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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;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
Molecular Weight:
345.37
MDL Number:
MOL File:
701947-53-7.mol
MSDS File:
SDS
Last updated:2023-05-18 11:31:17

3,5-dimethyl PIT-1 Properties

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

3,5-dimethyl PIT-1 price More Price(10)

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

3,5-dimethyl PIT-1 Chemical Properties,Uses,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

3,5-dimethyl PIT-1 Suppliers

Global( 28)Suppliers
Supplier Tel Email Country ProdList Advantage
Aladdin Scientific
+1-+1(833)-552-7181 sales@aladdinsci.com United States 52927 58
Sigma-Aldrich 021-61415566 800-8193336 orderCN@merckgroup.com China 51471 80
Shanghai EFE Biological Technology Co., Ltd. 021-65675885 18964387627 info@efebio.com China 9707 58
Shanghai Hongye Biotechnology Co. Ltd 400-9205774 sales@glpbio.cn China 6870 58
DC Chemicals 021-58447131 13564518121 sales@dcchemicals.com China 9412 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 18818260767 sales@chemegen.com China 11289 58
MedBioPharmaceutical Technology Inc 021-69568360 18916172912 order@med-bio.cn China 8141 58
TargetMol Chemicals Inc. 4008200310 marketing@tsbiochem.com China 23980 58
Shanghai Yiyan Biotechnology Co. , Ltd. 021-69985186 13611928337 3427709316@qq.com China 7979 58
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 701947-53-7