pi3kδ-in-3

PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function.

PI3Kδ/γ-IN-3 (Compound 58) is an orally active dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 16 nM), effective in inducing apoptosis of tumor cells and applicable to B-cell malignant tumor studies.

PI3K-IN-38 is an orally available and potent PI3K inhibitor with an IC50 value of 0.541 µM for PI3K-α. PI3K-IN-38 exhibits anticancer and anti-inflammatory activity and inhibits tumor growth in vivo.

PI3K-IN-34 (Compound 6g) is a highly selective inhibitor of PI3K, targeting PI3K-α (IC50: 11.73 μM), PI3K-β (IC50: 6.09 μM), and PI3K-δ (IC50: 11.18 μM), and can be used to study leukaemia.

PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50 values of 3.7 nM for PI3Kα, 74 nM for PI3Kβ, 14.6 nM for PI3Kγ, and 9.9 nM for PI3Kδ. PI3K-IN-31 has demonstrated anticancer activity.

PI3K-IN-37 (Example 84.1) is an inhibitor of PI3K α (IC50: 6 nM), PI3K β (IC50: 8 nM), and PI3K δ (IC50: 4 nM), and also inhibits mTOR with an IC50 of 4 nM.

PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50 values of 5.1 nM for PI3Kα, 136 nM for PI3Kβ, 30.7 nM for PI3Kγ, and 8.9 nM for PI3Kδ.

PI3K-IN-35 (Compound 6l) is a highly selective inhibitor of PI3K, targeting PI3K-α (IC50: 13.98 μM), PI3K-β (IC50: 7.22 μM), and PI3K-δ (IC50: 10.94 μM). It blocks the cell cycle in the G2/M phase and induces apoptosis, making it useful for studying leukemia.

PI3K-IN-33 is a highly selective PI3K inhibitor that acts on PI3K-α (IC50: 11.73 μM), PI3K-β (IC50: 6.09 μM) and PI3K-δ (IC50: 11.18 μM). PI3K-IN-33 is capable of blocking the cell cycle in G2/M phase and can induce apoptosis and can be for the study of leukemia.

PI3K-IN-36 is a potent inhibitor of PI3K, suitable for research applications in follicular lymphoma (FL).

PI4KIIIbeta-IN-9 is a potent inhibitor of PI4KIIIβ [IC50 of 7 nM].

Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.

TYM-3-98 is a novel, selective PI3Kδ inhibitor (IC50=7.1 nM). It induces apoptosis by blocking PI3K/AKT/mTOR signaling in B-cell lymphoma models.

PI3Kδ-IN-21 (Compound 31) is a selective inhibitor of phosphoinositide 3-kinase δ (PI3Kδ), with an IC50 of 13.6 nM. It impedes the proliferation and differentiation of T cells through the PI3K/AKT/mTOR signaling pathway. In rat models, PI3Kδ-IN-21 exhibits favorable pharmacokinetic properties and demonstrates activity in improving experimental autoimmune encephalomyelitis induced by myelin oligodendrocyte glycoprotein (MOG) in EAE models.

DHW-221 is an orally active dual PI3K/mTOR inhibitor demonstrating potent inhibition at nanomolar levels across 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). By blocking the PI3K/Akt/mTOR pathway, DHW-221 induces mitochondrial apoptosis and paraptosis (through endoplasmic reticulum stress and MAPK signaling) and causes cell cycle arrest, thereby inhibiting cell migration, invasion, and angiogenesis to exert its antitumor effects. It suppresses tumor growth in A549/Taxol and HCC827 mouse models and is applicable in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer[1][2][3].

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.

(S)-PI3Kα-IN-4, a potent inhibitor of PI3Kα with an IC50 of 2.3 nM, demonstrates 38.3-, 4.25-, and 4.93-fold selectivity over PI3Kβ, PI3Kδ, and PI3Kγ, respectively, and is suitable for cancer research[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1].

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

PI3Kδ-IN-9 is a selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with an IC50 value of 3.8 nM.

PI3K/AKT-IN-1 is a dual PI3K and AKT inhibitor with anti-cancer activity. It inhibits PI3Kγ, PI3Kδ, and AKT, suppressing the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis, suitable for cancer research.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

Linperlisib (PI3Kδ-IN-2) is a potent and selective inhibitor of PI3Kδ