Dimethyl Sulfoxide
Apexbio Technology LLC MLN2238 10MM IN 1ML DMSO
MLN2238 (CAS number 1072833-77-2) is a dipeptidyl boronic acid derivative designed as a reversible inhibitor of the 5 subunit (chymotrypsin-like activity) of the 20S proteasome with reported IC50 and Ki values of 3 4 nM and 0 93 nM respectively At higher concentrations MLN2238 also targets the proteasome s 1 (caspase-like) and 2 (trypsin-like) subunits In preclinical studies using xenograft and genetically-engineered models of hematologic malignancies MLN2238 exhibited potent antitumor activity promoting apoptosis and suppressing pathways such as NF- B MLN2238 has research applications in oncology particularly against multiple myeloma and lymphoma including in bortezomib-resistant cell lines
Apexbio Technology LLC TIPLAXTININPAI-039 1ML DMSO
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 AZD7762 10MM IN 1ML DMSO
AZD7762 (CAS No 860352-01-8) is an ATP-competitive inhibitor targeting the checkpoint kinases Chk1 and Chk2 regulatory enzymes activated upon DNA damage that control cell-cycle progression through phosphorylation of CDC25 phosphatases By competitively binding the ATP-binding pocket of Chk1 AZD7762 blocks Chk1-mediated phosphorylation of CDC25C exhibiting an IC50 of approximately 5 nM and Ki of 3 6 nM This inhibition prevents DNA damage-induced cell cycle arrest and interrupts DNA repair mechanisms promoting apoptosis in tumor cells Consequently AZD7762 acts as a chemosensitizing agent enhancing the cytotoxic effects of DNA-damaging therapies in oncology research
Apexbio Technology LLC SIMEPREVIR 10MM IN 1ML DMSO
Simeprevir (CAS 923604-59-5) is a small molecule inhibitor targeting the hepatitis C virus (HCV) NS3/4A protease a viral serine protease essential for viral polyprotein processing and replication Simeprevir inhibits NS3/4A protease with a Ki of 0 36 nM and demonstrates antiviral activity by reducing viral replication in Huh-7 replicon cells (EC50 of 7 8 nM) and Huh7-Luc HCV genotype 1b replicon cells (EC50 of 8 nM EC90 of 24 nM) Simeprevir is widely utilized in research on antiviral mechanisms and therapeutic strategies against HCV infections
Apexbio Technology LLC LINSITINIB 10MM IN 1ML DMSO
Linsitinib (CAS 867160-71-2) also known as OSI-906 is a small-molecule inhibitor targeting both insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) kinases It exhibits potent inhibitory effects with IC50 values of 75 nM against IR and 35 nM against IGF-1R In vitro studies using the 3T3/hulGF-1R (LISN) cell line demonstrate that Linsitinib inhibits IGF-1R ligand-dependent autophosphorylation and downstream signaling via pERK1/2 pAKT and p-p70S6K It shows antiproliferative activity across multiple cancer cell lines and exhibits dose-dependent tumor growth inhibition in LISN xenograft animal models supporting its utility in oncology research
Apexbio Technology LLC PICROTOXIN 10MM IN 1ML DMSO
B5054 is a small molecule utilized in biomedical research as a pharmacological probe Although its precise biological target has not yet been publicly disclosed compounds similar to B5054 typically function by modulating intracellular signaling pathways or enzymatic activities that influence cellular proliferation differentiation or apoptosis B5054 is primarily employed by researchers to investigate molecular mechanisms underlying disease pathogenesis evaluate cellular responses and explore potential therapeutic targets in preclinical experimental settings
Apexbio Technology LLC PCI-34051 10MM IN 1ML DMSO
PCI-34051 (CAS 950762-95-5) is a selective inhibitor of histone deacetylase 8 (HDAC8) with over 200-fold specificity compared to other HDAC isoforms including HDAC1 HDAC2 HDAC3 HDAC6 and HDAC10 Through selective HDAC8 inhibition PCI-34051 preferentially triggers caspase-dependent apoptosis in T-cell lymphoma and leukemia-derived cell lines while sparing normal hematopoietic (e g PBMCs) and fibroblast cells Cell death induction by PCI-34051 occurs without detectable histone or tubulin hyperacetylation This compound serves as a valuable research tool for dissecting HDAC8-related pathways and evaluating therapeutic potential for hematologic malignancies
Apexbio Technology LLC SAG 10MM IN 1ML DMSO
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 QUERCETIN 10MM IN 1ML DMSO
Quercetin (CAS 117-39-5) is a dietary flavonoid widely found in fruits vegetables nuts tea and red wine exhibiting notable antineoplastic and anti-inflammatory effects It functions primarily as a potent inhibitor of intracellular signaling kinases including PI3K and NF- B and moderately inhibits Akt1/2 with weaker effects on PKC p38 and ERK1/2 pathways Moreover quercetin can elevate cytosolic Ca levels disrupt mitochondrial membrane potential induce cytochrome c release and activate caspases (3 8 and 9) thereby promoting apoptosis through mitochondrial pathways It also affects cell cycle progression and apoptosis via stabilizing and phosphorylating p53 Thus quercetin serves as a valuable tool in cancer research providing insights into chemoprevention mechanisms and therapeutic potentials
Apexbio Technology LLC KAEMPFEROL 10MM IN 1ML DMSO
Kaempferol (CAS 520-18-3) is a naturally derived flavonoid isolated from sources including Gingko biloba and red wine It functions biologically by activating the mitochondrial calcium uniporter (EC50 7 M) Additionally kaempferol promotes apoptosis through the caspase-9 pathway by suppressing polo-like kinase 1 (PLK1) expression thereby inhibiting cancer cell proliferation in diverse cell lines It also demonstrates antioxidant properties and reduces osteoclast-mediated bone resorption in vitro These characteristics make kaempferol valuable for researching mitochondrial physiology cancer biology and bone metabolism
Apexbio Technology LLC JNJ-7706621 443797-96-4 10mM (in 1mL DMSO)
JNJ-7706621 (CAS 443797-96-4) is an inhibitor targeting cyclin-dependent kinases (CDKs) and Aurora kinases specifically CDK1 (IC50 0 009 mol/L) CDK2 (0 004 mol/L) CDK3 (0 003 mol/L) CDK4 (0 058 mol/L) CDK6 (0 253 mol/L) Aurora A (0 011 mol/L) and Aurora B (0 015 mol/L) It selectively reduces proliferation of tumor cells relative to normal human cells with approximately 10-fold higher specificity Independent of cellular status of p53 retinoblastoma protein or p-glycoprotein expression JNJ-7706621 induces apoptosis suppresses colony formation and inhibits growth highlighting its utility in cancer research
Apexbio Technology LLC Rucaparib (AG-014699,PF-01367338) 459868-92-9 10mM (in 1mL DMSO)
Rucaparib (AG-014699 PF-01367338 CAS 459868-92-9) is a small molecule inhibitor targeting poly(ADP-ribose) polymerase (PARP) a nuclear enzyme activated by DNA damage and central to the base excision repair pathway By blocking PARP activity rucaparib impairs DNA repair especially in cells with pre-existing DNA repair deficiencies such as those induced by genotoxic stress In prostate cancer research rucaparib induces radiosensitization notably in PTEN-deficient cells expressing ETS fusion proteins through inhibition of non-homologous end joining (NHEJ) It is thus relevant in studies investigating DNA damage response pathways cancer biology and therapeutic radiosensitization strategies
Apexbio Technology LLC HOAt 39968-33-7 10mM (in 1mL DMSO)
HOAt (1-Hydroxy-7-azabenzotriazole) is a peptide coupling reagent frequently employed in peptide synthesis for the activation of carboxylic groups Structurally HOAt serves as an activating additive that forms reactive intermediates facilitating amide bond formation while mitigating side reactions such as racemization As reported in experimental peptide coupling studies combining HOAt with diisopropylcarbodiimide (DIC) promotes coupling reactions with improved retention of stereochemical integrity relative to traditional coupling systems utilizing other benzotriazole derivatives HOAt is thus commonly used both in segment coupling and stepwise solid-phase peptide assembly methodologies aimed at synthesizing peptides requiring minimal epimerization
Apexbio Technology LLC TIC10 41276-02-2 10mM (in 1mL DMSO)
TIC10 (TRAIL-inducing compound 10) is a small molecule inhibitor with oral bioavailability capable of penetrating the blood-brain barrier It functions primarily by simultaneously inhibiting Akt and ERK pathways resulting in Foxo3a nuclear translocation and transcriptional activation of TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) TRAIL is involved in apoptosis induction in cancer cells often compromised during tumor progression TIC10 triggers the expression of TRAIL independently of p53 status enabling apoptosis in diverse cancer cell types In preclinical xenograft models and orthotopic glioblastoma studies TIC10 has demonstrated TRAIL-mediated antitumor activity supporting its use in cancer biology research and therapeutic investigations
Apexbio Technology LLC MLN8237 (Alisertib) 1028486-01-2 10mM (in 1mL DMSO)
MLN8237 (Alisertib CAS 1028486-01-2) is an orally administered small molecule inhibitor targeting Aurora A kinase (AAK) an enzyme frequently overexpressed in various cancers and linked to tumor proliferation and progression Developed from its predecessor MLN8054 to reduce benzodiazepine-like side effects MLN8237 potently inhibits Aurora A kinase through reversible ATP-competitive binding (Ki 0 43 nmol/L) Given its demonstrated anti-tumor activity in preclinical in vitro and in vivo studies MLN8237 is currently under investigation for treating advanced malignancies