Home / Histone Acetyltransferase Inhibitors / A 485

A 485

Catalog #: 6387
13 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6387/25
6387/5
A 485 | CAS No. 1889279-16-6 | Histone Acetyltransferase Inhibitors
1 Image
Description: Potent and selective p300/CBP inhibitor; orally bioavailable

Chemical Name: (1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide

Purity: ≥98%

Product Details
Citations (13)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

A 485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC50 values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively), which displays > 1000-fold selectivity over closely related HATs. A 485 suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro, and also inhibits tumor growth in a castration-resistant prostate cancer xenograft model. A 485 is orally bioavailable.

To request the negative control for A 485, please fill out the A 486 request form on the SGC website.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 485 is reviewed on the chemical probes website.

Technical Data

M.Wt:
536.48
Formula:
C25H24F4N4O5
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1889279-16-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A-485 probe summary on the SGC website.

Product Datasheets

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Citations for A 485

The citations listed below are publications that use Tocris products. Selected citations for A 485 include:

13 Citations: Showing 1 - 10

  1. Oncohistone Mutations Occur at Functional Sites of Regulatory ADP-Ribosylation.
    Authors: Anusha Et al.
    Cancer Res  2022;82:2361-2377
  2. A mitotic chromatin phase transition prevents perforation by microtubules.
    Authors: Lynda K Et al.
    Nature  2022;609:183-190
  3. 3D chromatin remodeling potentiates transcriptional programs driving cell invasion.
    Authors: Adriana Et al.
    Proc Natl Acad Sci U S A  2022;119:e2203452119
  4. H3K27ac bookmarking promotes rapid post-mitotic activation of the pluripotent stem cell program without impacting 3D chromatin reorganization.
    Authors: Aristotelis Et al.
    Mol Cell  2021;81:1732-1748.e8
  5. A unique bipartite Polycomb signature regulates stimulus-response transcription during development.
    Authors: Hubertus Et al.
    Nat Genet  2021;53:379-391
  6. The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress.
    Authors: Johan Et al.
    Nat Aging  2021;1:165-178
  7. The single-cell epigenomic and transcriptional landscape of immunity to influenza vaccination.
    Authors: Peggie Et al.
    Cell  2021;184:3915-3935.e21
  8. Nuclear ADP-ribosylation drives IFNγ-dependent STAT1α enhancer formation in macrophages.
    Authors: Rebecca Et al.
    Nat Commun  2021;12:3931
  9. Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer.
    Authors: Marc Et al.
    Elife  2021;10
  10. ARID1A Mutations Promote P300-Dependent Endometrial Invasion through Super-Enhancer Hyperacetylation.
    Authors: Asgerally T Et al.
    Cell Rep  2020;33:108366

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