PI3Kα Inhibitor

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.

PI3K/mTOR-IN-23 dihydrochloride is a dual inhibitor of PI3K and mTOR with IC₅₀ values of 49 and 41 nM. PI3K/mTOR-IN-23 dihydrochloride inhibits cancer cells proliferation.

WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC₅₀ of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC₅₀s of 81 nM and 3.11 μM, respectively.

PI3K/mTOR-IN-23 is a dual inhibitor of PI3K and mTOR with IC₅₀ values of 49 and 41 nM. PI3K/mTOR-IN-23 inhibits cancer cells proliferation.

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.

PF-4989216 is a potent and selective PI3Kα inhibitor with a K_i of 0.6 nM.

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.

PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

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.

PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC₅₀ of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC₅₀ = 23 nM), PI3Kδ (IC₅₀ = 340 nM), PI3KC2α (IC₅₀ = 140 nM) and PI3KC2β (IC₅₀ = 370 nM). PIK-124 is applicable to breast cancer-related research.

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.