Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

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.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-​(((2-Hydroxy-​5-​nitrophenyl)amino)thioxomethyl)-​3,​5-​dimethyl-​benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI

524619
Purchase on Sigma-Aldrich

Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
701947-53-7C₁₆H₁₅N₃O₄S

Products

RéférenceConditionnement Qté
524619-25MG Flacon en verre 25 mg
Description
OverviewA 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).
Catalogue Number524619
Brand Family Calbiochem®
SynonymsN-​(((2-Hydroxy-​5-​nitrophenyl)amino)thioxomethyl)-​3,​5-​dimethyl-​benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI
References
ReferencesMiao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
Skidan, I., et al. 2009. Drug Deliv. 16, 45.
Product Information
CAS number701947-53-7
FormOff-white powder
Hill FormulaC₁₆H₁₅N₃O₄S
Chemical formulaC₁₆H₁₅N₃O₄S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Regulatory Review
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
524619-25MG 04055977197464

Documentation

PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem Certificats d'analyse

TitreNuméro de lot
524619

Références bibliographiques

Aperçu de la référence bibliographique
Miao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
Skidan, I., et al. 2009. Drug Deliv. 16, 45.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision17-July-2012 JSW
SynonymsN-​(((2-Hydroxy-​5-​nitrophenyl)amino)thioxomethyl)-​3,​5-​dimethyl-​benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI
DescriptionA cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH (pleckstrin-homology) domains of Akt1 (IC50 ≥31 µM using recombinant human Akt1 aa 1-123), ARNO, GRP1, and PKD1, while lacking activity against PIP3 Btk PH domain ineraction, PI-4,5-P2 (Cat. Nos. 524614, 524644, and 524646) PLC-δ PH domain binding, or PI-3,4-P2 TAPP1/2 PH domains binding, resulting in effective blockage of PIP3-dependent PI3K-PDK1-Akt signaling pathway activation in human glioblastoma U87MG cultures (25 to 100 µM for 3 d) and (5 min 100 ng/ml) PDGF-induced Akt and GRP membrane translocation (by 85% and 70%, respectively, with 1 h 100 µM pretreatment) in serum-starved human breast cancer SUM159 cells, while being inactive against PDGF-induced Btk translocation or (5 min 250 ng/ml) 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 is reported to enhance its solubility (up to 1 mM), and presumably delivery efficiency (57% vs. 67% U87MG viability after 24 h 50 µM drug treatment, respectively, with or without PEG-PE encapsulation), making large dosage delivery possible for more effective in vivo administrations (5% vs. 41% of control 4T1 tumor size in mice after 8 daily i.v. dosages of 1 mg/kg micelles-formulated or 0.4 mg/kg free drug, respectively).
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number701947-53-7
Chemical formulaC₁₆H₁₅N₃O₄S
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Regulatory Review
ReferencesMiao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
Skidan, I., et al. 2009. Drug Deliv. 16, 45.