Dimethyl Sulfoxide
Apexbio Technology LLC Nisoldipine 63675-72-9 10mM (in 1mL DMSO)
Nisoldipine (CAS 63675-72-9) is a dihydropyridine-based calcium channel blocker selective for the voltage-dependent L-type calcium channel Cav1 2 It inhibits Cav1 2-mediated calcium influx with an IC50 of approximately 10 nM By modulating calcium entry nisoldipine is frequently utilized in cardiovascular research to study vascular smooth muscle contraction calcium signaling pathways and cardiovascular pharmacology Its selective blockade helps elucidate the functional importance of Cav1 2 channels under physiological and pathological conditions
Apexbio Technology LLC LY364947 396129-53-6 10mM (in 1mL DMSO)
LY364947 (CAS 396129-53-6) is a selective inhibitor targeting the kinase domain of transforming growth factor- (TGF- ) type I receptor TGF- signaling regulates crucial biological processes such as cell proliferation differentiation and tissue homeostasis In vitro studies demonstrated that LY364947 inhibits the receptor kinase activity with an IC50 of 51 nM effectively suppressing TGF- -dependent luciferase activity in mink lung epithelial cells (p3TP Lux assay) and growth of NIH 3T3 fibroblasts In vivo LY364947 showed protective effects against NMDA-induced retinal degeneration in rats attenuating retinal ganglion cell loss and capillary degradation Thus LY364947 serves as a valuable pharmacological tool in TGF- -related research and associated pathological conditions
Apexbio Technology LLC MDL 28170 88191-84-8 10mM (in 1mL DMSO)
MDL 28170 (CAS 88191-84-8) is a selective inhibitor of calpain and cathepsin B with Ki values of approximately 10 nM and 25 nM respectively It acts by directly blocking the catalytic site of these cysteine proteases without inhibiting serine proteases MDL 28170 readily penetrates the blood-brain barrier inhibiting protease activity in brain tissue and mitigating ischemia-induced neurological damage in animal models The compound reduces muscle fiber sensitivity to calcium influx post-ischemia and limits myocardial injury caused by calcium overload It also exhibits antiparasitic activity in vitro significantly lowering Trypanosoma cruzi survival in infected macrophages MDL 28170 is used in biomedical research to study protease-related pathology ischemic injury and parasite-host interactions
Apexbio Technology LLC LMK 235 1418033-25-6 10mM (in 1mL DMSO)
LMK 235 (CAS 1418033-25-6) is a histone deacetylase (HDAC) inhibitor exhibiting preferential selectivity against HDAC4 and HDAC5 isoforms HDAC enzymes (EC 3 5 1 98) catalyze the removal of acetyl groups from lysine residues on histone proteins influencing DNA-histone interactions and gene expression In vitro LMK 235 demonstrates potent inhibition at nanomolar concentrations against HDAC4/5 and notable cytotoxic effects toward multiple cancer cell lines including A2780 Cal27 Kyse510 and MDA-MB231 In animal studies LMK 235 enhances the antitumor efficacy of cytarabine suggesting applications in overcoming chemoresistance in leukemia models Currently LMK 235 remains under preclinical investigation
Apexbio Technology LLC VX-809 936727-05-8 10mM (in 1mL DMSO)
VX-809 (CAS 936727-05-8) is a small molecule CFTR corrector that partially restores the functional expression of F508del-CFTR the most common mutation associated with cystic fibrosis (CF) VX-809 stabilizes the misfolded CFTR protein by interacting with its membrane-spanning domain 1 (MSD1) thus facilitating proper maturation and membrane localization In F508del-CFTR-expressing Fischer rat thyroid (FRT) cells VX-809 enhanced CFTR protein processing (EC50 0 1 M) and improved chloride transport (EC50 0 5 M) VX-809 is utilized predominantly as a research tool in CF studies to understand and restore CFTR function often in combination with CFTR potentiators
Apexbio Technology LLC ABT-737 852808-04-9 10mM (in 1mL DMSO)
ABT-737 (CAS 852808-04-9) is a small molecule inhibitor targeting the BCL-2 protein family exhibiting high binding affinity toward the anti-apoptotic proteins BCL-2 BCL-X L and BCL-w ABT-737 disrupts BCL-2/BAX protein interactions leading to apoptosis primarily via the BAK-mediated intrinsic pathway independent of BIM In preclinical studies ABT-737 demonstrated single-agent antitumor activity in lymphoma multiple myeloma and small-cell lung cancer models Additionally research indicates activity against acute myeloid leukemia (AML) cells progenitor cells and leukemia stem cells while sparing normal hematopoietic populations highlighting its potential for therapeutic research in hematologic malignancies
Apexbio Technology LLC Valganciclovir HCl 175865-59-5 10mM (in 1mL DMSO)
Valganciclovir hydrochloride is an antiviral prodrug that undergoes rapid enzymatic conversion to the active metabolite ganciclovir after oral administration Ganciclovir inhibits viral replication by selectively targeting viral DNA polymerase thereby interfering with viral DNA synthesis and slowing cytomegalovirus (CMV) proliferation Valganciclovir is commonly utilized in laboratory studies to evaluate antiviral activity against CMV and related herpesviruses and to investigate its therapeutic potential in CMV-associated infections including retinitis and organ transplant-associated CMV infections In vitro studies report an IC50 value for valganciclovir-derived ganciclovir ranging approximately from 0 2 to 2 8 M depending on experimental cell type and viral strain
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 (+)-Bicuculline 485-49-4 10mM (in 1mL DMSO)
( )-Bicuculline is a competitive antagonist of gamma-aminobutyric acid type A (GABA A) receptors frequently employed as a pharmacological tool to elucidate the functional roles of inhibitory neurotransmission mediated by GABA A By antagonizing GABA binding this compound prevents chloride ion influx leading to reductions in neuronal inhibitory postsynaptic potentials (IPSPs) Additionally ( )-Bicuculline blocks small conductance calcium-activated potassium (SK) channels affecting neuronal excitability and firing patterns It is commonly utilized in electrophysiological studies such as patch-clamp or extracellular recordings to investigate synaptic transmission neuroplasticity mechanisms and epileptic activity models ( )-Bicuculline inhibits GABA A receptors with an IC 50 typically reported in the low micromolar range (approximately 2 5 M)
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC vinblastine 865-21-4 10mM (in 1mL DMSO)
Vinblastine is a naturally-derived alkaloid isolated from Catharanthus roseus It functions as a microtubule inhibitor by binding specifically to tubulin disrupting microtubule polymerization and thereby arresting mitosis at metaphase Due to this mechanism vinblastine is widely investigated for antitumor activities and is commonly employed in biomedical research to study cell division cytoskeletal dynamics and therapeutic interventions in oncology Vinblastine should be stored under sealed dry and cool conditions to maintain molecular integrity and biological activity
Apexbio Technology LLC Santacruzamate A (CAY10683) 1477949-42-0 10mM (in 1mL DMSO)
Santacruzamate A (CAY10683 CAS 1477949-42-0) is a selective histone deacetylase (HDAC) inhibitor originally identified in the marine cyanobacterium cf Symploca sp Its mechanism of action involves targeting HDAC enzymes particularly demonstrating high selectivity towards HDAC2 (IC 0 112 nM) when compared with HDAC6 (IC 433 nM) and minimal potency against HDAC4 (IC 1 M) In cellular assays Santacruzamate A reduces growth of tumor cell lines such as HCT-116 colon cancer cells (GI 28 M) and HuT-78 cutaneous T-cell lymphoma cells (GI 1 3 M) It is valuable in epigenetics and oncology research for selectively modulating HDAC2 activity
Apexbio Technology LLC Dronedarone 141626-36-0 10mM (in 1mL DMSO)
Dronedarone (CAS 141626-36-0) is a benzofuran derivative structurally related to amiodarone designed to manage cardiac arrhythmias It exerts its pharmacological effects primarily through multichannel blockade inhibiting sodium potassium and calcium ion currents and demonstrating anti-adrenergic properties By prolonging action potential duration and refractory periods dronedarone contributes to the stabilization and restoration of regular cardiac rhythm In biomedical research contexts dronedarone serves as a valuable tool for exploring arrhythmogenesis mechanisms and developing therapeutic approaches for atrial fibrillation and atrial flutter
Apexbio Technology LLC Bedaquiline 843663-66-1 10mM (in 1mL DMSO)
Bedaquiline a diarylquinoline antibiotic targets Mycobacterium tuberculosis via dual inhibition of subunits c and within the bacterial F1FO-ATP synthase complex disrupting ATP production It is applied primarily in research addressing multi-drug resistant (MDR) tuberculosis Recent studies have expanded its use into oncology where bedaquiline inhibits mitochondrial respiratory function and reduces glycolytic activity in cancer stem-cell-like populations In vitro experiments employing breast cancer MCF7 cells revealed bedaquiline increased ROS levels and reduced mitochondrial membrane potential Reported IC50 values for growth inhibition range approximately 1-10 M depending on cell lines and experimental conditions
Apexbio Technology LLC UMI-77(Synonyms: UMI 77, UMI77, UMI-77 Mcl-1 inhibitor, Mcl-1 inhibitor UMI-77, 518303-20-3), 10mM (in 1mL DMSO), CAS: 518303-20-3.
UMI-77 (CAS 518303-20-3) is a small-molecule inhibitor targeting the anti-apoptotic protein Myeloid cell leukemia-1 (Mcl-1) a member of the Bcl-2 protein family implicated in apoptotic regulation and cell survival signaling Biochemical assays demonstrate that UMI-77 binds selectively to the BH3-binding groove of Mcl-1 protein competing effectively against pro-apoptotic BH3 peptides (Ki 0 49 M) Additionally UMI-77 disrupts the interaction of Mcl-1 with pro-apoptotic factors such as Bax (IC50 1 43 M) promoting apoptosis in cancer cells Preclinical studies on pancreatic cancer cell lines and BxPC-3 xenograft mouse models show that UMI-77 suppresses tumor growth and induces apoptotic cell death highlighting its value as a research tool for studying apoptosis-related oncogenic pathways