PI3Kγ Inhibitor

SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC₅₀ of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC₅₀ of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy.

AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC₅₀ of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases.

PI3K/HDAC-IN-5 is a dual PI3K/HDAC inhibitor. PI3K/HDAC-IN-5 inhibits PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC₅₀ values of 25.41, 134.52, 166.75, and 41.58 nM, respectively) and inhibits downstream PI3K/AKT signaling. PI3K/HDAC-IN-5 inhibits HDAC6, HDAC8, and HDAC11 (IC₅₀ values of 29.35, 157.27, and 382.26 nM, respectively), increases α-tubulin and SMC3 acetylation, while not affecting histone H3/H4 acetylation. PI3K/HDAC-IN-5 induces S phase cell cycle arrest and apoptosis, and inhibits the proliferation of cervical cancer cell lines. PI3K/HDAC-IN-5 can be used for research on cervical cancer.

FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer.

PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC₅₀s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research.

IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC₅₀ values for PI3Kγ and PI3Kδ of 4.0 and 9.1 nM, respectively. IHMT-PI3K-315 has antitumor activity.

PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pK_i of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC₅₀ of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats.

Rac)-AZD8186 is the racemate of AZD8186 (HY-12330), a PI3K inhibitor that inhibits PI3Kβ (IC₅₀=4 nM), PI3Kδ (IC₅₀=12 nM), PI3Kα (IC₅₀=35 nM) and PI3Kγ (IC₅₀=675 nM).

AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC₅₀: 8 nM; K_i: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC₅₀ values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC₅₀ values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice.

MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.

PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC₅₀s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research.

PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC₅₀ values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research.

LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC₅₀ = 0.071 μM, PI3Kβ IC_{50 =} 0.17 μM, PI3Kγ IC₅₀ = 0.66 μM, PI3Kδ IC₅₀ = 0.072 μM, BRD4 BD1 IC₅₀ = 0.19 μM, and BRD4 BD2 IC₅₀ = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma.

HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC₅₀s of 4  and 5  μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research.

PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC₅₀ values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity. PI3Kγ inhibitor 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.

IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC₅₀s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8⁺ killing T cells.IHMT-PI3K-455 is used in cancer research.

PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC₅₀ = 5.8), with pKi values of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. PI3Kδ-IN-12 can be used in the study of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

PP162 is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ of 53 nM. PP162 selectively inhibits DNA-PK by binding to a conserved hydrophobic pocket. PP162 exhibits weak inhibitory activity against various tyrosine kinases and PI3K family members. PP162 can be used for research on selective kinase targeting.