6387/5 | Tocris Bioscience 6387/5 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

6387/5

catalog :

6387/5

quantity :

5 mg (also 25 mg)

price :

307 USD

more info or order :

Tocris Bioscience product webpage

citations: 13

Reference
Lebeau B, Jangal M, Zhao T, Wong C, Wong N, Ca xf1 edo E, et al. 3D chromatin remodeling potentiates transcriptional programs driving cell invasion. Proc Natl Acad Sci U S A. 2022;119:e2203452119 pubmed publisher
Schneider M, Gibson B, Otsuka S, Spicer M, Petrovic M, Blaukopf C, et al. A mitotic chromatin phase transition prevents perforation by microtubules. Nature. 2022;609:183-190 pubmed publisher
Huang D, Camacho C, Martire S, Nagari A, Setlem R, Gong X, et al. Oncohistone Mutations Occur at Functional Sites of Regulatory ADP-Ribosylation. Cancer Res. 2022;82:2361-2377 pubmed publisher
Wimmers F, Donato M, Kuo A, Ashuach T, Gupta S, Li C, et al. The single-cell epigenomic and transcriptional landscape of immunity to influenza vaccination. Cell. 2021;184:3915-3935.e21 pubmed publisher
Gupte R, Nandu T, Kraus W. Nuclear ADP-ribosylation drives IFNγ-dependent STAT1α enhancer formation in macrophages. Nat Commun. 2021;12:3931 pubmed publisher
Inoue Y, Nikolic A, Farnsworth D, Shi R, Johnson F, Liu A, et al. Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. elife. 2021;10: pubmed publisher
Pelham Webb B, Polyzos A, Wojenski L, Kloetgen A, Li J, Di Giammartino D, et al. H3K27ac bookmarking promotes rapid post-mitotic activation of the pluripotent stem cell program without impacting 3D chromatin reorganization. Mol Cell. 2021;81:1732-1748.e8 pubmed publisher
Li T, Sleiman M, Li H, Gao A, Mottis A, Bachmann A, et al. The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress. Nat Aging. 2021;1:165-178 pubmed publisher
Kitazawa T, Machlab D, Joshi O, Maiorano N, Kohler H, Ducret S, et al. A unique bipartite Polycomb signature regulates stimulus-response transcription during development. Nat Genet. 2021;53:379-391 pubmed publisher
Wilson M, Reske J, Holladay J, Neupane S, Ngo J, Cuthrell N, et al. ARID1A Mutations Promote P300-Dependent Endometrial Invasion through Super-Enhancer Hyperacetylation. Cell Rep. 2020;33:108366 pubmed publisher
Gao Y, Nihira N, Bu X, Chu C, Zhang J, Kolodziejczyk A, et al. Acetylation-dependent regulation of PD-L1 nuclear translocation dictates the efficacy of anti-PD-1 immunotherapy. Nat Cell Biol. 2020;22:1064-1075 pubmed publisher
Gal J, Chen J, Na D, Tichacek L, Barnett K, Zhu H. The Acetylation of Lysine-376 of G3BP1 Regulates RNA Binding and Stress Granule Dynamics. Mol Cell Biol. 2019;39: pubmed publisher
Oliva J, Galasinski S, Richey A, Campbell A, Meyers M, Modi N, et al. Clinically advanced p38 inhibitors suppress DUX4 expression in cellular and animal models of facioscapulohumeral muscular dystrophy. J Pharmacol Exp Ther. 2019;: pubmed publisher

product information

master code :

6387

SKU :

6387/5

product name :

A 485

unit size :

5 mg (also 25 mg)

description :

Potent and selective p300/CBP inhibitor; orally bioavailable

target :

Histone Acetyltransferase Inhibitors

category :

Small Molecules

purity :

98%

observed molecular weight :

536.48

url print :

?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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.

top caption :

Potent and selective p300/CBP inhibitor; orally bioavailable

extended description :

Potent and selective p300/CBP inhibitor; orally bioavailable

chemical name text :

(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

formula :

C25H24F4N4O5

formula text :

C25H24F4N4O5

cas num :

1889279-16-6

USD :

307 USD

product details :

Potent and selective p300/CBP inhibitor; orally bioavailable

storage :

Store at -20░C

more info or order :

Tocris Bioscience product webpage