1. PI3K/Akt/mTOR
    Metabolic Enzyme/Protease
  2. PI3K
    Cytochrome P450
  3. IHMT-PI3Kδ-372

IHMT-PI3Kδ-372 

Cat. No.: HY-131910
Handling Instructions

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

For research use only. We do not sell to patients.

IHMT-PI3Kδ-372 Chemical Structure

IHMT-PI3Kδ-372 Chemical Structure

CAS No. : 2429889-62-1

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Description

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research[1].

IC50 & Target[1]

PI3Kδ

14 nM (IC50)

CYP2C9

2.7 μM (IC50)

In Vitro

IHMT-PI3Kδ-372 (Compound (S)-18; 0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC50 value of 67 nM[1].
IHMT-PI3Kδ-372 (compound (S)-18) shows moderate inhibition of CYP2C9 (IC50 of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC50s > 10 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Raji cells
Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 1 hour
Result: Inhibited PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC50 value of 67 nM.
In Vivo

IHMT-PI3Kδ-372 (Compound (S)-18; 1-5 mg/kg; inhalation; daily; for 28 days) improves lung function and reduced the inflammatory patterns characteristic of COPD. The lung function parameters such as forced expiratory volume in the first second (FEV1), forced vital capacity (FVC), and peak expiratory flow (PEF) are improved dose-dependently. The abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes are also reduced. IHMT-PI3Kδ-372 decreases the inflammatory cell infiltration in a dose-dependent manner[1].
In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (compound (S)-18) displays a half-life of 2.3 h, low exposure of 66 ng/mL, and high clearance of 348.5 mL/min/kg in plasma but high exposure of 5599 ng/g (6 h after inhalation) in lung tissue[1].
IHMT-PI3Kδ-372 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats (5-week-old) induced with cigarette-smoke and LPS[1]
Dosage: 1 mg/kg, 3 mg/kg, and 5 mg/kg
Administration: Inhalation; daily; for 28 days
Result: Improved lung function and reduced the inflammatory patterns characteristic of COPD.
Molecular Weight

503.50

Formula

C₂₆H₂₃F₂N₇O₂

CAS No.

2429889-62-1

SMILES

NC1=NC=NC2=C1C(C3=CC=C(C(F)=C3)OC)=NN2[[email protected]](C(N4C5CC5)=NC6=C(C4=O)C(F)=CC=C6)CC

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

IHMT-PI3Kδ-372PI3KCytochrome P450Phosphoinositide 3-kinaseCYPsPI3KδCOPDinhalationCYP2C9chronicobstructivepulmonarydiseaseInhibitorinhibitorinhibit

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IHMT-PI3Kδ-372
Cat. No.:
HY-131910
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