GNE-317 is a potent, brain-penetrant PI3K inhibitor.

FHND5032 is an orally active miR-124 inducer. FHND5032 significantly upregulates miR-124 expression in macrophages. FHND5032 disrupts inflammatory signaling, promotes macrophage reprogramming, and restores the epithelial barrier function by inhibiting the PIK3R2/PI3K/Akt axis. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mice. FHND5032 can be used for the study of ulcerative colitis.

DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research[1][2][3].

Psicose is a natural and low-calorie sweetener. Psicose can activate the PI3K/Akt/mTOR pathway to promote muscle synthesis. Psicose can upregulate IGF-1 and downregulate Myostatin. Psicose regulates mitochondrial function by increasing G6P activity. Psicose enhances antioxidant enzyme activity and reduces oxidative stress markers. Psicose reduces plasma triglycerides and total cholesterol. Psicose can improve muscle fiber size and reduce fibrosis. Psicose can be used for research on sarcopenia.

PI3Kα Ligand-1 is the ligand for PI3Kα that can be used for synthesis of PROTACs, such as PI3Kα degrader-1.

RLX (PD 139530) hydrochloride is the hydrochloride of RLX). RLX is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness.

PF-05139962 is a cyclic sulfone mTOR kinase inhibitor. PF-05139962 exhibits potent mTOR (Ki = 5 nM, pS473 IC50 = 48 nM, pS6 IC50 = 6 nM) inhibitory activity and high selectivity.

AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer.

SM1-71-R is a reversible analog o SM1-71). SM1-71-R lacks the acrylamide warhead and therefore cannot form a covalent bond with the kinase. SM1-71-R can be used as a control compound for SM1-71.

SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia.

Ganglioside GT1b is a member of the ganglioside family. Ganglioside GT1b acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b enhances porcine oocyte maturation and induce activation of EGFR and ERK1/2 signaling. Ganglioside GT1b is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease.

D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) (Ins(1,3,4,5,6)P5 (ammonium salt)) is an isomer of inositol phosphate that acts as a small and soluble second messenger in the transmission of cellular signals. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can bind to the PH domain of Grp1 with a Kd of 590 nM. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can inhibit the phosphorylation and kinase activity of Akt/PKB, inducing apoptosis in ovarian, lung, and breast cancer cells. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exhibits antiangiogenic activity in vitro and blocks capillary tube formation of HUVEC. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exerts antitumor effects against cancer xenografts in nude mice.

Tanerasertib (Compound 456) is an AKT1 inhibitor with an IC50 of less than 15 nM against AKT1 E17K. Tanerasertib can be used in the study of cancer.

X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).

MT-44 is a highly selective and potent mTOR inhibitor with an IC50 of 49.4 nM. MT-44 can inhibit cancer cells proliferation, migration and invasion. MT-44 can induce cells apoptosis and ROS production and cause G2/M phase arrest. MT-44 can activate the cGAS/STING pathway. MT-44 can be used for the research of cancer, such as triple-negative breast cancer.

PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research.

mTOR inhibitor-28 (SM-3) is a potent mTOR inhibitor. mTOR inhibitor-28 inhibits A549, H292, and H460 cells with IC50s of 72.74, 67.66, and 43.24 μM, respectively.

Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

PWT-33597 (VDC-597) is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

PWT-33597 (VDC-597) free base is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 free base is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 free base has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

TMX-4140 is a selective PIP4K2C inhibitor with a KD of 7.2 nM for PIP4K2C over PIP4K2B. TMX-4140 can be used for synthesis of PROTAC TMX-4153.

Tezampanel etibutil is an orally active AMPA/GluR antagonist. Tezampanel etibutil can be used in the research of pain, migraine, and neurological disorders.

ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7. ARUK2010489 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 7%, 39% and 26% at 1 μM. ARUK2010489 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

ARUK2010694 (Compound 20) is a potent and selective NUAK1 inhibitor with a pIC50 of 8.7. ARUK2010694 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 13%, 63% and 32% at 1 μM. ARUK2010694 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

ML-220 is a PI3K modulator that can be used for the study of neoplasms and infectious diseases.

Archexin is an antisense oligonucleotide (ASO) against Akt1. It is used for the study of metastatic renal cancer.

Archexin sodium is an antisense oligonucleotide (ASO) against Akt1. It is used for the study of metastatic renal cancer.

LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

bpV(bipy) hydrate is the inhibitor for phosphoinositide 3-phosphatase (PTEN) and protein tyrosine phosphatases (PTP-β and PTP-1B) with IC50s of 18, 60.3, and 164 nM, respectively.