PI3K Inhibitor

Quercetin-d₅ is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC₅₀ of 1.7 nM.

Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research.

KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer.

PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF).

PI3K-IN-36 (compound A68) is a potent PI3K inhibitor. PI3K-IN-36 can be used in research of follicular lymphoma (FL).

4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.

RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS^G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS^G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research.

Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research.

Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.

Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

α-Linolenic acid-d₅ is the deuterium labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.

Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC₅₀ of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

Hawthorn Extract is an orally active hawthorn extract. Hawthorn Extract decreases Bax expression and increases Bcl-2 expression in the aorta. Hawthorn Extract regulates the AMPK signaling pathway, induces apoptosis, enhances the hepatic antioxidant system, and ameliorates symptoms of liver injury, inflammation and cancer. Hawthorn Extract reduces plasma levels of pro-inflammatory factors, increases plasma levels of anti-inflammatory adiponectin, and alleviates atherosclerotic plaque lesions in the aorta. Hawthorn Extract improves symptoms associated with chronic heart failure. Hawthorn Extract inhibits FMLP-induced superoxide anion production, Elastase release, ILB₄ generation and calcium signaling in neutrophils, and also reduces LPS-induced cytokine production in neutrophils. Hawthorn Extract induces autophagy and inhibits the proliferation of intestinal stem cells. Hawthorn Extract can be used in research related to atherosclerosis, hepatitis, alcoholic liver disease, non-alcoholic fatty liver disease, hepatocellular carcinoma, chronic heart failure and hypotension.

MTX-216 is a dual ATP-competitive inhibitor of PI3K and EGFR. MTX-216 cosuppresses Ki-67 and ribosomal S6 phosphorylation and induces apoptosis in NF1^LOF cells. MTX-216 suppresses the activity of SYK kinase, with an IC₅₀ of 281 nM. MTX-216 is used in the research of Melanoma.

WCY-8-67 is an orally active and selective USP5 inhibitor, with an IC₅₀ value of 1.33 μM. WCY-8-67 induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways in vitro. WCY-8-67 inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 can be used for the study of acute myeloid leukemia.

KHK-2898 is a monoclonal antibody targeting CD98, which binds to the extracellular domain of CD98 on the tumor cell membrane in a non-covalent antigen-specific mode. KHK-2898 can disrupt the heterodimeric complex formed by CD98 with LAT1 and xCT light chains, reduce the amino acid uptake capacity of tumor cells, block the PI3K/AKT/mTOR proliferative signaling cascade, and mediate antibody-dependent cytotoxicity. KHK-2898 can be used for cancer-related research. The isotype control of KHK-2898 can be found in Human IgG1 kappa, Isotype Control (HY-P99001).

Leniolisib-d5 is a deuterated labeled Leniolisib. Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.

(Rac)-AZD 6482 ((Rac)-KIN-193) is the racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC₅₀ of 0.69 nM.