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

IHMT-PI3Kδ-372 

Cat. No.: HY-131910 Purity: 99.75%
COA 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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Solution
10 mM * 1 mL in DMSO USD 255 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 230 In-stock
10 mg USD 368 In-stock
25 mg USD 736 In-stock
50 mg USD 1177 In-stock
100 mg USD 1880 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

IHMT-PI3Kδ-372 Related Antibodies

Top Publications Citing Use of Products

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 CYP19 CYP26 CYP51

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

IHMT-PI3Kδ-372 Related Antibodies

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

Appearance

Solid

Formula

C26H23F2N7O2
CAS No.
SMILES

CC[C@H](C(N1C2CC2)=NC3=CC=CC(F)=C3C1=O)N4C5=NC=NC(N)=C5C(C6=CC(F)=C(C=C6)OC)=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (82.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9861 mL 9.9305 mL 19.8610 mL
5 mM 0.3972 mL 1.9861 mL 3.9722 mL
10 mM 0.1986 mL 0.9930 mL 1.9861 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.13 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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IHMT-PI3Kδ-372 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

IHMT-PI3Kδ-3722429889-62-1PI3KCytochrome P450Phosphoinositide 3-kinaseCYPsPI3KδCOPDinhalationCYP2C9chronicobstructivepulmonarydiseaseInhibitorinhibitorinhibit

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