C646

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

C646  纯度: ≥98.0%

C646 是一种竞争性的选择性 histone acetyltransferase p300 抑制剂,Ki 值为 400 nM,对其他的乙酰转移酶作用较小。

C646

C646 Chemical Structure

CAS No. : 328968-36-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1078 In-stock
10 mg ¥980 In-stock
50 mg ¥3800 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1].

IC50 & Target

Ki: 400 nM (histone acetyltransferase p300)

体外研究
(In Vitro)

C646 is a linear competitive inhibitor of p300 versus acetyl-CoA with a Ki of 400 nM. C646 shows a noncompetitive pattern of p300 inhibition versus H4-15 peptide substrate. C646 treatment reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 has a more potent effect on cell growth than Lys-CoA-Tat does[1]. C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells[2]. C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Suppression of P300 by c646 (intraperitoneally injected, 30 nmol/g/d for 2 weeks) dramatically reduces the level of blood glucose in db/db mice[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fourteen-week-old male db/db mice and normal m/m mice[4]
Dosage: 30 nmol/g
Administration: Intraperitoneally injected; daily; 2 weeks
Result: The db/db mice showed greater body masses and higher levels of fasting blood glucose than the m/m mice.

分子量

445.42

Formula

C24H19N3O6

CAS 号

328968-36-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (37.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2451 mL 11.2254 mL 22.4507 mL
5 mM 0.4490 mL 2.2451 mL 4.4901 mL
10 mM 0.2245 mL 1.1225 mL 2.2451 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Bowers EM, et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28;17(5):471-82.

    [2]. Oike T, et al. C646, a selective small molecule inhibitor of histone acetyltransferase p300, radiosensitizes lung cancer cells by enhancing mitotic catastrophe. Radiother Oncol. 2014 May;111(2):222-7.

    [3]. Zheng WW, et al. EDAG positively regulates erythroid differentiation and modifies GATA1 acetylation through recruiting p300. Stem Cells. 2014 Aug;32(8):2278-89.

    [4]. Zhen Fan, et al. Type 2 diabetes-induced overactivation of P300 contributes to skeletal muscle atrophy by inhibiting autophagic flux. Life Sci. 2020 Aug 10;258:118243.

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