跳转至内容
Merck
CN

SML2192

A-485

≥98% (HPLC), catalytic p300/CBP inhibitor, powder

别名:

N-(4-fluorobenzyl)-2-((R)-5-(3-methylureido)-2′,4′-dioxo-2,3-dihydrospiro[indene-1,5′-ozazolidine]-3′-7 yl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide, Spiro[1H-indene-1,5′-oxazolidine]-3′-acetamide, N-[(4-fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2′,4′-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-, (1R)-

登录 查看组织和合同定价。

选择尺寸

关于此项目

经验公式（希尔记法）:
C25H24F4N4O5
化学文摘社编号:
1889279-16-6
分子量:
536.48
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD31619258

主要文件

查看所有文档
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助

产品名称

A-485, ≥98% (HPLC)

InChI

1S/C25H24F4N4O5/c1-14(25(27,28)29)32(12-15-3-5-17(26)6-4-15)20(34)13-33-21(35)24(38-23(33)37)10-9-16-11-18(7-8-19(16)24)31-22(36)30-2/h3-8,11,14H,9-10,12-13H2,1-2H3,(H2,30,31,36)/t14-,24+/m0/s1

InChI key

VRVJKILQRBSEAG-LFPIHBKWSA-N

SMILES string

CNC(NC1=CC=C2C(CC[C@]23C(N(CC(N(CC4=CC=C(F)C=C4)[C@@H](C)C(F)(F)F)=O)C(O3)=O)=O)=C1)=O

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +40 to +50°, c = 0.5 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

相关类别

Application

A-485 has been used as a p300 regulated RelA acetylation inhibitor to study the effect of fatty acid oxidation (FAO) derived cytoplasmic acetyl-CoA on CD47 transcription and protein stability via citrate/acetyl-CoA mediated RelA acetylation in glioblastoma.

Biochem/physiol Actions

A-485 exhibits an anti-tumor effect and may show therapeutic effects against the growth hormone pituitary adenoma (GHPA). It can specifically block the acetylation of histone H3 lysine 27 (H3K27) and lysine 18 (H3K18) sites catalyzed by p300.
A-485 is a potent and selective catalytic inhibitor of the p300 and CREB-binding protein (CBP) histone acetyltransferases (HATs) with an IC50 value of 60 nM. A-485 was most active against haematological malignancies including most multiple myeloma cell lines as well as androgen receptor-positive prostate cancer. It was also shown to inhibit the proliferation of castration-resistant prostate cancer cells and in vivo tumour growth in SCID mice.
Selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000484875
0000484874
0000484874
0000484875
0000405938

没有发现合适的版本？

如果您需要特殊版本，可通过批号或批次号查找具体证书。

搜索COA

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

Chenxing Ji et al.
The Journal of clinical endocrinology and metabolism, 107(6), e2291-e2300 (2022-03-06)
Growth hormone pituitary adenoma (GHPA), a major subtype of pituitary adenoma (PA), can lead to progressive somatic disfigurement, multiple complications, and even increased mortality. The efficacy of current treatments is limited; thus, a novel pharmacological treatment is urgently needed. As
Loren M Lasko et al.
Nature, 550(7674), 128-132 (2017-09-28)
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases (HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of gene transcription and is associated with multiple diseases. Histone deacetylase inhibitors are currently approved to treat certain
Nian Jiang et al.
Nature communications, 13(1), 1511-1511 (2022-03-23)
Glioblastoma multiforme (GBM) remains the top challenge to radiotherapy with only 25% one-year survival after diagnosis. Here, we reveal that co-enhancement of mitochondrial fatty acid oxidation (FAO) enzymes (CPT1A, CPT2 and ACAD9) and immune checkpoint CD47 is dominant in recurrent

我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系客户支持