1. Cell Cycle/DNA Damage
    Epigenetics
    Anti-infection
  2. Sirtuin
    HBV
  3. OSS_128167

OSS_128167 

Cat. No.: HY-107454 Purity: 98.22%
Handling Instructions

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.

For research use only. We do not sell to patients.

OSS_128167 Chemical Structure

OSS_128167 Chemical Structure

CAS No. : 887686-02-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 4 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1][2]

SIRT6

89 μM (IC50)

SIRT2

751 μM (IC50)

SIRT1

1578 μM (IC50)

HBV

 

In Vitro

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[1].
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[1].
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[2].
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[3].

Western Blot Analysis[1]

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[2]

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.
In Vivo

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[2].

Animal Model: Male HBV transgenic mice (6-8-week-old)[2]
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.
Molecular Weight

366.32

Formula

C₁₉H₁₄N₂O₆

CAS No.

887686-02-4

SMILES

O=C(C1=CC(NC(C2=CC=CO2)=O)=CC=C1)NC3=CC(C(O)=O)=C(O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 103.3 mg/mL (281.99 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

OSS_128167SirtuinHBVHepatitis B virusSIRT6deacetylasediabetesimmuneanti-cancerH3K9acetylationGLUT-1TNF-αchemosensitizationantiviralPPARαInhibitorinhibitorinhibit

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OSS_128167
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