56-5 10mM (in 1mL DMSO)
YO-01027 (Dibenzazepine DBZ CAS 209984-56-5) is a potent inhibitor targeting -secretase a multimeric aspartyl protease involved in the proteolytic cleavage of type I integral membrane proteins notably amyloid precursor protein-like (APPL) proteins and Notch receptors YO-01027 interacts with the N-terminal regions of presenilin dose-dependently inhibiting cleavage of APPL and Notch proteins Research indicates that YO-01027 modulates cell differentiation by suppressing Notch signaling pathways influencing cellular transitions and mucin (MUC16) synthesis illustrating its utility in cell biology and therapeutic studies of Notch-related signaling processes
Apexbio Technology LLC MC1568 852475-26-4 10mM (in 1mL DMSO)
MC1568 (CAS 852475-26-4) is a histone deacetylase (HDAC) inhibitor derived from the (aryloxopropenyl)pyrrolyl hydroxyamide chemical class It selectively targets class II HDAC enzymes particularly class IIa subtypes (HDAC4 HDAC5 HDAC7 HDAC9) inhibiting maize class II HDAC activity with an IC50 of 22 M MC1568 modulates muscle differentiation pathways by reducing MEF2D expression stabilizing HDAC-HDAC3-MEF2D complexes and preventing MEF2D acetylation in cultured myocytes It also interferes with differentiation signals mediated via RAR and PPAR nuclear receptors serving as a valuable tool in epigenetic and cellular differentiation studies
Apexbio Technology LLC Telaprevir (VX-950) 402957-28-2 10mM (in 1mL DMSO)
Telaprevir (VX-950) is an inhibitor that targets the hepatitis C virus (HCV) NS3-4A protease an essential enzyme for HCV replication Structurally derived from the viral NS5A/5B substrate Telaprevir binds to the NS3-4A protease in a covalent reversible manner through a slow-binding and dissociation mechanism thereby interrupting viral polyprotein processing Experimental studies have demonstrated that Telaprevir inhibits genotype 1 (H strain) NS3 protease with a reported inhibition constant (Ki) of approximately 7 nM In HCV replicon cell assays Telaprevir exhibits antiviral activity effectively suppresses viral replication and delays the development of viral resistance showing synergy when combined with interferon-alpha (IFN- ) Telaprevir serves as a research tool for studying antiviral mechanisms and therapeutic combinations in preclinical HCV models
Apexbio Technology LLC (S)-(+)-Ibuprofen(Synonyms: Dexibuprofen, (S)-Ibuprofen, (S)-(+)-2-(4-Isobutylphenyl)propionic acid), 10mM (in 1mL DMSO), CAS: 51146-56-6.
(S)-( )-Ibuprofen (CAS 51146-56-6) is the pharmacologically active enantiomer of the racemic nonsteroidal anti-inflammatory drug (NSAID) ibuprofen Unlike its R(-)-counterpart the S( )-form selectively inhibits cyclooxygenase (COX) enzymes thereby suppressing prostaglandin synthesis at concentrations relevant to clinical settings Due to this stereoselectivity (S)-( )-ibuprofen is widely utilized in biomedical research investigating pain inflammation pathways COX enzyme activity and related drug-target interactions
Apexbio Technology LLC GYY 4137 morpholine salt(Synonyms: GYY4137, Morpholin-4-ium 4-methoxyphenyl(morpholino)phosphinodithioate, GYY-4137), 10mM (in 1mL DMSO), CAS: 106740-09-4.
GYY 4137 morpholine salt (CAS 106740-09-4) is a slow-releasing hydrogen sulfide (H S) donor that exerts biological activity by modulating signaling pathways involved in vasodilation and blood pressure regulation In experimental studies this compound demonstrates the capacity to suppress cellular proliferation induce apoptosis and arrest cell cycle progression Due to these properties GYY 4137 morpholine salt is widely utilized in research investigating hypertension inflammation and cancer biology
Apexbio Technology LLC (+)-MK 801(Synonyms: Dizocilpine, Dizocilpine maleate, MK-801, (+)-MK-801, (+)-Dizocilpine), 10mM (in 1mL DMSO), CAS: 70449-94-4.
( )-MK 801 (CAS 70449-94-4) is a potent selective and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor displaying a Ki of approximately 30 5 nM This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes predominantly localized within the hippocampus In vitro assays utilizing rat cortical slice preparations indicate that ( )-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents Due to these pharmacological properties ( )-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events neurotoxicity convulsions and excitatory neurotransmission pathways
Apexbio Technology LLC Anidulafungin(Synonyms: Eraxis, Ecalta, LY303366, VER-002, Anidulafungin acetate, V-echinocandin, Vicuron echinocandin), 10mM (in 1mL DMSO), CAS: 166663-25-8.
Anidulafungin (CAS 166663-25-8) also known as LY-303366 is a semisynthetic derivative of echinocandin B exhibiting antifungal activity It acts by inhibiting fungal cell wall synthesis through interference with the enzyme -(1 3)-D-glucan synthase In vitro analyses demonstrate that Anidulafungin inhibits various Candida species including C albicans C glabrata C tropicalis and C parapsilosis (MIC90 0 08 0 32 0 32 5 12 g/ml respectively) as well as Aspergillus species (MIC90 0 02 g/ml) Lack of significant efficacy was shown against Cryptococcus neoformans and Blastomyces dermatitidis This compound is useful for research exploring antifungal resistance mechanisms and therapeutics
Apexbio Technology LLC Bay 11-7085(Synonyms: BAY-11-7085, BAY 117085, BAY117085, Bay11-7085, BAY 11 7085, BAY-117085, Bay 11 7085), 10mM (in 1mL DMSO), CAS: 196309-76-9.
Bay 11-7085 (CAS 196309-76-9) is a soluble inhibitor of nuclear factor-kappa B (NF- B) activation It inhibits cell proliferation and promotes apoptosis in various cell types through interference with NF- B signaling pathways Studies have demonstrated that Bay 11-7085 decreases DNA synthesis in endometriotic stromal cells (ECSCs) leading to cell cycle arrest at G0/G1 phase Furthermore treatment with Bay 11-7085 induces apoptosis by downregulating anti-apoptotic proteins such as Bcl-2 and Bcl-XL while enhancing activation of caspase-3 caspase-8 and caspase-9 Bay 11-7085 is commonly employed as a chemical probe in biomedical research on inflammation and apoptosis pathways
Apexbio Technology LLC GW788388 452342-67-5 10mM (in 1mL DMSO)
GW788388 (CAS 452342-67-5) is a selective inhibitor targeting activin receptor-like kinase 5 (ALK5) the type I receptor for transforming growth factor-beta (TGF- ) It inhibits the kinase activity of ALK5 suppressing TGF- -mediated signaling cascades GW788388 demonstrates potent inhibition of ALK5 autophosphorylation with an IC50 of 18 nM leading to decreased Smad2 phosphorylation It also inhibits TGF- -induced epithelial-mesenchymal transition (EMT) cellular proliferation fibrosis and angiogenesis in various cell models such as NMuMG MDA-MB-231 RCC and U2OS In animal studies GW788388 ameliorates renal fibrosis in diabetic db/db mouse models highlighting its utility in investigating TGF- -driven pathophysiological processes