ChemicalBook > CAS DataBase List > 3,5-dimethyl PIT-1

3,5-dimethyl PIT-1

Product Name
3,5-dimethyl PIT-1
CAS No.
701947-53-7
Chemical Name
3,5-dimethyl PIT-1
Synonyms
DM-PIT-1;3,5-dimethyl PIT-1;DM-PIT-1 (3,5-dimethyl PIT-1);3,5 dimethyl PIT 1,3,5dimethyl PIT1;3,5-dimethyl PIT-1, PIP3/protein binding inhibitor;PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem;N-[(2-hydroxy-5-nitrophenyl)carbamothioyl]-3,5-dimethylbenzamide;Benzamide, N-[[(2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-3,5-dimethyl-
CBNumber
CB42590015
Molecular Formula
C16H15N3O4S
Formula Weight
345.37
MOL File
701947-53-7.mol
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3,5-dimethyl PIT-1 Property

storage temp. 
+2C to +8C
solubility 
DMF:30.0(Max Conc. mg/mL);86.86(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.45(Max Conc. mM)
DMSO:20.0(Max Conc. mg/mL);57.91(Max Conc. mM)
Ethanol:0.2(Max Conc. mg/mL);0.58(Max Conc. mM)
form 
Off-white powder
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
524619
Product name
PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem<br />The PIP3 Antagonist II, DM-PIT-1, also referenced under CAS 701947-53-7, controls the biological activity of PIP3.
Packaging
25mg
Price
$251
Updated
2024/03/01
Cayman Chemical
Product number
10727
Product name
3,5-dimethyl PIT-1
Purity
≥98%
Packaging
1mg
Price
$26
Updated
2024/03/01
Cayman Chemical
Product number
10727
Product name
3,5-dimethyl PIT-1
Purity
≥98%
Packaging
5mg
Price
$111
Updated
2024/03/01
Cayman Chemical
Product number
10727
Product name
3,5-dimethyl PIT-1
Purity
≥98%
Packaging
10mg
Price
$195
Updated
2024/03/01
Cayman Chemical
Product number
10727
Product name
3,5-dimethyl PIT-1
Purity
≥98%
Packaging
25mg
Price
$426
Updated
2024/03/01
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3,5-dimethyl PIT-1 Chemical Properties,Usage,Production

Description

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.

General Description

A cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH domains of Akt1 (IC50 ≥31 μM), ARNO, GRP1, and PKD1. Effectively blocks PIP3-dependent cellular PI3K-PDK1-Akt signaling pathway activation in U87MG (25 to 100 μM for 3 d) and PDGF-induced Akt and GRP membrane translocation in serum-starved SUM159 cells (1 h 100 μM pretreatment), while being inactive against PDGF-induced Btk translocation or PMA-induced PLC-δ and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles enhances its solubility (up to 1 mM) and i.v. dosing limit for more effective in vivo administrations (5% vs. 41% of control 4T1 tumor size in mice via 1 mg/kg micelles-formulated or 0.4 mg/kg free drug daily i.v., respectively).

3,5-dimethyl PIT-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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701947-53-7, 3,5-dimethyl PIT-1Related Search:


  • 3,5-dimethyl PIT-1
  • N-[(2-hydroxy-5-nitrophenyl)carbamothioyl]-3,5-dimethylbenzamide
  • DM-PIT-1 (3,5-dimethyl PIT-1)
  • PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem
  • Benzamide, N-[[(2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-3,5-dimethyl-
  • DM-PIT-1
  • 3,5 dimethyl PIT 1,3,5dimethyl PIT1
  • 3,5-dimethyl PIT-1, PIP3/protein binding inhibitor
  • 701947-53-7