PI3Kδ Inhibitor

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.

TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC₅₀ of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity.

PI3Kδ-IN-23 (compound A11) is a potent inhibitor of PI3Kδ, with the IC₅₀ of 0.27 nM. PI3Kδ-IN-23 bounds to PI3Kδ by covalent-bonding interactions with Lys779. PI3Kδ-IN-23 plays an important role in cancer research.

PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC₅₀ of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis.

PI3Kδ-IN-26 (Compound 58) is a selective and orally active PI3Kδ inhibitor with an IC₅₀ of 14  nM. PI3Kδ-IN-26 significantly attenuates the inflammatory responses in house dust mite (HDM) induced chronic asthma mouse models. PI3Kδ-IN-26 can be used for inflammatory, autoimmune and hyperproliferative diseases research.

LTURM 36 (20i) is a PI3K inhibitor, with IC₅₀ values ​​of 0.64 μM and 5.0 μM for PI3Kδ and PI3Kβ, respectively. LTURM 36 can be used in anticancer research.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. CC-M-1 inhibits PI3Kα/β/γ/δ and mTOR with IC₅₀ values of 0.68, 1.02, 1.03, 8.03, and 15 nM, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines, including HCT-116 (IC₅₀ = 0.38 μM) and HT-29 (IC₅₀ = 1.70 μM). CC-M-1 can be used for colorectal cancer (CRC) research.

RV-6153 is a potent and selective dual inhibitor of PI3Kδ and PI3Kγ, with IC₅₀ values of 2.5 nM and 28 nM, respectively. RV-6153 dually inhibits PI3Kδ and PI3Kγ, blocking Akt phosphorylation, thereby inhibiting ROS production and cytokine release at the cellular level, and reducing neutrophil and macrophage accumulation in the airways in vivo. RV-6153 can be used in research on chronic obstructive pulmonary disease, asthma, and other inflammatory diseases.

PI3K-IN-54 (compound 10w) is a pan-PI3K inhibitor. The IC₅₀ values of PI3K-IN-54 for p110α, p110β, and p110δ are 0.22 nM, 1.4 nM, and 0.38 nM, respectively. PI3K-IN-54 can be used in cancer research.

PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC₅₀s of <100 nM.

AS2541019 is a PI3Kδ (p110δ) inhibitor. AS2541019 inhibits B cell activation and proliferation, and suppresses xenograft antibody production.

Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC₅₀ value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers).

AM-0687 is a selective inhibitor for PI3Kδ with an IC₅₀ of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC₅₀=0.8 nM) and the phosphorylation of AKT (IC₅₀=0.7 nM), and exhibits anti-inflammatory efficacy.

CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.

PI3Kδ-IN-27 is an PI3Kδ inhibitor with an IC₅₀ of 355.3 nM. PI3Kδ-IN-27 exhibits anti-SARS-CoV-2 activity. PI3Kδ-IN-27 can be used for the research of infection, such as COVID-19.

PIK-C98 is a potent and selective PI3K inhibitor, with IC₅₀s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma.

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.

PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 3.8 nM.