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Chemical Structure| 304896-28-4 Chemical Structure| 304896-28-4

Structure of AGK2
CAS No.: 304896-28-4

Chemical Structure| 304896-28-4

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AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.

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Product Details of AGK2

CAS No. :304896-28-4
Formula : C23H13Cl2N3O2
M.W : 434.27
SMILES Code : O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3
MDL No. :MFCD01909444
InChI Key :SVENPFFEMUOOGK-SDNWHVSQSA-N
Pubchem ID :2130404

Safety of AGK2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AGK2

epigenetics

Isoform Comparison

Biological Activity

Target
  • SIRT2

    SIRT2, IC50:3.5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary hepatocytes 10 µM 12 hours hypoxia, 6 hours reoxygenation AGK2 treatment significantly reduced hypoxia-reoxygenation-induced apoptosis Hepatology. 2017 Jan;65(1):225-236.
Lung macrophages 20 ng/ml 24 hours To assess the expression of CCL17 and alternative activation markers JCI Insight. 2019 Feb 21;4(4):e124710.
HCCLM3 and SMMC-7721 cells 20 µM 8 hours To enhance FGL1 acetylation and reduce its protein levels. J Clin Invest. 2023 May 1;133(9):e164528.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice Busulfan-induced non-obstructive azoospermic mouse model Intraperitoneal injection 1 mg/kg Daily for five weeks To investigate the effect of AGK2 on the protective role of Npre in promoting spermatogenesis and alleviating ferroptosis in BU-treated mice. The results showed that AGK2 injection almost abolished the recovery effect of Npre on SIRT2 level, sperm concentration, and motility, and mitigated the protective effects of Npre on ferroptosis and spermatogenesis. Theranostics. 2024 Apr 15;14(6):2622-2636
C57Bl/6J mice NAFLD model Intraperitoneal injection 1 mg/kg/day Once daily for two weeks To test whether inhibition of SIRT2 affects the NR-induced anti-NAFLD effects in mice. The results showed that AGK2 treatment significantly compromised the therapeutic effects of NR on NAFLD, including improvements in hepatic steatosis, inflammation, and fibrosis. Theranostics. 2021 Feb 25;11(9):4381-4402
C57BL/6 mice and BALB/c mice Hepa 1-6 and H22 syngeneic cancer models Intraperitoneal injection 10 mg/kg Three times a week To suppress tumor growth and enhance the therapeutic effect of PD-L1 blockade. J Clin Invest. 2023 May 1;133(9):e164528.
Mice Allergic asthma model Intraperitoneal injection 10 mg/kg Days 12, 13, and 14, administered 30 minutes prior to DRA challenge To attenuate allergic inflammation by modulating alternative activation of macrophages and CCL17 production JCI Insight. 2019 Feb 21;4(4):e124710.
C57BL/6 mice HSV-1 infection model Intraperitoneal injection 40 mg/kg 1 day before and 1 day after HSV-1 infection AGK2 pretreatment significantly reduced HSV-1 RNA levels in the blood, brain, and liver tissues of mice and increased IFN-β production. EMBO Rep. 2023 Dec 6;24(12):e57500
C57BL/6 mice DSS-induced colitis Intraperitoneal injection 50 mg/kg Three times via intraperitoneal (IP) injection AGK2 showed protection in the IBD mouse model Proc Natl Acad Sci U S A. 2024 Apr 30;121(18):e2319833121

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.51mL

2.30mL

1.15mL

23.03mL

4.61mL

2.30mL

References

 

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