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Chemical Structure| 1001908-89-9 Chemical Structure| 1001908-89-9

Structure of SRT 2183
CAS No.: 1001908-89-9

Chemical Structure| 1001908-89-9

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SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1.

Synonyms: SRT 2183

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Product Details of SRT 2183

CAS No. :1001908-89-9
Formula : C27H24N4O2S
M.W : 468.57
SMILES Code : O=C(NC1=CC=CC=C1C2=CN3C(SC=C3CN4C[C@H](O)CC4)=N2)C5=CC=C6C=CC=CC6=C5
Synonyms :
SRT 2183
MDL No. :MFCD22419825

Safety of SRT 2183

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of SRT 2183

epigenetics

Isoform Comparison

Biological Activity

Description
SRT 2183 is a selective activator of Sirtuin-1 (SIRT1), with an EC1.5 of 0.36 μM[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
U87 20 μmol/L 1 hour Enhanced RSL3-induced SIRT1 activation and cell death Redox Biol. 2024 Feb;69:103030.
HUVEC 10 μM 24, 48, 72 h SRT2183 inhibited the growth of HUVEC cells. BMC Cancer. 2019 Jul 18;19(1):706.
SF767 10 μM 24, 48, 72 h SRT2183 inhibited the growth of SF767 cells. BMC Cancer. 2019 Jul 18;19(1):706.
SF539 10 μM 24, 48, 72 h SRT2183 inhibited the growth of SF539 cells. BMC Cancer. 2019 Jul 18;19(1):706.
U118 20 μmol/L 1 hour Enhanced RSL3-induced SIRT1 activation and cell death Redox Biol. 2024 Feb;69:103030.
U251 20 μmol/L 1 hour Enhanced RSL3-induced SIRT1 activation and cell death Redox Biol. 2024 Feb;69:103030.
U87 40 μmol/L 24 hours Induced SIRT1 upregulation, acetyl-p53 downregulation, and downregulation of SLC7A11 and GPX4 Redox Biol. 2024 Feb;69:103030.
U87MG 10 μM 24, 48, 72 h SRT2183 inhibited the growth of U87MG cells, induced cell cycle arrest and apoptosis, accompanied by upregulation of Bim and downregulation of Bcl-2 and Bcl-xL. BMC Cancer. 2019 Jul 18;19(1):706.
LN229 10 μM 24, 48, 72 h SRT2183 inhibited the growth of LN229 cells, induced cell cycle arrest and apoptosis, accompanied by upregulation of Bim and downregulation of Bcl-2 and Bcl-xL. BMC Cancer. 2019 Jul 18;19(1):706.
U2OS cells 10 μM SRT2183 was used as a positive control due to its good tolerance in cellular assays and it decreased the acetylation state of p53, a known SIRT1 substrate Nature. 2007 Nov 29;450(7170):712-6.
Mouse renal medullary interstitial cells 5-20 μM 8 hours SRT2183 dose-dependently increased COX2 expression. J Clin Invest. 2010 Apr;120(4):1056-68.
Ly3 cells 10 μM 24 hours SRT2183 reduced the acetylation levels of STAT3 and NF-κB in Ly3 cells and inhibited their DNA-binding activity. Cell Death Dis. 2013 May 16;4(5):e635.
MOLT-4 cells 10 μM 48 hours SRT2183 induced apoptosis in MOLT-4 cells with an IC50 of approximately 8.7 μM. Cell Death Dis. 2013 May 16;4(5):e635.
Nalm-6 cells 10 μM 48 hours SRT2183 significantly inhibited the proliferation of Nalm-6 cells with an IC50 of approximately 3.2 μM and induced apoptosis. Cell Death Dis. 2013 May 16;4(5):e635.
Reh cells 10 μM 48 hours SRT2183 significantly inhibited the proliferation of Reh cells with an IC50 of approximately 8.7 μM and induced apoptosis. Cell Death Dis. 2013 May 16;4(5):e635.
SK-OV-3 cells 1 μM 14 days To evaluate the effect of SRT2183 on cell growth, results showed that SRT2183 inhibited the growth of SK-OV-3 cells. Aging (Albany NY). 2020 Nov 20;12(23):24208-24218.
SW626 cells 1 μM 14 days To evaluate the effect of SRT2183 on cell growth, results showed that SRT2183 inhibited the growth of SW626 cells. Aging (Albany NY). 2020 Nov 20;12(23):24208-24218.
Caov-3 cells 1 μM 14 days To evaluate the effect of SRT2183 on cell growth, results showed that SRT2183 inhibited the growth of Caov-3 cells. Aging (Albany NY). 2020 Nov 20;12(23):24208-24218.
A2780 cells 1 μM 24 and 48 hours To evaluate the effect of SRT2183 on apoptosis, results showed that SRT2183 significantly increased apoptosis in A2780 cells. Aging (Albany NY). 2020 Nov 20;12(23):24208-24218.
OVCAR-3 cells 1 μM 24 and 48 hours To evaluate the effect of SRT2183 on apoptosis, results showed that SRT2183 significantly increased apoptosis in OVCAR-3 cells. Aging (Albany NY). 2020 Nov 20;12(23):24208-24218.
U87 and U251 glioma cells 10 μmol/L 1 h pretreatment followed by co-incubation with 450 nmol/L DPT for 24 h SRT2183 enhanced DPT-induced PARP1 activation and glioma cell death, as evidenced by increased LDH release, upregulation of PARP1 and PAR, and elevated levels of γ-H2AX and phospho-ATM. Acta Pharmacol Sin. 2023 Oct;44(10):2125-2138.
Bone marrow-derived macrophages (BMMs) 1 μM 4 days SRT2183 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival. PLoS One. 2015 Jul 30;10(7):e0134391.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.34mL

4.27mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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