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506071 InSolution™ I-BET - CAS 1260907-17-2 - Calbiochem

A 50 mM sterile-filtered solution of I-BET in DMSO.

InSolution™ I-BET - CAS 1260907-17-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide

Primary Target: tandem bromodomains of BET
506071
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1260907-17-2C₂₂H₂₂ClN₅O₂

Products

Catalogue NumberPackaging Qty/Pack
5.06071.0001 Sklená flaša 5 mg
Description
Catalogue Number506071
Brand Family Calbiochem®
Synonyms(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
References
ReferencesNicodeme, E., et al. 2010. Nature 468, 1119.
Product Information
CAS number1260907-17-2
FormLiquid
FormulationA 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.
Hill FormulaC₂₂H₂₂ClN₅O₂
Chemical formulaC₂₂H₂₂ClN₅O₂
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targettandem bromodomains of BET
Purity≥98% by Chiral 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 Dry Ice Only
Toxicity Standard Handling
Storage ≤ -70°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Avoid freeze/thaw Avoid freeze/thaw
Do not freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots 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
Catalogue Number GTIN
5.06071.0001 04055977243048

Documentation

InSolution™ I-BET - CAS 1260907-17-2 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Nicodeme, E., et al. 2010. Nature 468, 1119.
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.

Revision11-July-2014 JSW
Synonyms(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
DescriptionA cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain) family members BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity (Kd = 61.3, 50.5, and 55.2 nM, respectively, by ITC) and effectively competes against tetra-acetylated H4 peptide (Millipore cat. no. 12-379) for BRD2/3/4 binding (IC50 = 32.5, 42,4, and 36.1 nM, respectively, in competitive equilibrium binding assays), while exhibiting little affinity toward 5 other bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140) or a panel of 38 cellular enzymes, GPCRs, transporters, and ion channels. Shown to differentially modulate LPS-induced gene expression, notably suppressing LPS-induced upregulation of genes involved in inflammatory response, in murine BMDMs (bone marrow-derived macrophages) in vitro (30 min 1 µM pretreatment) and effectively prevent LPS-, heat-killed Salmonella typhimurium-, and CLP- (caecal ligation and puncture) induced death in mice in vivo (30 mg/kg i.v.). Cellular Brd2/3/4 knockdown using siRNA results in mostly the same effect as I-BET treatment in modulating LPS gene induction profile in murine BMDMs, but not without exceptions, indicating that not all BET-dependent transcription regulations are mediated via its binding to acetylated histones.
FormLiquid
FormulationA 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.
Intert gas (Yes/No) Packaged under inert gas
CAS number1260907-17-2
Chemical formulaC₂₂H₂₂ClN₅O₂
Structure formulaStructure formula
Purity≥98% by Chiral HPLC
Storage Protect from light
Avoid freeze/thaw
≤ -70°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesNicodeme, E., et al. 2010. Nature 468, 1119.