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5-(3-(呋喃-2-甲酰胺基)苯甲酰氨基)-2-羟基苯甲酸 /OSS_128167 {[allProObj[0].p_purity_real_show]}

货号:A724428 同义名: OSS-128167;SIRT6-IN-1

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-cancer, anti-inflammation and anti-viral effects.

OSS_128167 化学结构 CAS号:887686-02-4
OSS_128167 化学结构
CAS号:887686-02-4
OSS_128167 3D分子结构
CAS号:887686-02-4
OSS_128167 化学结构 CAS号:887686-02-4
OSS_128167 3D分子结构 CAS号:887686-02-4
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OSS_128167 纯度/质量文件 产品仅供科研

货号:A724428 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 SIRT1 SIRT2 SIRT3 SIRT5 SIRT6 SIRT7 Sirtuin 其他靶点 纯度
Selisistat ++++

SIRT1, IC50: 38 nM

99%+
Resveratrol 98%
Inauhzin p53 99%+
Suramin sodium salt +++

SirT1, IC50: 297 nM

++

SirT5, IC50: 22 μM

99%+
Salermide 98%
Quercetin Dihydrate 95%
Sirtinol +

SIRT1, IC50: 131 μM

++

SIRT2, IC50: 38 μM

98%+
AGK2 +++

SIRT2, IC50: 3.5 μM

99%+
Tenovin-3 p53 99%+
3-TYP ++++

SIRT1, IC50: 88 nM

++++

SIRT2, IC50: 92 nM

++++

SIRT3, IC50: 16 nM

95%
Tenovin-6 ++

SIRT1, IC50: 21 μM

++

SIRT2, IC50: 10 μM

+

SIRT3, IC50: 67 μM

p53 99%+
SirReal2 +++

SIRT2, IC50: 140 nM

99%+
Thiomyristoyl ++++

SIRT2, IC50: 28 nM

99%+
Et-29 98%
OSS_128167 +

SIRT1, IC50: 1578 μM

+

SIRT2, IC50: 751 μM

+

SIRT6, IC50: 89 μM

98%
SIRT7 inhibitor 97491 +++

SIRT7, IC50: 325 nM

97%
Nicotinamide 99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

OSS_128167 生物活性

靶点
  • SIRT1

    SIRT1, IC50:1578 μM

  • SIRT2

    SIRT2, IC50:751 μM

  • SIRT6

    SIRT6, IC50:89 μM

描述 Sirtuin 6 (SIRT6) is a NAD+-dependent deacetylase that regulates DNA repair, telomere maintenance, glucose and lipid metabolism, inflammation, and cancer. OSS_128167 is a selective SIRT6 inhibitor with IC50 values of 89 ± 5μM, 1578 ± 47μM, and 751 ± 23μM for SIRT6, SIRT1, and SIRT2, respectively[4]. OSS_128167 inhibited hepatitis B virus (HBV) transcription and replication in vitro at a concentration of 100μM. In HepG2.2.15 and HBV-infected HepG2-sodium taurocholate cotransporting polypeptide cells, the promotion of SIRT6 overexpression on HBV transcription and replication was blocked by OSS_128167 at 100μM. Administration of HBV transgenic mice with 50mg/kg OSS_128167 resulted in a significant reduction of HBV DNA in serum, as well as serum hepatitis B surface antigen and hepatitis B envelope antigen[5].

OSS_128167 参考文献

[1]Parenti MD, et al. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804.

[2]Jiang H, et al. SIRT6 Inhibitor, OSS_128167 Restricts Hepatitis B Virus Transcription and Replication Through Targeting Transcription Factor Peroxisome Proliferator-Activated Receptors α. Front Pharmacol. 2019 Oct 25;10:1270.

[3]Cea M, et al. Evidence for a role of the histone deacetylase SIRT6 in DNA damage response of multiple myeloma cells. Blood. 2016 Mar 3;127(9):1138-50.

[4]Parenti MD, Grozio A, Bauer I, Galeno L, Damonte P, Millo E, Sociali G, Franceschi C, Ballestrero A, Bruzzone S, Del Rio A, Nencioni A. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804.

[5]Jiang H, Cheng ST, Ren JH, Ren F, Yu HB, Wang Q, Huang AL, Chen J. SIRT6 Inhibitor, OSS_128167 Restricts Hepatitis B Virus Transcription and Replication Through Targeting Transcription Factor Peroxisome Proliferator-Activated Receptors α. Front Pharmacol. 2019 Oct 25;10:1270.

OSS_128167 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.65mL

2.73mL

1.36mL

27.30mL

5.46mL

2.73mL

OSS_128167 技术信息

CAS号887686-02-4
分子式C19H14N2O6
分子量 366.324
别名 OSS-128167;SIRT6-IN-1
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 100 mg/mL(272.98 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water 12 mg/mL

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