OSS_128167
目录号 : KM2768 CAS No. : 887686-02-4 纯度 : 98%

OSS_128167 是一种有效的选择性沉默调节蛋白 6 (SIRT6) 抑制剂,对 SIRT6,SIRT1 和 SIRT2 的 IC50 分别为 89 μM,1578 μM 和 751 μM。OSS_128167 具有抗 HBV 活性,可抑制 HBV 的转录和复制。OSS_128167 具有抗癌,抗炎和抗病毒作用。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC50s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-acncer, anti-inflammation and anti-viral effects.

体外研究

OSS_128167 (Compound 9; 100 µM; 0-24 hours; BxPC3 cells) treatment increases H3K9 acetylation. And also increases GLUT-1 expression in BxPC-3 cells.
OSS_128167 (Compound 9) effectively blunts phorbol myristate acetate (PMA)-induced TNF-α secretion in cultured BxPC-3 cells. OSS_128167 increases glucose uptake in cells.
OSS_128167 (100 µM; 96 hours; HepG2.2.15 and HepG2-NTCP cells) treatment significantly decreaseS HBV core DNA and 3.5-Kb RNA levels. OSS_128167 treatment also inhibits hepatitis B surface antigen (HBsAg) and hepatitis B envelope antigen (HBeAg) secretions, as well as HBsAg expression in cell lysates.
OSS_128167 (200 μM) induces chemosensitization in primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines.

Western Blot Analysis

Cell Line: BxPC3 cells
Concentration: 100 µM
Incubation Time: 0 hours, 2 hours, 6 hours, 18 hours, 24 hours
Result: Increased H3K9 acetylation.

RT-PCR

Cell Line: HepG2.2.15 and HepG2-sodium taurocholate cotransporting polypeptide (NTCP) cells
Concentration: 100 µM
Incubation Time: 96 hours
Result: Significantly decreased HBV core DNA and 3.5-Kb RNA levels.
体内研究

OSS_128167 (50 mg/kg; intraperitoneal injection; every 4 days; for 12 days; male HBV transgenic mice) treatment markedly suppresses the level of HBV DNA and 3.5-Kb RNA in HBV transgenic mice.

Animal Model: Male HBV transgenic mice (6-8-week-old)
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; every 4 days; for 12 days
Result: The level of HBV DNA and 3.5-Kb RNA were markedly suppressed in HBV transgenic mice.
分子式
C19H14N2O6
分子量
366.32
CAS号
887686-02-4
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 : 103.3 mg/mL (281.99 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7299 mL 13.6493 mL 27.2985 mL
5 mM 0.5460 mL 2.7299 mL 5.4597 mL
10 mM 0.2730 mL 1.3649 mL 2.7299 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: ≥ 2.5 mg/mL (6.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.82 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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