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Catalog No.
Product Name
Application
Product Information
Citations
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allosteric Akt1/Akt2 inhibitor
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively. -
dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). -
GSK-3β inhibitor
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM. -
PI3Kγ inhibitor
PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively. -
PI4KB inhibitor
T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM. -
PI3Kδ inhibitor
PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM. -
CDK1, CDK5, and GSK-3βinhibitor
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively. -
GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively. -
PI3Kα inhibitor
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). -
Akt inhibitor
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family. -
PI3K inhibitor
CAL-130 Hydrochloride is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kδ/γ as therapy for T cell acute lymphoblastic leukemia (T-ALL). -
mTOR inhibitor
mTOR inhibitor is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 1.5 nM. -
PI3K Inhibitor
NVP-BKM120 Hydrochloride is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNA-PK, with little activity to PI4Kβ. -
PI3K Inhibitor
PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. -
PTEN inhibitor
VO-Ohpic trihydrate is an inhibitor of PTEN (phosphatase and tensin homologue deleted on chromosome 10). -
PI3K Inhibitor
XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases. -
PI4KIII beta inhibitor
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIII beta inhibitor with IC50 of 5.7 nM. -
p70S6K inhibitor
LY-2584702 tosylate salt is an orally available inhibitor of p70S6K signaling; inhibits p70S6K and prevents phosphorylation of the S6 subunit of ribosomes. -
p110α inhibitor
MLN1117, also known as INK1117 and TAK-117, is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. -
GSK-3 inhibitor
BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity. -
PTP/PTEN Inhibitor
bpV(phen) is a potent inhibitor of protein tyrosine phosphatases (PTPs) and PTEN, exhibiting IC50 values of 38 nM, 343 nM, and 920 nM for PTEN, PTP-β, and PTP-1B, respectively. This compound demonstrates significant anti-proliferative effects on the protozoan parasite Leishmania in vitro. Additionally, bpV(phen) enhances the secretion of various chemokines and pro-inflammatory cytokines while promoting a Th1-type immune response characterized by IL-12 and IFNγ production. It also induces apoptosis and exhibits anti-angiogenic and anti-tumor properties, making it valuable for research in cancer and inflammation biology. -
PI3Kα/β/δ Inhibitor
BAY1082439 is a selective inhibitor of the PI3Kα, β, and δ isoforms, demonstrating oral bioavailability. This compound effectively inhibits both wild-type and mutated forms of PIK3CA, making it a valuable tool in cancer research. Notably, BAY1082439 has shown significant efficacy in suppressing the growth of Pten-null prostate cancer, highlighting its potential in therapeutic applications targeting specific tumors. -
ATR Inhibitor
AD1058 is a selective, orally active inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR) with an IC50 of 1.6 nM. This compound demonstrates significant anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis in various cancer models. AD1058 is particularly relevant for research focused on advanced malignancies and brain metastases, providing a valuable tool for investigating therapeutic strategies in these challenging areas. -
PI3Kα Inhibitor
PI3Kα-IN-9 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 4.4 nM while demonstrating lesser potency against PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 128, 146, and 153 nM, respectively. This compound is notable for its long-acting oral activity and ability to induce apoptosis alongside antiproliferative effects in cancer cells. PI3Kα-IN-9 serves as a valuable reagent for cancer research, particularly in studies focused on PI3K signaling pathways. -
GSK-3β Inhibitor
GSK-3β Inhibitor 3 is a potent and selective irreversible covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), exhibiting an IC50 of 6.6 μM. This compound is instrumental in research applications related to acute promyelocytic leukemia, providing insights into GSK-3β's role in cancer signaling pathways and therapeutic strategies. Its specificity allows for detailed studies of GSK-3β inhibition effects on cellular processes and pathways involved in oncogenesis. -
PDK1 Inhibitor
PDK1-IN-1 is a selective inhibitor of PDK1, which plays a crucial role in cellular signaling pathways related to growth and survival. Additionally, it exhibits inhibitory effects on other kinases, including FGFR3, NTRK3, RP-S6K, and WEE1, as well as microtubule affinity regulating kinase (MARK). This compound is valuable for research applications in the study of myeloproliferative disorders, cancer, and neurodegenerative diseases such as Alzheimer's disease. -
mTOR Inhibitor
CC214-2 is a selective mTOR kinase inhibitor that targets both mTORC1 and mTORC2 pathways, affecting pS6 and pAktS473 signaling. This compound induces autophagy, making it a promising candidate for host-directed therapy in tuberculosis, demonstrating synergistic bactericidal effects that can shorten treatment duration. Additionally, CC214-2 has shown efficacy in inhibiting Rapamycin-resistant signaling and suppressing glioblastoma growth in vitro and in vivo, positioning it as a valuable tool in cancer research and infectious disease studies. -
GSK-3β Inhibitor
Manzamine A is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and cyclin-dependent kinase 5 (CDK-5), with respective IC50 values of 10.2 μM and 1.5 μM. This compound exhibits significant biological activity, including antimalarial and anticancer effects, and has been shown to inhibit autophagy in pancreatic cancer cells by targeting vacuolar ATPases. Additionally, Manzamine A demonstrates potent antiviral properties against herpes simplex virus type 1 (HSV-1), making it a valuable reagent for diverse research applications in cancer, autophagy, and virology studies. -
mTOR Inhibitor
T133 is a potent ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR) with an IC50 of 0.34 nM and a Ki of 0.17 nM. It effectively suppresses the phosphorylation of downstream targets, including AKT, S6K1, and 4EBP1, leading to the inhibition of cancer cell proliferation and migration, induction of apoptosis, cell cycle arrest, and promotion of autophagy. T133 demonstrates significant antitumor efficacy in xenograft mouse models and serves as a valuable tool in cancer research, particularly for studies involving gastric and lung cancers. -
AMPK Activator/mTOR Inhibitor
OSU-53 is an orally active AMPK activator and a direct mTOR inhibitor, exhibiting an EC50 of 0.3 μM. This compound induces autophagy by facilitating the conversion of LC3 I to LC3 II and plays a crucial role in modulating energy homeostasis by downregulating fatty acid biosynthesis while enhancing oxidative metabolism through upregulation of PGC1α and NRF-1. OSU-53 demonstrates antitumor activity across various cancer models, including breast and thyroid cancers, making it a valuable tool for cancer research and metabolic studies. -
mTOR Inhibitor
4-FPBUA is a semisynthetic analog of usnic acid that functions as an inhibitor of mTOR. It enhances cellular autophagy and supports blood-brain barrier (BBB) integrity, facilitating the transport of Amyloid β (Aβ) across monolayer cell systems. This compound is of particular interest in Alzheimer's disease research due to its potential to reverse BBB disruption and promote neuroprotection. -
mTOR Inhibitor
3HOI-BA-01 is a potent mTOR inhibitor that plays a critical role in modulating cellular processes. It has been shown to reduce infarct size and induce autophagy in murine models of myocardial ischemia/reperfusion injury. This compound is valuable for research applications focused on cardiac health, autophagy pathways, and cellular stress responses. -
mTORC1 Inhibitor
ICSN3250 hydrochloride is a potent mTORC1 inhibitor that acts by binding to the FRB domain of mTOR, effectively displacing phosphatidic acid and reversing mTORC1 activation. This compound exhibits significant cytotoxicity in cancer cells at nanomolar concentrations via a caspase-independent cell death mechanism. By selectively inhibiting the mTORC1 pathway, ICSN3250 hydrochloride promotes autophagy and induces G0-G1 cell cycle arrest in cancer cells, making it a valuable tool for cancer research. -
mTORC1 Inhibitor
ICSN3250 is a selective mTORC1 inhibitor that operates by directly binding to the FRB domain of mTOR, effectively displacing phosphatidic acid and reversing mTORC1 activation. This compound demonstrates significant cytotoxicity in cancer cells at nanomolar concentrations via a caspase-independent cell death mechanism. Additionally, ICSN3250 specifically inhibits the mTORC1 pathway, promoting autophagy and inducing G0-G1 cell-cycle arrest. It is suitable for research applications focused on cancer biology and therapeutic exploration. -
ATR Inhibitor
ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer.
