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OSS_128167

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Chemical Structure| 887686-02-4 同义名 : OSS-128167;SIRT6-IN-1
CAS号 : 887686-02-4
货号 : A724428
分子式 : C19H14N2O6
纯度 : 98%
分子量 : 366.324
MDL号 : MFCD07114226
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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

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].
实验方案
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
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.