p110δ inhibitor

Idelalisib-D5, a version of Idelalisib (T8651) marked with deuterium, is an orally bioavailable and highly selective inhibitor of p110δ.

Compound P110 (Drp1 peptide inhibitor P110) is a selective Drp1 peptide inhibitor with neuroprotective effects. It inhibits the activation of Drp1, prevents Drp1 mitochondrial translocation induced by MPTP, and alleviates dopamine neuron loss, dopaminergic terminal damage, and behavioral deficits caused by MPTP. This compound is useful for Alzheimer's disease research. Additionally, Compound P110 reduces mitochondrial and organ damage in animal models of Huntington's disease, cerebral ischemia, and myocardial infarction.

Drp1 peptide inhibitor P110 (Compound P110) TFA is a selective Drp1 peptide inhibitor with neuroprotective properties. It suppresses the activation of Drp1, prevents Drp1 mitochondrial translocation induced by MPTP, and reduces MPTP-induced loss of dopaminergic neurons, damage to dopaminergic nerve terminals, and behavioral defects, making it useful for Alzheimer's disease research. Furthermore, Drp1 peptide inhibitor P110 TFA mitigates mitochondrial and organ damage in animal models of Huntington's disease, cerebral ischemic injury, and myocardial infarction.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β/p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

Idelalisib (GS-1101) is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

Zandelisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K)(p110δ, IC50 of 3.5 nM), and with antineoplastic activity.

Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent PI3Kα inhibitor (IC₅₀ = 5 nM) with selectivity and oral bioavailability, exhibiting activity against PI3Kβ/γ/δ that is dozens of times weaker than against PI3Kα (IC₅₀ = 250/290/1200 nM). Alpelisib exhibits targeting activity against PIK3CA-mutated tumors and may be utilized in cancer research.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

IPI-3063 is an effective and selective inhibitor of PI3K p110δ (IC50: 2.5 ± 1.2 nM).

Buparlisib Hydrochloride (BKM120 HCl) is a specific and orally bioavailable pan-class I PI3K inhibitor that competitively inhibits PI3K/AKT kinase at the nanomolar level and suppresses cancer cell growth, making it suitable for studying breast cancer, glioblastoma, and solid tumours.

P110δ-IN-1 (PWT-143) is an effective and selective inhibitor of P110δ (IC50: 8.4 nM).

Sonolisib is an irreversible and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)).

Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).

Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

Pictilisib (GDC-0941) (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ).

GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.

PIK-294 is a excellently specific p110δ inhibitor(IC50=10 nM).