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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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

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524619
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
701947-53-7C₁₆H₁₅N₃O₄S

Pricing & Availability

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524619-25MG
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      		 Glass bottle 25 mg
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      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
      Catalog Number GTIN
      524619-25MG 04055977197464

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      524619

      References

      Reference overview
      Miao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
      Skidan, I., et al. 2009. Drug Deliv. 16, 45.
      Data Sheet

      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.