Dimethyl Sulfoxide
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 Olaparib (AZD2281, Ku-0059436) 763113-22-0 10mM (in 1mL DMSO)
Olaparib (AZD2281 Ku-0059436 CAS 763113-22-0) is a selective inhibitor of poly(ADP-ribose) polymerase-1 and -2 (PARP-1/2) By targeting PARP enzymes involved in DNA repair Olaparib specifically inhibits the proliferation of BRCA-deficient tumor cell lines and enhances radiosensitivity in experimental tumor models In xenograft mouse models of non-small cell lung carcinoma (NSCLC) Olaparib has been shown to elevate radiation sensitivity and improve tumor perfusion The compound is widely utilized in studies focused on DNA damage responses tumor radiosensitization and targeted therapy strategies for BRCA-associated cancers
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 Preladenant 377727-87-2 10mM (in 1mL DMSO)
Preladenant is a potent and selective antagonist targeting the adenosine A2A receptor (Ki 1 1 nM) developed from structural modifications of SCH 58261 Structurally it is a methoxy derivative carrying enhanced affinity and selectivity towards human and rat A2A receptors over A1 A2B and A3 subtypes Mechanistically Preladenant competitively blocks A2A receptor-mediated adenylate cyclase activation In preclinical studies Preladenant reduces Parkinsonian symptoms in primate and rodent models alone or in combination with L-Dopa thus widely employed in experimental research for Parkinson s disease and associated movement disorders
Apexbio Technology LLC Apatinib 10mM (in 1mL DMSO)
B2303 is a synthetic small molecule designed for biomedical research acting primarily as an inhibitor targeting specific intracellular signaling pathways involved in cell proliferation and survival It modulates intracellular signaling cascades implicated in pathological conditions such as inflammation cancer progression and aberrant cell growth B2303 serves as a molecular probe suitable for investigating intracellular processes and as a tool for dissecting signal transduction mechanisms enabling researchers to explore therapeutic targets for various diseases
Apexbio Technology LLC Chlorothiazide 58-94-6 10mM (in 1mL DMSO)
Chlorothiazide is a sulfonamide-derived diuretic compound known for its inhibitory action on carbonic anhydrase enzymes It functions by reducing sodium and chloride ion reabsorption via blockade of renal tubular transport mechanisms which subsequently promotes increased urine output Structurally Chlorothiazide contains a benzothiadiazine ring system contributing to its specific interaction with renal transport channels and carbonic anhydrase enzymes In biomedical research Chlorothiazide serves as a pharmacological tool to investigate ion transport pathways renal physiologic processes and mechanisms underlying fluid balance regulation Additionally it is utilized in experimental models studying electrolyte homeostasis and disorders associated with abnormal sodium or chloride retention
Apexbio Technology LLC EHT 1864(Synonyms: EHT-1864, EHT1864, RAC inhibitor EHT1864, Rac GTPase inhibitor EHT 1864), 10mM (in 1mL DMSO), CAS: 754240-09-0.
EHT 1864 (CAS 754240-09-0) is a small-molecule inhibitor targeting Rac family GTPases with strongest affinity and inhibitory activity toward Rac1 It interacts directly with Rac isoforms Rac1 Rac1b Rac2 and Rac3 exhibiting Kd values of approximately 40 nM 50 nM 60 nM and 250 nM respectively By disrupting nucleotide binding EHT 1864 blocks Rac1 activation and prevents the formation of active Rac1/PAK-RBD complexes thus inhibiting downstream cellular functions such as PDGF-stimulated lamellipodia formation and Rac1-mediated cellular transformation This compound serves as a valuable tool in cell biology research for studying Rac-dependent signaling pathways and cellular dynamics
Apexbio Technology LLC KPT-330 1393477-72-9 10mM (in 1mL DMSO)
KPT-330 (CAS 1393477-72-9) is an orally bioavailable small-molecule inhibitor selectively targeting chromosome region maintenance 1 protein (CRM1) a nuclear export receptor involved in the active transport of tumor suppressors transcription factors and cell-cycle regulators Overexpression and deregulation of CRM1 are frequently associated with cancer progression KPT-330 inhibits CRM1 function promoting nuclear retention of regulatory proteins such as p21 and inducing apoptosis through activation of apoptotic signaling pathways (e g PAR-4 activation Bax upregulation PARP cleavage caspase-3 activation) In preclinical studies KPT-330 demonstrated antitumor activity against renal cell carcinoma non-small cell lung cancer and pancreatic cancer models
Apexbio Technology LLC Tiplaxtinin(PAI-039)(Synonyms: Tiplaxtinin, PAI-039, Tiplaxtinin (PAI-039), Tiplaxitin, PAI1 inhibitor, PAI-1 antagonist, RWJ-676070), 10mM (in 1mL DMSO), CAS: 393105-53-8.
Tiplaxtinin (PAI-039 CAS 393105-53-8) is an orally bioavailable small molecule inhibitor targeting plasminogen activator inhibitor-1 (PAI-1) a physiological regulator of the plasminogen activation system Elevated PAI-1 levels stabilize thrombi by inhibiting tissue- and urokinase-type plasminogen activators Tiplaxtinin binds selectively to PAI-1 with a Kd of approximately 480 nM and inhibits its activity with an IC50 value around 2 7 M In animal models oral administration of Tiplaxtinin significantly delayed arterial thrombus-induced occlusion supporting its utility as a research tool for studying fibrinolytic pathways and thrombotic disorders
Apexbio Technology LLC BMH-21(Synonyms: BMH21, BMH 21, CID 46835406, RNA polymerase I inhibitor BMH-21, RNA Pol I inhibitor BMH-21), 10mM (in 1mL DMSO), CAS: 896705-16-1.
BMH-21 (CAS 896705-16-1) is a planar heterocyclic small molecule DNA intercalator that selectively inhibits RNA polymerase I (Pol I)-mediated transcription It preferentially inserts into GC-rich double-stranded DNA regions leading to Pol I blockade and subsequent degradation of its catalytic subunit RPA194 BMH-21 exhibits cytotoxic activity across various human cancer cell lines independently of the p53 status disrupting nucleolar integrity and RNA synthesis Furthermore BMH-21 promotes p53 expression in epithelial compartments of human prostate tissues demonstrating tissue permeability and highlighting its applicability in anticancer research
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 Riociguat 625115-55-1 10mM (in 1mL DMSO)
Riociguat (CAS 625115-55-1) chemically known as BAY 63-2521 is a small-molecule stimulator of soluble guanylate cyclase (sGC) It directly activates sGC independently and also enhances the enzyme s sensitivity to nitric oxide (NO) leading to elevated cyclic guanosine monophosphate (cGMP) levels Elevated cGMP induces smooth muscle relaxation and vasodilation Riociguat has been examined clinically for potential therapeutic roles in chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH)
Apexbio Technology LLC Zafirlukast 107753-78-6 10mM (in 1mL DMSO)
Zafirlukast (CAS 107753-78-6) is an antagonist targeting cysteinyl leukotriene receptors (CysLTR) which mediate inflammatory signaling pathways By competitively inhibiting leukotriene receptor binding it disrupts the leukotriene-driven inflammatory response Zafirlukast demonstrates antagonist potency against leukotriene receptors with an IC50 value of approximately 0 6 M and exhibits moderate inhibitory activity on CYP2C9 enzyme (IC50 of about 7 0 M) In biomedical research Zafirlukast serves as a pharmacological tool for studying leukotriene-mediated inflammation and receptor signaling processes