PI3Kβ Inhibitor

ON 146040 is a potent PI3Kα and PI3Kδ (IC₅₀≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC₅₀<150 nM).

PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC₅₀=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC₅₀=13/190 nM, respectively).

SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC₅₀s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects.

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC₅₀ of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC₅₀ of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.

PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC₅₀ value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies.

PIK-293, an analog of IC87114, is a PI3K inhibitor, with IC₅₀ values of 0.24 μM, 10 μM, 25 μM and 100 μM for p110δ, p110β, p110γ and p110α, respectively.

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

PI3Kδ-IN-15 (compound 6b) is a selective PI3Kδ inhibitor with an IC₅₀ of 0.5 nM for p110δ. PI3Kδ-IN-15 inhibits PI3Kδ with >30-fold higher potency than PI3Kγ, PI3Kβ, and PI3Kα.

Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach.

Nemiralisib hydrochloride (GSK2269557) is a potent and highly selective PI3Kδ inhibitor with a pK_i of 9.9.

Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach.

PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC₅₀ of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC₅₀=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity.

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC₅₀s of 8.1 nM and 1.4 nM, respectively.

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC₅₀s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.

PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC₅₀ values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC₅₀ values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC₅₀ values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively.

AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC₅₀ of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases.

AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC₅₀ of 4.6 nM. AM-1430 exhibits IC₅₀s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases.

PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC₅₀ values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research.