C646|cas:328968-36-1|西域试剂

C646,98.0%

产品编号：Bellancom-13823| CAS NO：328968-36-1| 分子式：C₂₄H₁₉N₃O₆| 分子量：445.42

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-13823		￥980.00	杭州北京（现货）
Bellancom-13823		￥3800.00	杭州北京（现货）

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C646

产品介绍

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

生物活性

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

体外研究

C646 is a linear competitive inhibitor of p300 versus acetyl-CoA with a K_i 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. C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells. C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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].

西域 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.

体内研究

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].

西域 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.

性状

Solid

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (3.75 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (3.75 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明