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500614 Survivin Inhibitor III, LLP-3 - Calbiochem

Survivin Inhibitor III, LLP-3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Survivin-Ran Interaction Blocker, LLP3, 4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile

Primary Target: survivin
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Přehled

Replacement Information

Tabulka spec. kláve

Empirical Formula
C₃₂H₂₃ClN₂O₄
Description
Overview

This product has been discontinued.



A cell-permeable, dihydropyridinone compound that selectively disrupts survivin-Ran interaction in cell-free binding assays (IC50 <0.3 µM) and in U87 glioma cells (by 55% in 24 h; 20 µM) via direct binding at survivin protein-protein interaction interface, while exhibiting much reduced or little potency against survivin-Smac/DIABLO, survivin-survivin, or XIAP-Smac/DIABLO interaction. LLP-3 treatment abrogates neurosphere formation in GMB cultures (IC50 ≤35 µM) by selectively depleting CD133+ GSC population via apoptosis induction. TMZ (Cat. No. 500609), in comparison, enriches GMB GSC population by preferentially eradicating non-GSC population. LLP-3 is also efficacious in treating human GMB xenograft in mice in vivo (25 mg/kg/day via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number500614
Brand Family Calbiochem®
SynonymsSurvivin-Ran Interaction Blocker, LLP3, 4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile
References
ReferencesGuvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.
Product Information
FormYellow solid
Hill FormulaC₃₂H₂₃ClN₂O₄
Chemical formulaC₃₂H₂₃ClN₂O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targetsurvivin
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
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
Katalogové číslo GTIN
500614 0

Documentation

Survivin Inhibitor III, LLP-3 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
Guvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.
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.

Revision10-May-2013 JSW
SynonymsSurvivin-Ran Interaction Blocker, LLP3, 4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile
DescriptionA cell-permeable, bioavailable dihydropyridinone compound that selectively disrupts survivin-Ran interaction (IC50 <0.3 µM) in cell-free binding assays and in cells (by 55% in U87 glioma cells after 24 h 20 µM treatment) via direct binding at survivin protein-protein interaction interface, while exhibiting much reduced or little potency against survivin-Smac/DIABLO, survivin-survivin, or XIAP-Smac/DIABLO interaction. Survivin and Ran expressions are reported to be upregulated in GSCs (glioma stem cells; CD133-/Nestin-/Sox2-/MELK-positive and TuJ1-negative) when compared to non-GSC (TuJ1-positive) population in patients-derived GMB (Glioblastoma multiforme) cultures and LLP-3 treatment abrogates neurosphere formation in GMB cultures (IC50 ≤35 µM) by selectively depleting CD133+ GSC population (89% drop of CD133+ population vs. 33% drop in CD133- population in GBM528 cultures after 7 d 25 µM treatment) via apoptosis induction. TMZ treatment, in comparison, results in GMB GSC population enrichment by preferentially eradicating non-GSC population. LLP-3 is also efficacious in treating human GMB xenograft in mice in vivo (median survival days = 35 vs. 15.5 with or without treatment; 25 mg/kg/day via i.p.; 5 d/wk for 2 wks starting d10 post GMB xenograft). TMZ (Cat. No. 500609), in comparison, enriches GMB GSC population by preferentially eradicating non-GSC population.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₂H₂₃ClN₂O₄
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 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 Standard Handling
ReferencesGuvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.