(-)-DHMEQ Dehydroxymethylepoxyquinomicin|cas:287194-40-5|西域试剂

(-)-DHMEQ Dehydroxymethylepoxyquinomicin,98.47%

产品编号：Bellancom-14645| CAS NO：287194-40-5| 分子式：C₁₃H₁₁NO₅| 分子量：261.23

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货号	价格	库存与货期
Bellancom-14645	￥1400.00	杭州北京（现货）
Bellancom-14645	￥2200.00	杭州北京（现货）
Bellancom-14645	￥3000.00	杭州北京（现货）
Bellancom-14645	￥6000.00	杭州北京（现货）

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(-)-DHMEQ Dehydroxymethylepoxyquinomicin

产品介绍

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) 是一种有效，选择性且不可逆的 NF-κB 抑制剂，与半胱氨酸残基共价结合。(-)-DHMEQ 抑制 NF-κB 的核易位，并显示抗炎和抗癌活性。

生物活性

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.

体外研究

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity.
(-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines.
(-)-DHMEQ (10 μg/mL; 4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9.
(-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ.
(-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB.

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

Cell Proliferation Assay

Cell Line:	TL-Om1, MT-1, KK-1, ST-1 and K562 cells
Concentration:	2 μg/mL, 5 μg/mL, 10 μg/mL
Incubation Time:	12 hours, 24 hours, 48 hours
Result:	Significantly reduced the viability of all cell lines in a dose- and time-dependent manner.

Apoptosis Analysis

Cell Line:	TL-Om1, MT-1 and K562 cells
Concentration:	10 μg/mL
Incubation Time:	0 hours, 24 hours, 48 hours
Result:	Annexin V-positive cells were significantly increased after 24 to 48 hours.

Western Blot Analysis

Cell Line:	MT-1 cells
Concentration:	10 μg/mL
Incubation Time:	4 hours, 8 hours, 16 hours
Result:	Annexin V-positive cells were significantly increased after 24 to 48 hours.

体内研究
(In Vivo)

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 4 mg/kg or 12 mg/kg; intraperitoneal injection; on day 0 and 3 times a week; for one month; SCID mice) treatment shows a significant increase in the survival rate in mice.

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

Animal Model:	Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells
Dosage:	4 mg/kg or 12 mg/kg
Administration:	Intraperitoneal injection; on day 0 and 3 times a week; for one month
Result:	Showed a significant increase in the survival rate in mice.

体内研究

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

Animal Model:	Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells
Dosage:	4 mg/kg or 12 mg/kg
Administration:	Intraperitoneal injection; on day 0 and 3 times a week; for one month
Result:	Showed a significant increase in the survival rate in mice.

体内研究

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

Animal Model:	Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells
Dosage:	4 mg/kg or 12 mg/kg
Administration:	Intraperitoneal injection; on day 0 and 3 times a week; for one month
Result:	Showed a significant increase in the survival rate in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (191.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8280 mL	19.1402 mL	38.2804 mL
5 mM	0.7656 mL	3.8280 mL	7.6561 mL
10 mM	0.3828 mL	1.9140 mL	3.8280 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 (stored under nitrogen)。-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: 5 mg/mL (19.14 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (19.14 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 50.0 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