推荐产品
产品名称
组蛋白乙酰转移酶p300抑制剂，C646, Histone Acetyltransferase p300 Inhibitor, C646, CAS 328968-36-1, is a cell-permeable, reversible inhibitor of p300/CBP HAT (Ki = 400 nM). Competes with acetyl-CoA for the p300 Lys-CoA binding pocket.
质量水平
方案
≥99% (sum of isomers, HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
brick red
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-
InChI key
HEKJYZZSCQBJGB-UNOMPAQXSA-N
一般描述
一种可逆、细胞可渗透吡唑啉酮p300/CBP HAT抑制剂（Ki = 400 nM），可与乙酰辅酶A竞争p300 Lys-CoA结合袋。该化合物在10 nM处对p300有86%的抑制作用，但在化学筛选测定中对羟色胺N-乙酰转移酶、PCAF组蛋白乙酰转移酶、GCN5组蛋白乙酰转移酶、Rtt109组蛋白乙酰转移酶、Sas组蛋白乙酰转移酶以及MOZ组蛋白乙酰转移酶的抑制作用均小于10%。使用25µ M化合物处理C3H 10T1/2小鼠成纤维细胞可对组蛋白H3和H4的基础和TSA诱导乙酰化产生抑制效果。研究还表明，与25 µM基于多肽双底物p300/CBP HAT抑制剂Lys-CoA-Tat相比，10µM时可抑制黑色素瘤和非小细胞肺（NSCL）癌细胞系中人类细胞生长，并且具有相似或更高的药效。
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，分装并冷冻保存（-20°C。储备液在-20°C条件下可稳定保存3个月。
其他说明
Bowers, EM., et al. 2010.Chem Biol17, 471.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Kee-Beom Kim et al.
Science advances, 8(7), eabl4618-eabl4618 (2022-02-17)
EP300, a transcription coactivator important in proliferation and differentiation, is frequently mutated in diverse cancer types, including small cell lung cancer (SCLC). While these mutations are thought to result in loss of EP300 function, the impact on tumorigenesis remains largely
Daniel J Puleston et al.
Cell, 184(16), 4186-4202 (2021-07-04)
Polyamine synthesis represents one of the most profound metabolic changes during T cell activation, but the biological implications of this are scarcely known. Here, we show that polyamine metabolism is a fundamental process governing the ability of CD4+ helper T cells (TH)
Virender Kumar Sharma et al.
Scientific reports, 11(1), 16427-16427 (2021-08-14)
Api5, is a known anti-apoptotic and nuclear protein that is responsible for inhibiting cell death in serum-starved conditions. The only known post-translational modification of Api5 is acetylation at lysine 251 (K251). K251 acetylation of Api5 is responsible for maintaining its
Kenji Ohshima et al.
The Journal of pathology, 256(2), 164-173 (2021-10-27)
Cancer cells have an altered metabolic state that supports their growth, for example, aerobic glycolysis, known as the Warburg effect. Colorectal cancer cells have been reported to exhibit the Warburg effect and mainly rely on glycolysis for progression and have
Lu Yang et al.
Communications biology, 4(1), 1373-1373 (2021-12-10)
Tumor suppressor p53, a critical regulator of cell fate, is frequently mutated in cancer. Mutation of p53 abolishes its tumor-suppressing functions or endows oncogenic functions. We recently found that p53 binds via its proline-rich domain to peptidase D (PEPD) and
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.
联系技术服务部门