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505760 HDAC6 Inhibitor II, BRD9757 - CAS 1423058-85-9 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1423058-85-8C₆H₉NO₂

Products

Catalog NumberPackaging Qty/Pack
5.05760.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced potency against class IIa HDAC4/5/7/9 (IC50 >12.61 µM). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation in HeLa cells (10 & 30 µM; 24 h) without inducing histone H3 acetylation increase seen with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187). Unlike other Zinc-binding group-containing HDAC inhibitors, BRD9757 does not contain an apparent selectivity-imparting capping structure linked to its hydroxamate.
Catalogue Number505760
Brand Family Calbiochem®
SynonymsN-Hydroxycyclopent-1-enecarboxamide, HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI
References
ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.
Product Information
CAS number1423058-85-8
FormPale orange solid
Hill FormulaC₆H₉NO₂
Chemical formulaC₆H₉NO₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetHDAC6
Purity≥98% 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
Catalog Number GTIN
5.05760.0001 04055977243505

Documentation

HDAC6 Inhibitor II, BRD9757 - CAS 1423058-85-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Wagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.

Technical Info

Title
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
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.

Revision03-September-2020 JSW
SynonymsN-Hydroxycyclopent-1-enecarboxamide, HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI
DescriptionA cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced or little potency against class IIa HDAC4/5/7/9 (IC50 = 21.80, 18.32, 12.61, and >33.33 µM, respectively). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation level in HeLa cells (10 & 30 µM; 24 h) without inducing detectable histone H3 acetylation increase seen in cells treated with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187) or the general HDAC inhibitor SAHA. BRD9757 does not contain an apparent selectivity-imparting capping structure linked to the zinc-binding hydroxamate as seen in other ZBG- (Zinc binding group) containing HDAC inhibitors.
FormPale orange solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1423058-85-8
Chemical formulaC₆H₉NO₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 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
ReferencesWagner, F.F., et al. 2013. J. Med. Chem. 56, 1772.